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Inavolisib - Wikipedia

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class="vector-toc-numb">2</span> <span>Side effects</span> </div> </a> <ul id="toc-Side_effects-sublist" class="vector-toc-list"> </ul> </li> <li id="toc-History" class="vector-toc-list-item vector-toc-level-1 vector-toc-list-item-expanded"> <a class="vector-toc-link" href="#History"> <div class="vector-toc-text"> <span class="vector-toc-numb">3</span> <span>History</span> </div> </a> <ul id="toc-History-sublist" class="vector-toc-list"> </ul> </li> <li id="toc-Structure,_reactivity,_and_synthesis" class="vector-toc-list-item vector-toc-level-1 vector-toc-list-item-expanded"> <a class="vector-toc-link" href="#Structure,_reactivity,_and_synthesis"> <div class="vector-toc-text"> <span class="vector-toc-numb">4</span> <span>Structure, reactivity, and synthesis</span> </div> </a> <ul id="toc-Structure,_reactivity,_and_synthesis-sublist" class="vector-toc-list"> </ul> </li> <li id="toc-Metabolism_and_biotransformation" class="vector-toc-list-item vector-toc-level-1 vector-toc-list-item-expanded"> <a class="vector-toc-link" href="#Metabolism_and_biotransformation"> <div class="vector-toc-text"> <span class="vector-toc-numb">5</span> <span>Metabolism and biotransformation</span> </div> </a> <ul id="toc-Metabolism_and_biotransformation-sublist" class="vector-toc-list"> </ul> </li> <li id="toc-Molecular_mechanisms_of_action" class="vector-toc-list-item vector-toc-level-1 vector-toc-list-item-expanded"> <a class="vector-toc-link" href="#Molecular_mechanisms_of_action"> <div class="vector-toc-text"> <span class="vector-toc-numb">6</span> <span>Molecular mechanisms of action</span> </div> </a> <ul id="toc-Molecular_mechanisms_of_action-sublist" class="vector-toc-list"> </ul> </li> <li id="toc-Toxicity" class="vector-toc-list-item vector-toc-level-1 vector-toc-list-item-expanded"> <a class="vector-toc-link" href="#Toxicity"> <div class="vector-toc-text"> <span class="vector-toc-numb">7</span> <span>Toxicity</span> </div> </a> <ul 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data-unpinned-container-id="vector-appearance-unpinned-container" > <div class="vector-pinnable-header-label">Appearance</div> <button class="vector-pinnable-header-toggle-button vector-pinnable-header-pin-button" data-event-name="pinnable-header.vector-appearance.pin">move to sidebar</button> <button class="vector-pinnable-header-toggle-button vector-pinnable-header-unpin-button" data-event-name="pinnable-header.vector-appearance.unpin">hide</button> </div> </div> </div> </nav> </div> </div> <div id="bodyContent" class="vector-body" aria-labelledby="firstHeading" data-mw-ve-target-container> <div class="vector-body-before-content"> <div class="mw-indicators"> </div> <div id="siteSub" class="noprint">From Wikipedia, the free encyclopedia</div> </div> <div id="contentSub"><div id="mw-content-subtitle"></div></div> <div id="mw-content-text" class="mw-body-content"><div class="mw-content-ltr mw-parser-output" lang="en" dir="ltr"><div class="shortdescription nomobile noexcerpt noprint searchaux" style="display:none">Chemical compound</div> <p class="mw-empty-elt"> </p> <style data-mw-deduplicate="TemplateStyles:r1257001546">.mw-parser-output .infobox-subbox{padding:0;border:none;margin:-3px;width:auto;min-width:100%;font-size:100%;clear:none;float:none;background-color:transparent}.mw-parser-output .infobox-3cols-child{margin:auto}.mw-parser-output .infobox .navbar{font-size:100%}@media screen{html.skin-theme-clientpref-night .mw-parser-output .infobox-full-data:not(.notheme)>div:not(.notheme)[style]{background:#1f1f23!important;color:#f8f9fa}}@media screen and (prefers-color-scheme:dark){html.skin-theme-clientpref-os .mw-parser-output .infobox-full-data:not(.notheme) div:not(.notheme){background:#1f1f23!important;color:#f8f9fa}}@media(min-width:640px){body.skin--responsive .mw-parser-output .infobox-table{display:table!important}body.skin--responsive .mw-parser-output .infobox-table>caption{display:table-caption!important}body.skin--responsive .mw-parser-output .infobox-table>tbody{display:table-row-group}body.skin--responsive .mw-parser-output .infobox-table tr{display:table-row!important}body.skin--responsive .mw-parser-output .infobox-table th,body.skin--responsive .mw-parser-output .infobox-table td{padding-left:inherit;padding-right:inherit}}</style><table class="infobox" style="border-spacing:2px;"><caption class="infobox-title"><span title="International nonproprietary name (INN): Inavolisib">Inavolisib</span></caption><tbody><tr><td colspan="2" class="infobox-image notheme" style="background-color: #f8f9fa;"><span class="mw-default-size" typeof="mw:File/Frameless"><a href="/wiki/File:Inavolisib.svg" class="mw-file-description"><img src="//upload.wikimedia.org/wikipedia/commons/thumb/2/28/Inavolisib.svg/220px-Inavolisib.svg.png" decoding="async" width="220" height="105" class="mw-file-element" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/2/28/Inavolisib.svg/330px-Inavolisib.svg.png 1.5x, //upload.wikimedia.org/wikipedia/commons/thumb/2/28/Inavolisib.svg/440px-Inavolisib.svg.png 2x" data-file-width="840" data-file-height="400" /></a></span></td></tr><tr><th colspan="2" class="infobox-header" style="background:#ddd">Clinical data</th></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;"><a href="/wiki/Drug_nomenclature#Trade_names" title="Drug nomenclature">Trade names</a></th><td class="infobox-data">Itovebi</td></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;">Other names</th><td class="infobox-data">GDC-0077, RG6114, Ro7113755</td></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;"><a href="/wiki/American_Society_of_Health-System_Pharmacists" title="American Society of Health-System Pharmacists">AHFS</a>/<a href="/wiki/Drugs.com" title="Drugs.com">Drugs.com</a></th><td class="infobox-data"><span title="www.drugs.com"><a rel="nofollow" class="external text" href="https://www.drugs.com/Itovebi.html">Itovebi</a></span></td></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;"><a href="/wiki/Regulation_of_therapeutic_goods" title="Regulation of therapeutic goods">License data</a></th><td class="infobox-data"><style data-mw-deduplicate="TemplateStyles:r1126788409">.mw-parser-output .plainlist ol,.mw-parser-output .plainlist ul{line-height:inherit;list-style:none;margin:0;padding:0}.mw-parser-output .plainlist ol li,.mw-parser-output .plainlist ul li{margin-bottom:0}</style><div class="plainlist"> <ul><li><small><abbr class="country-name" title="United States">US</abbr></small>&#160;<a href="/wiki/DailyMed" title="DailyMed">DailyMed</a>:&#160;<span title="dailymed.nlm.nih.gov"><a rel="nofollow" class="external text" href="https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&amp;query=Inavolisib">Inavolisib</a></span></li></ul></div> </td></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;"><a href="/wiki/Route_of_administration" title="Route of administration">Routes of<br />administration</a></th><td class="infobox-data"><a href="/wiki/By_mouth" class="mw-redirect" title="By mouth">By mouth</a></td></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;"><a href="/wiki/Drug_class" title="Drug class">Drug class</a></th><td class="infobox-data"><a href="/wiki/PI3K_inhibitor" class="mw-redirect" title="PI3K inhibitor">PI3K inhibitor</a></td></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;"><a href="/wiki/Anatomical_Therapeutic_Chemical_Classification_System" title="Anatomical Therapeutic Chemical Classification System">ATC code</a></th><td class="infobox-data"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1126788409"><div class="plainlist"><ul><li>None</li></ul></div></td></tr><tr><th colspan="2" class="infobox-header" style="background:#ddd">Legal status</th></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;"><a href="/wiki/Regulation_of_therapeutic_goods" title="Regulation of therapeutic goods">Legal status</a></th><td class="infobox-data"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1126788409"><div class="plainlist"> <ul><li><small><abbr class="country-name" title="United States">US</abbr>:</small>&#x20;<a href="/wiki/Prescription_drug" title="Prescription drug">℞-only</a><sup id="cite_ref-Itovebi_FDA_label_1-0" class="reference"><a href="#cite_note-Itovebi_FDA_label-1"><span class="cite-bracket">&#91;</span>1<span class="cite-bracket">&#93;</span></a></sup></li></ul></div> </td></tr><tr><th colspan="2" class="infobox-header" style="background:#ddd">Identifiers</th></tr><tr><td colspan="2" class="infobox-full-data"><div class="collapsible-list mw-collapsible mw-collapsed" style="text-align: left;"> <div style="line-height: 1.6em; font-weight: bold;"><div><a href="/wiki/IUPAC_nomenclature_of_chemistry" title="IUPAC nomenclature of chemistry">IUPAC name</a></div></div> <ul class="mw-collapsible-content" style="margin-top: 0; margin-bottom: 0; line-height: inherit; list-style: none; margin-left: 0; word-break:break-all; text-align:left; padding-left:1.5em; text-indent:-1.5em;"><li style="line-height: inherit; margin: 0"><div style="font-size: 97%;">(2<i>S</i>)-2-[[2-[(4<i>S</i>)-4-(difluoromethyl)-2-oxo-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]amino]propanamide</div></li></ul> </div></td></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;"><a href="/wiki/CAS_Registry_Number" title="CAS Registry Number">CAS Number</a></th><td class="infobox-data"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1126788409"><div class="plainlist"><ul><li><span title="commonchemistry.cas.org"><a rel="nofollow" class="external text" href="https://commonchemistry.cas.org/detail?cas_rn=2060571-02-8">2060571-02-8</a></span></li></ul></div></td></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;"><a href="/wiki/PubChem#CID" title="PubChem">PubChem</a> <span style="font-weight:normal"><abbr title="Compound ID">CID</abbr></span></th><td class="infobox-data"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1126788409"><div class="plainlist"><ul><li><span title="pubchem.ncbi.nlm.nih.gov"><a rel="nofollow" class="external text" href="https://pubchem.ncbi.nlm.nih.gov/compound/124173720">124173720</a></span></li></ul></div></td></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;"><a href="/wiki/Guide_to_Pharmacology" title="Guide to Pharmacology">IUPHAR/BPS</a></th><td class="infobox-data"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1126788409"><div class="plainlist"><ul><li><span title="www.guidetopharmacology.org"><a rel="nofollow" class="external text" href="https://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=9636">9636</a></span></li></ul></div></td></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;"><a href="/wiki/DrugBank" title="DrugBank">DrugBank</a></th><td class="infobox-data"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1126788409"><div class="plainlist"><ul><li><span title="www.drugbank.ca"><a rel="nofollow" class="external text" href="https://www.drugbank.ca/drugs/DB15275">DB15275</a></span></li></ul></div></td></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;"><a href="/wiki/ChemSpider" title="ChemSpider">ChemSpider</a></th><td class="infobox-data"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1126788409"><div class="plainlist"><ul><li><span title="www.chemspider.com"><a rel="nofollow" class="external text" href="https://www.chemspider.com/Chemical-Structure.59718498.html">59718498</a></span></li></ul></div></td></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;"><a href="/wiki/Unique_Ingredient_Identifier" title="Unique Ingredient Identifier">UNII</a></th><td class="infobox-data"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1126788409"><div class="plainlist"><ul><li><span title="precision.fda.gov"><a rel="nofollow" class="external text" href="https://precision.fda.gov/uniisearch/srs/unii/L4C1UY2NYH">L4C1UY2NYH</a></span></li></ul></div></td></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;"><a href="/wiki/KEGG" title="KEGG">KEGG</a></th><td class="infobox-data"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1126788409"><div class="plainlist"><ul><li><span title="www.kegg.jp"><a rel="nofollow" class="external text" href="https://www.kegg.jp/entry/D11942">D11942</a></span></li></ul></div></td></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;"><a href="/wiki/ChEMBL" title="ChEMBL">ChEMBL</a></th><td class="infobox-data"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1126788409"><div class="plainlist"><ul><li><span title="www.ebi.ac.uk"><a rel="nofollow" class="external text" href="https://www.ebi.ac.uk/chembl/explore/compound/ChEMBL4650215">ChEMBL4650215</a></span></li></ul></div></td></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;"><a href="/wiki/Protein_Data_Bank" title="Protein Data Bank">PDB ligand</a></th><td class="infobox-data"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1126788409"><div class="plainlist"><ul><li>X3N (<span title="www.ebi.ac.uk"><a rel="nofollow" class="external text" href="https://www.ebi.ac.uk/pdbe-srv/PDBeXplore/ligand/?ligand=X3N">PDBe</a></span>, <span title="www.rcsb.org"><a rel="nofollow" class="external text" href="https://www.rcsb.org/ligand/X3N">RCSB&#160;PDB</a></span>)</li></ul></div></td></tr><tr><th colspan="2" class="infobox-header" style="background:#ddd">Chemical and physical data</th></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;"><a href="/wiki/Chemical_formula" title="Chemical formula">Formula</a></th><td class="infobox-data"><span title="Carbon">C</span><sub>18</sub><span title="Hydrogen">H</span><sub>19</sub><span title="Fluorine">F</span><sub>2</sub><span title="Nitrogen">N</span><sub>5</sub><span title="Oxygen">O</span><sub>4</sub></td></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;"><a href="/wiki/Molar_mass" title="Molar mass">Molar mass</a></th><td class="infobox-data"><span class="nowrap"><span data-sort-value="7002407378000000000♠"></span>407.378</span>&#160;g·mol<sup>−1</sup></td></tr><tr><th scope="row" class="infobox-label" style="line-height:1.2em;">3D model (<a href="/wiki/JSmol" class="mw-redirect" title="JSmol">JSmol</a>)</th><td class="infobox-data"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1126788409"><div class="plainlist"><ul><li><span title="chemapps.stolaf.edu (3D interactive model)"><a rel="nofollow" class="external text" href="https://chemapps.stolaf.edu/jmol/jmol.php?model=C%5BC%40%40H%5D%28C%28%3DO%29N%29NC1%3DCC2%3DC%28C%3DC1%29C3%3DNC%28%3DCN3CCO2%29N4%5BC%40%40H%5D%28COC4%3DO%29C%28F%29F">Interactive image</a></span></li></ul></div></td></tr><tr><td colspan="2" class="infobox-full-data"><div class="collapsible-list mw-collapsible mw-collapsed" style="text-align: left;"> <div style="line-height: 1.6em; font-weight: bold;"><div><a href="/wiki/Simplified_molecular-input_line-entry_system" class="mw-redirect" title="Simplified molecular-input line-entry system">SMILES</a></div></div> <ul class="mw-collapsible-content" style="margin-top: 0; margin-bottom: 0; line-height: inherit; list-style: none; margin-left: 0; word-break:break-all;"><li style="line-height: inherit; margin: 0"><div style="word-wrap:break-word; text-indent:-1.5em; text-align:left; padding-left:1.5em; font-size:97%; line-height:120%;">C[C@@H](C(=O)N)NC1=CC2=C(C=C1)C3=NC(=CN3CCO2)N4[C@@H](COC4=O)C(F)F</div></li></ul> </div></td></tr><tr><td colspan="2" class="infobox-full-data"><div class="collapsible-list mw-collapsible mw-collapsed" style="text-align: left;"> <div style="line-height: 1.6em; font-weight: bold;"><div><a href="/wiki/International_Chemical_Identifier" title="International Chemical Identifier">InChI</a></div></div> <ul class="mw-collapsible-content" style="margin-top: 0; margin-bottom: 0; line-height: inherit; list-style: none; margin-left: 0; word-break:break-all;"><li style="line-height: inherit; margin: 0"><div style="word-wrap:break-word; text-indent:-1.5em; text-align:left; padding-left:1.5em; font-size:97%; line-height:120%;">InChI=1S/C18H19F2N5O4/c1-9(16(21)26)22-10-2-3-11-13(6-10)28-5-4-24-7-14(23-17(11)24)25-12(15(19)20)8-29-18(25)27/h2-3,6-7,9,12,15,22H,4-5,8H2,1H3,(H2,21,26)/t9-,12-/m0/s1</div></li><li style="line-height: inherit; margin: 0"><div style="word-wrap:break-word; text-indent:-1.5em; text-align:left; padding-left:1.5em; font-size:97%; line-height:120%;">Key:SGEUNORSOZVTOL-CABZTGNLSA-N</div></li></ul> </div></td></tr></tbody></table> <p><b>Inavolisib</b>, sold under the brand name <b>Itovebi</b>, is an <a href="/wiki/Anti-cancer_medication" class="mw-redirect" title="Anti-cancer medication">anti-cancer medication</a> used for the treatment of breast cancer.<sup id="cite_ref-Itovebi_FDA_label_1-1" class="reference"><a href="#cite_note-Itovebi_FDA_label-1"><span class="cite-bracket">&#91;</span>1<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-FDA_20241010_2-0" class="reference"><a href="#cite_note-FDA_20241010-2"><span class="cite-bracket">&#91;</span>2<span class="cite-bracket">&#93;</span></a></sup> It is an <a href="/wiki/Phosphoinositide_3-kinase_inhibitor" title="Phosphoinositide 3-kinase inhibitor">inhibitor</a> and degrader of mutant <a href="/wiki/Phosphoinositide_3-kinase" title="Phosphoinositide 3-kinase">phosphatidylinositol 3-kinase (PI3K) alpha</a>.<sup id="cite_ref-Hanan_2022_3-0" class="reference"><a href="#cite_note-Hanan_2022-3"><span class="cite-bracket">&#91;</span>3<span class="cite-bracket">&#93;</span></a></sup> The PI3K-mediated signalling pathway has shown to play an important role in the development of tumours as dysregulation is commonly associated with tumour growth and resistance to antineoplastic agents and radiotherapy.<sup id="cite_ref-CID_124173720_4-0" class="reference"><a href="#cite_note-CID_124173720-4"><span class="cite-bracket">&#91;</span>4<span class="cite-bracket">&#93;</span></a></sup> </p><p>The most common adverse reactions include decreased neutrophils, decreased hemoglobin, increased fasting glucose, decreased platelets, decreased lymphocytes, stomatitis, diarrhea, decreased calcium, fatigue, decreased potassium, increased creatinine, increased ALT, nausea, decreased sodium, decreased magnesium, rash, decreased appetite, COVID-19 infection, and headache.<sup id="cite_ref-FDA_20241010_2-1" class="reference"><a href="#cite_note-FDA_20241010-2"><span class="cite-bracket">&#91;</span>2<span class="cite-bracket">&#93;</span></a></sup> </p><p>Inavolisib was approved by the US <a href="/wiki/Food_and_Drug_Administration" title="Food and Drug Administration">Food and Drug Administration</a> (FDA) for treatment of <a href="/wiki/PIK3CA" class="mw-redirect" title="PIK3CA">PIK3CA</a>-mutant breast cancer in October 2024.<sup id="cite_ref-FDA_20241010_2-2" class="reference"><a href="#cite_note-FDA_20241010-2"><span class="cite-bracket">&#91;</span>2<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-:0_5-0" class="reference"><a href="#cite_note-:0-5"><span class="cite-bracket">&#91;</span>5<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-6" class="reference"><a href="#cite_note-6"><span class="cite-bracket">&#91;</span>6<span class="cite-bracket">&#93;</span></a></sup> </p> <meta property="mw:PageProp/toc" /> <div class="mw-heading mw-heading2"><h2 id="Medical_uses">Medical uses</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inavolisib&amp;action=edit&amp;section=1" title="Edit section: Medical uses"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>Inavolisib is <a href="/wiki/Indicated" class="mw-redirect" title="Indicated">indicated</a> in combination with <a href="/wiki/Palbociclib" title="Palbociclib">palbociclib</a> and <a href="/wiki/Fulvestrant" title="Fulvestrant">fulvestrant</a> for the treatment of adults with endocrine-resistant, PIK3CA-mutated, hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, locally advanced or metastatic breast cancer, as detected by an FDA-approved test, following recurrence on or after completing adjuvant endocrine therapy.<sup id="cite_ref-FDA_20241010_2-3" class="reference"><a href="#cite_note-FDA_20241010-2"><span class="cite-bracket">&#91;</span>2<span class="cite-bracket">&#93;</span></a></sup> </p> <div class="mw-heading mw-heading2"><h2 id="Side_effects">Side effects</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inavolisib&amp;action=edit&amp;section=2" title="Edit section: Side effects"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>The most common adverse reactions include decreased neutrophils, decreased hemoglobin, increased fasting glucose, decreased platelets, decreased lymphocytes, stomatitis, diarrhea, decreased calcium, fatigue, decreased potassium, increased creatinine, increased ALT, nausea, decreased sodium, decreased magnesium, rash, decreased appetite, COVID-19 infection, and headache.<sup id="cite_ref-FDA_20241010_2-4" class="reference"><a href="#cite_note-FDA_20241010-2"><span class="cite-bracket">&#91;</span>2<span class="cite-bracket">&#93;</span></a></sup> </p> <div class="mw-heading mw-heading2"><h2 id="History">History</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inavolisib&amp;action=edit&amp;section=3" title="Edit section: History"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>Efficacy was evaluated in INAVO120 (NCT04191499), a randomized, double-blind, placebo-controlled, multicenter trial in 325 participants with endocrine-resistant, PIK3CA-mutated HR-positive, HER2-negative locally advanced or metastatic breast cancer whose disease progressed during or within twelve months of completing adjuvant endocrine therapy and who had not received prior systemic therapy for locally advanced or metastatic disease.<sup id="cite_ref-FDA_20241010_2-5" class="reference"><a href="#cite_note-FDA_20241010-2"><span class="cite-bracket">&#91;</span>2<span class="cite-bracket">&#93;</span></a></sup> Primary endocrine resistance was defined as relapse while on the first two years of adjuvant endocrine therapy (ET) and secondary endocrine resistance was defined as relapse while on adjuvant ET after at least two years or relapse within twelve months of completing adjuvant ET.<sup id="cite_ref-FDA_20241010_2-6" class="reference"><a href="#cite_note-FDA_20241010-2"><span class="cite-bracket">&#91;</span>2<span class="cite-bracket">&#93;</span></a></sup> </p> <div class="mw-heading mw-heading2"><h2 id="Structure,_reactivity,_and_synthesis"><span id="Structure.2C_reactivity.2C_and_synthesis"></span>Structure, reactivity, and synthesis</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inavolisib&amp;action=edit&amp;section=4" title="Edit section: Structure, reactivity, and synthesis"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>Inavolisib is a synthetic, organic, small compound (the full structure can be seen <a rel="nofollow" class="external text" href="https://www.guidetopharmacology.org/GRAC/LigandDisplayForward?tab=structure&amp;ligandId=9636">here</a>).<sup id="cite_ref-IUPHAR/BPS_Inavolisib_7-0" class="reference"><a href="#cite_note-IUPHAR/BPS_Inavolisib-7"><span class="cite-bracket">&#91;</span>7<span class="cite-bracket">&#93;</span></a></sup> When binding to phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit alpha (p110α), inavolisib’s carbonyl group can accept a <a href="/wiki/Hydrogen_bond" title="Hydrogen bond">hydrogen bond</a> from the Tyr836 (conserved) in p110α. The difluoromethyl group can interact with the hydroxyl group presented on Ser774 (conserved) in p110α, which is 3.2<a href="/wiki/Angstrom" title="Angstrom">Å</a> nearer than of which on the equivalent residue Ser754 in p110δ. Additionally, the amide group can interact with Gln859 (non-conserved). This results in a very high selectivity regarding PI3Kα isoforms.<sup id="cite_ref-Hanan_2022_3-1" class="reference"><a href="#cite_note-Hanan_2022-3"><span class="cite-bracket">&#91;</span>3<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-8" class="reference"><a href="#cite_note-8"><span class="cite-bracket">&#91;</span>8<span class="cite-bracket">&#93;</span></a></sup> </p><p>Compared to similar PI3K inhibiting compounds, inavolisib has a higher thermodynamic aqueous solubility that proved advantageous in the formulation process and aiding greater consistency in predictions of absorption.<sup id="cite_ref-Hanan_2022_3-2" class="reference"><a href="#cite_note-Hanan_2022-3"><span class="cite-bracket">&#91;</span>3<span class="cite-bracket">&#93;</span></a></sup> </p><p>Inavolisibcan be developed as a derivative of <a href="/wiki/Oxazole" title="Oxazole">1,3-oxazole</a><sup id="cite_ref-9" class="reference"><a href="#cite_note-9"><span class="cite-bracket">&#91;</span>9<span class="cite-bracket">&#93;</span></a></sup> or by means of stereo-controlled N-arylation of alpha-amino acids.<sup id="cite_ref-10" class="reference"><a href="#cite_note-10"><span class="cite-bracket">&#91;</span>10<span class="cite-bracket">&#93;</span></a></sup> </p> <div class="mw-heading mw-heading2"><h2 id="Metabolism_and_biotransformation">Metabolism and biotransformation</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inavolisib&amp;action=edit&amp;section=5" title="Edit section: Metabolism and biotransformation"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>Inavolisib is orally administered, though there is little knowledge about its metabolism.<sup id="cite_ref-DB15275_11-0" class="reference"><a href="#cite_note-DB15275-11"><span class="cite-bracket">&#91;</span>11<span class="cite-bracket">&#93;</span></a></sup><sup class="noprint Inline-Template" style="white-space:nowrap;">&#91;<i><a href="/wiki/Wikipedia:Identifying_reliable_sources_(medicine)" title="Wikipedia:Identifying reliable sources (medicine)"><span title="Material near this tag may rely on an unreliable or less reliable medical source. (October 2024)">unreliable medical source?</span></a></i>&#93;</sup> However, absorption, metabolism, and excretion data of <a href="/wiki/Taselisib" title="Taselisib">taselisib</a>, a molecule with a related chemical scaffold, suggest moderately slow absorption into the systemic circulation, metabolism to play a minor role in drug clearance, and biliary excretion to be the main route of excretion.<sup id="cite_ref-12" class="reference"><a href="#cite_note-12"><span class="cite-bracket">&#91;</span>12<span class="cite-bracket">&#93;</span></a></sup> </p> <div class="mw-heading mw-heading2"><h2 id="Molecular_mechanisms_of_action">Molecular mechanisms of action</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inavolisib&amp;action=edit&amp;section=6" title="Edit section: Molecular mechanisms of action"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>Inavolisib is a selective PI3K-p110α (<a href="/wiki/P110%CE%B1" title="P110α">PIK3CA</a>) inhibitor, which may offer antineoplastic functionality.<sup id="cite_ref-IUPHAR/BPS_Inavolisib_7-1" class="reference"><a href="#cite_note-IUPHAR/BPS_Inavolisib-7"><span class="cite-bracket">&#91;</span>7<span class="cite-bracket">&#93;</span></a></sup> Therefore, it may serve as a new addition to combination therapy with conventional cancer treatment, such as chemotherapy. Combining inavolisib with <a href="/wiki/Palbociclib" title="Palbociclib">palbociclib</a> and <a href="/wiki/Fulvestrant" title="Fulvestrant">fulvestrant</a> might improve treatment of <a href="/wiki/Breast_cancer" title="Breast cancer">breast cancer</a>.<sup id="cite_ref-13" class="reference"><a href="#cite_note-13"><span class="cite-bracket">&#91;</span>13<span class="cite-bracket">&#93;</span></a></sup> </p><p>Next to its inhibitory enzymatic ability, it is suggested that inavolisib binds to - and activates degradation of - mutated forms of p110α. Members of the PI3K family regulate cellular processes such as cell growth and proliferation, survival, remodelling, and intracellular transport of organelles.<sup id="cite_ref-14" class="reference"><a href="#cite_note-14"><span class="cite-bracket">&#91;</span>14<span class="cite-bracket">&#93;</span></a></sup> PI3K also plays an essential role for the immune system. </p><p>The class I isoform PI3K alpha (PI3Kα) is often times expressed in solid tumours through gene amplification or activated mutations.<sup id="cite_ref-Hanan_2022_3-3" class="reference"><a href="#cite_note-Hanan_2022-3"><span class="cite-bracket">&#91;</span>3<span class="cite-bracket">&#93;</span></a></sup> Mutations in PI3Kα can often be found in cancer cells, especially HR+ breast cancer, which causes a disruption of the PI3K pathway. This leads to increased tumour growth and metastasis. One of the most common mutations can be found in <i>PIK3CA</i>, which plays a significant role in tumour cell proliferation. </p><p>In preclinical studies, inavolisib has shown to specifically initiate the degradation of this p110α oncogene with the help of proteasomes.<sup id="cite_ref-15" class="reference"><a href="#cite_note-15"><span class="cite-bracket">&#91;</span>15<span class="cite-bracket">&#93;</span></a></sup> After binding to the mutant PI3Kα, inavolisib blocks phosphorylation of PIP<sub>2</sub> to PIP<sub>3</sub>, thereby stopping downstream signalling.<sup id="cite_ref-Genentech_Inavolisib_16-0" class="reference"><a href="#cite_note-Genentech_Inavolisib-16"><span class="cite-bracket">&#91;</span>16<span class="cite-bracket">&#93;</span></a></sup> </p><p>Consequently, biomarkers in the PI3K pathway are reduced, cell proliferation inhibited, and the rate of <i>PIK3CA</i>-mutant breast cancer apoptosis increased (in comparison to the wild type). The exact mechanism of action of inhibitors like inavolisib on mutated PI3Kα and the inhibitors' influence on mutant structures are still unknown.<sup id="cite_ref-17" class="reference"><a href="#cite_note-17"><span class="cite-bracket">&#91;</span>17<span class="cite-bracket">&#93;</span></a></sup> </p> <div class="mw-heading mw-heading2"><h2 id="Toxicity">Toxicity</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inavolisib&amp;action=edit&amp;section=7" title="Edit section: Toxicity"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>Inavolisib is able to induce a cytotoxic response but this is directed towards tumour cells that contain the PI3K mutation, thereby inhibiting further tumour growth and leading to cell loss.<sup id="cite_ref-18" class="reference"><a href="#cite_note-18"><span class="cite-bracket">&#91;</span>18<span class="cite-bracket">&#93;</span></a></sup> </p> <div class="mw-heading mw-heading2"><h2 id="Society_and_culture">Society and culture</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inavolisib&amp;action=edit&amp;section=8" title="Edit section: Society and culture"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <div class="mw-heading mw-heading3"><h3 id="Legal_status">Legal status</h3><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inavolisib&amp;action=edit&amp;section=9" title="Edit section: Legal status"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>In October 2024, the US <a href="/wiki/Food_and_Drug_Administration" title="Food and Drug Administration">Food and Drug Administration</a> FDA approved inavolisib for the treatment of <a href="/wiki/PIK3CA" class="mw-redirect" title="PIK3CA">PIK3CA</a>-mutant breast cancer based on the results from the INAVO120 trial.<sup id="cite_ref-FDA_20241010_2-7" class="reference"><a href="#cite_note-FDA_20241010-2"><span class="cite-bracket">&#91;</span>2<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-Novel_Drug_Approvals_for_2024_19-0" class="reference"><a href="#cite_note-Novel_Drug_Approvals_for_2024-19"><span class="cite-bracket">&#91;</span>19<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-20" class="reference"><a href="#cite_note-20"><span class="cite-bracket">&#91;</span>20<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-21" class="reference"><a href="#cite_note-21"><span class="cite-bracket">&#91;</span>21<span class="cite-bracket">&#93;</span></a></sup> The drug application was granted <a href="/wiki/Priority_review" title="Priority review">priority review</a> and <a href="/wiki/Breakthrough_therapy" title="Breakthrough therapy">breakthrough therapy</a> designations by the FDA.<sup id="cite_ref-FDA_20241010_2-8" class="reference"><a href="#cite_note-FDA_20241010-2"><span class="cite-bracket">&#91;</span>2<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-:0_5-1" class="reference"><a href="#cite_note-:0-5"><span class="cite-bracket">&#91;</span>5<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-22" class="reference"><a href="#cite_note-22"><span class="cite-bracket">&#91;</span>22<span class="cite-bracket">&#93;</span></a></sup> </p> <div class="mw-heading mw-heading3"><h3 id="Names">Names</h3><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inavolisib&amp;action=edit&amp;section=10" title="Edit section: Names"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>Inavolisib is the <a href="/wiki/International_nonproprietary_name" title="International nonproprietary name">international nonproprietary name</a>.<sup id="cite_ref-23" class="reference"><a href="#cite_note-23"><span class="cite-bracket">&#91;</span>23<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-24" class="reference"><a href="#cite_note-24"><span class="cite-bracket">&#91;</span>24<span class="cite-bracket">&#93;</span></a></sup> </p><p>Inavolisib is sold under the brand name Itovebi.<sup id="cite_ref-FDA_20241010_2-9" class="reference"><a href="#cite_note-FDA_20241010-2"><span class="cite-bracket">&#91;</span>2<span class="cite-bracket">&#93;</span></a></sup> </p> <div class="mw-heading mw-heading2"><h2 id="Research">Research</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inavolisib&amp;action=edit&amp;section=11" title="Edit section: Research"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>Due to inavolisib’s ability to inhibit the PI3K pathway through <a href="/wiki/HER2" title="HER2">HER2</a>-dependent degradation, it is undergoing clinical trials to potentially make use of it as an antineoplastic (anti-cancer) drug to treat <a href="/wiki/Breast_cancer" title="Breast cancer">breast cancer</a>.<sup id="cite_ref-Hanan_2022_3-4" class="reference"><a href="#cite_note-Hanan_2022-3"><span class="cite-bracket">&#91;</span>3<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-Vanhaesebroeck_2022_25-0" class="reference"><a href="#cite_note-Vanhaesebroeck_2022-25"><span class="cite-bracket">&#91;</span>25<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-Genentech_Inavolisib_16-1" class="reference"><a href="#cite_note-Genentech_Inavolisib-16"><span class="cite-bracket">&#91;</span>16<span class="cite-bracket">&#93;</span></a></sup> </p> <div class="mw-heading mw-heading2"><h2 id="References">References</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inavolisib&amp;action=edit&amp;section=12" title="Edit section: References"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <style data-mw-deduplicate="TemplateStyles:r1239543626">.mw-parser-output .reflist{margin-bottom:0.5em;list-style-type:decimal}@media screen{.mw-parser-output .reflist{font-size:90%}}.mw-parser-output .reflist .references{font-size:100%;margin-bottom:0;list-style-type:inherit}.mw-parser-output .reflist-columns-2{column-width:30em}.mw-parser-output .reflist-columns-3{column-width:25em}.mw-parser-output .reflist-columns{margin-top:0.3em}.mw-parser-output .reflist-columns ol{margin-top:0}.mw-parser-output .reflist-columns li{page-break-inside:avoid;break-inside:avoid-column}.mw-parser-output .reflist-upper-alpha{list-style-type:upper-alpha}.mw-parser-output .reflist-upper-roman{list-style-type:upper-roman}.mw-parser-output .reflist-lower-alpha{list-style-type:lower-alpha}.mw-parser-output .reflist-lower-greek{list-style-type:lower-greek}.mw-parser-output .reflist-lower-roman{list-style-type:lower-roman}</style><div class="reflist"> <div class="mw-references-wrap mw-references-columns"><ol class="references"> <li id="cite_note-Itovebi_FDA_label-1"><span class="mw-cite-backlink">^ <a href="#cite_ref-Itovebi_FDA_label_1-0"><sup><i><b>a</b></i></sup></a> <a href="#cite_ref-Itovebi_FDA_label_1-1"><sup><i><b>b</b></i></sup></a></span> <span class="reference-text"><style data-mw-deduplicate="TemplateStyles:r1238218222">.mw-parser-output cite.citation{font-style:inherit;word-wrap:break-word}.mw-parser-output .citation q{quotes:"\"""\"""'""'"}.mw-parser-output .citation:target{background-color:rgba(0,127,255,0.133)}.mw-parser-output .id-lock-free.id-lock-free a{background:url("//upload.wikimedia.org/wikipedia/commons/6/65/Lock-green.svg")right 0.1em center/9px no-repeat}.mw-parser-output .id-lock-limited.id-lock-limited a,.mw-parser-output .id-lock-registration.id-lock-registration a{background:url("//upload.wikimedia.org/wikipedia/commons/d/d6/Lock-gray-alt-2.svg")right 0.1em center/9px no-repeat}.mw-parser-output .id-lock-subscription.id-lock-subscription a{background:url("//upload.wikimedia.org/wikipedia/commons/a/aa/Lock-red-alt-2.svg")right 0.1em center/9px no-repeat}.mw-parser-output .cs1-ws-icon a{background:url("//upload.wikimedia.org/wikipedia/commons/4/4c/Wikisource-logo.svg")right 0.1em center/12px no-repeat}body:not(.skin-timeless):not(.skin-minerva) .mw-parser-output .id-lock-free a,body:not(.skin-timeless):not(.skin-minerva) .mw-parser-output .id-lock-limited a,body:not(.skin-timeless):not(.skin-minerva) .mw-parser-output .id-lock-registration a,body:not(.skin-timeless):not(.skin-minerva) .mw-parser-output .id-lock-subscription a,body:not(.skin-timeless):not(.skin-minerva) .mw-parser-output .cs1-ws-icon a{background-size:contain;padding:0 1em 0 0}.mw-parser-output .cs1-code{color:inherit;background:inherit;border:none;padding:inherit}.mw-parser-output .cs1-hidden-error{display:none;color:var(--color-error,#d33)}.mw-parser-output .cs1-visible-error{color:var(--color-error,#d33)}.mw-parser-output .cs1-maint{display:none;color:#085;margin-left:0.3em}.mw-parser-output .cs1-kern-left{padding-left:0.2em}.mw-parser-output .cs1-kern-right{padding-right:0.2em}.mw-parser-output .citation .mw-selflink{font-weight:inherit}@media screen{.mw-parser-output .cs1-format{font-size:95%}html.skin-theme-clientpref-night .mw-parser-output .cs1-maint{color:#18911f}}@media screen and (prefers-color-scheme:dark){html.skin-theme-clientpref-os .mw-parser-output .cs1-maint{color:#18911f}}</style><cite class="citation web cs1"><a rel="nofollow" class="external text" href="https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5de59f5b-e5db-410f-b692-658686ef4107">"Itovebi- inavolisib tablet, film coated"</a>. <i>DailyMed</i>. 11 October 2024<span class="reference-accessdate">. Retrieved <span class="nowrap">11 November</span> 2024</span>.</cite><span title="ctx_ver=Z39.88-2004&amp;rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&amp;rft.genre=unknown&amp;rft.jtitle=DailyMed&amp;rft.atitle=Itovebi-+inavolisib+tablet%2C+film+coated&amp;rft.date=2024-10-11&amp;rft_id=https%3A%2F%2Fdailymed.nlm.nih.gov%2Fdailymed%2FdrugInfo.cfm%3Fsetid%3D5de59f5b-e5db-410f-b692-658686ef4107&amp;rfr_id=info%3Asid%2Fen.wikipedia.org%3AInavolisib" class="Z3988"></span></span> </li> <li id="cite_note-FDA_20241010-2"><span class="mw-cite-backlink">^ <a href="#cite_ref-FDA_20241010_2-0"><sup><i><b>a</b></i></sup></a> <a href="#cite_ref-FDA_20241010_2-1"><sup><i><b>b</b></i></sup></a> <a href="#cite_ref-FDA_20241010_2-2"><sup><i><b>c</b></i></sup></a> <a href="#cite_ref-FDA_20241010_2-3"><sup><i><b>d</b></i></sup></a> <a href="#cite_ref-FDA_20241010_2-4"><sup><i><b>e</b></i></sup></a> <a href="#cite_ref-FDA_20241010_2-5"><sup><i><b>f</b></i></sup></a> <a href="#cite_ref-FDA_20241010_2-6"><sup><i><b>g</b></i></sup></a> <a href="#cite_ref-FDA_20241010_2-7"><sup><i><b>h</b></i></sup></a> <a href="#cite_ref-FDA_20241010_2-8"><sup><i><b>i</b></i></sup></a> <a href="#cite_ref-FDA_20241010_2-9"><sup><i><b>j</b></i></sup></a></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1238218222"><cite class="citation web cs1"><a rel="nofollow" class="external text" href="https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-inavolisib-palbociclib-and-fulvestrant-endocrine-resistant-pik3ca-mutated-hr-positive">"FDA approves inavolisib with palbociclib and fulvestrant for endocrine-resistant, PIK3CA-mutated, HR-positive, HER2-negative, advanced breast cancer"</a>. <i>U.S. <a href="/wiki/Food_and_Drug_Administration" title="Food and Drug Administration">Food and Drug Administration</a> (FDA)</i>. 10 October 2024<span class="reference-accessdate">. Retrieved <span class="nowrap">11 October</span> 2024</span>.</cite><span title="ctx_ver=Z39.88-2004&amp;rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&amp;rft.genre=unknown&amp;rft.jtitle=U.S.+Food+and+Drug+Administration+%28FDA%29&amp;rft.atitle=FDA+approves+inavolisib+with+palbociclib+and+fulvestrant+for+endocrine-resistant%2C+PIK3CA-mutated%2C+HR-positive%2C+HER2-negative%2C+advanced+breast+cancer&amp;rft.date=2024-10-10&amp;rft_id=https%3A%2F%2Fwww.fda.gov%2Fdrugs%2Fresources-information-approved-drugs%2Ffda-approves-inavolisib-palbociclib-and-fulvestrant-endocrine-resistant-pik3ca-mutated-hr-positive&amp;rfr_id=info%3Asid%2Fen.wikipedia.org%3AInavolisib" class="Z3988"></span> <span class="noviewer" typeof="mw:File"><span><img alt="Public Domain" src="//upload.wikimedia.org/wikipedia/en/thumb/6/62/PD-icon.svg/12px-PD-icon.svg.png" decoding="async" width="12" height="12" class="mw-file-element" srcset="//upload.wikimedia.org/wikipedia/en/thumb/6/62/PD-icon.svg/18px-PD-icon.svg.png 1.5x, //upload.wikimedia.org/wikipedia/en/thumb/6/62/PD-icon.svg/24px-PD-icon.svg.png 2x" data-file-width="196" data-file-height="196" /></span></span> This article incorporates text from this source, which is in the <a href="/wiki/Public_domain" title="Public domain">public domain</a>.</span> </li> <li id="cite_note-Hanan_2022-3"><span class="mw-cite-backlink">^ <a href="#cite_ref-Hanan_2022_3-0"><sup><i><b>a</b></i></sup></a> <a href="#cite_ref-Hanan_2022_3-1"><sup><i><b>b</b></i></sup></a> <a href="#cite_ref-Hanan_2022_3-2"><sup><i><b>c</b></i></sup></a> <a href="#cite_ref-Hanan_2022_3-3"><sup><i><b>d</b></i></sup></a> <a href="#cite_ref-Hanan_2022_3-4"><sup><i><b>e</b></i></sup></a></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1238218222"><cite id="CITEREFHananBraunHealdMacLeod2022" class="citation journal cs1">Hanan EJ, Braun MG, Heald RA, MacLeod C, Chan C, Clausen S, et&#160;al. (December 2022). "Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα". <i>Journal of Medicinal Chemistry</i>. <b>65</b> (24). American Chemical Society (ACS): 16589–16621. <a href="/wiki/Doi_(identifier)" class="mw-redirect" title="Doi (identifier)">doi</a>:<a rel="nofollow" class="external text" href="https://doi.org/10.1021%2Facs.jmedchem.2c01422">10.1021/acs.jmedchem.2c01422</a>. <a href="/wiki/PMID_(identifier)" class="mw-redirect" title="PMID (identifier)">PMID</a>&#160;<a rel="nofollow" class="external text" href="https://pubmed.ncbi.nlm.nih.gov/36455032">36455032</a>. <a href="/wiki/S2CID_(identifier)" class="mw-redirect" title="S2CID (identifier)">S2CID</a>&#160;<a rel="nofollow" class="external text" href="https://api.semanticscholar.org/CorpusID:254149451">254149451</a>.</cite><span title="ctx_ver=Z39.88-2004&amp;rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&amp;rft.genre=article&amp;rft.jtitle=Journal+of+Medicinal+Chemistry&amp;rft.atitle=Discovery+of+GDC-0077+%28Inavolisib%29%2C+a+Highly+Selective+Inhibitor+and+Degrader+of+Mutant+PI3K%CE%B1&amp;rft.volume=65&amp;rft.issue=24&amp;rft.pages=16589-16621&amp;rft.date=2022-12&amp;rft_id=https%3A%2F%2Fapi.semanticscholar.org%2FCorpusID%3A254149451%23id-name%3DS2CID&amp;rft_id=info%3Apmid%2F36455032&amp;rft_id=info%3Adoi%2F10.1021%2Facs.jmedchem.2c01422&amp;rft.aulast=Hanan&amp;rft.aufirst=EJ&amp;rft.au=Braun%2C+MG&amp;rft.au=Heald%2C+RA&amp;rft.au=MacLeod%2C+C&amp;rft.au=Chan%2C+C&amp;rft.au=Clausen%2C+S&amp;rft.au=Edgar%2C+KA&amp;rft.au=Eigenbrot%2C+C&amp;rft.au=Elliott%2C+R&amp;rft.au=Endres%2C+N&amp;rft.au=Friedman%2C+LS&amp;rft.au=Gogol%2C+E&amp;rft.au=Gu%2C+XH&amp;rft.au=Thibodeau%2C+RH&amp;rft.au=Jackson%2C+PS&amp;rft.au=Kiefer%2C+JR&amp;rft.au=Knight%2C+JD&amp;rft.au=Nannini%2C+M&amp;rft.au=Narukulla%2C+R&amp;rft.au=Pace%2C+A&amp;rft.au=Pang%2C+J&amp;rft.au=Purkey%2C+HE&amp;rft.au=Salphati%2C+L&amp;rft.au=Sampath%2C+D&amp;rft.au=Schmidt%2C+S&amp;rft.au=Sideris%2C+S&amp;rft.au=Song%2C+K&amp;rft.au=Sujatha-Bhaskar%2C+S&amp;rft.au=Ultsch%2C+M&amp;rft.au=Wallweber%2C+H&amp;rft.au=Xin%2C+J&amp;rft.au=Yeap%2C+S&amp;rft.au=Young%2C+A&amp;rft.au=Zhong%2C+Y&amp;rft.au=Staben%2C+ST&amp;rfr_id=info%3Asid%2Fen.wikipedia.org%3AInavolisib" class="Z3988"></span></span> </li> <li id="cite_note-CID_124173720-4"><span class="mw-cite-backlink"><b><a href="#cite_ref-CID_124173720_4-0">^</a></b></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1238218222"><cite class="citation web cs1"><a rel="nofollow" class="external text" href="https://pubchem.ncbi.nlm.nih.gov/compound/Inavolisib#section=3D-Conformer">"CID 124173720, Inavolisib"</a>. <i>PubChem</i>. National Center for Biotechnology Information, U.S. National Library of Medicine<span class="reference-accessdate">. Retrieved <span class="nowrap">21 September</span> 2023</span>.</cite><span title="ctx_ver=Z39.88-2004&amp;rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&amp;rft.genre=unknown&amp;rft.jtitle=PubChem&amp;rft.atitle=CID+124173720%2C+Inavolisib&amp;rft_id=https%3A%2F%2Fpubchem.ncbi.nlm.nih.gov%2Fcompound%2FInavolisib%23section%3D3D-Conformer&amp;rfr_id=info%3Asid%2Fen.wikipedia.org%3AInavolisib" class="Z3988"></span></span> </li> <li id="cite_note-:0-5"><span class="mw-cite-backlink">^ <a href="#cite_ref-:0_5-0"><sup><i><b>a</b></i></sup></a> <a href="#cite_ref-:0_5-1"><sup><i><b>b</b></i></sup></a></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1238218222"><cite class="citation web cs1"><a rel="nofollow" class="external text" href="https://www.targetedonc.com/view/fda-approves-inavolisib-plus-standard-therapy-in-pik3ca-mutant-breast-cancer">"FDA Approves Inavolisib Plus Standard Therapy in PIK3CA-Mutant Breast Cancer"</a>. <i>Targeted Oncology</i>. 10 October 2024<span class="reference-accessdate">. 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(January 2022). <a rel="nofollow" class="external text" href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9762331">"RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy"</a>. <i>Cancer Discovery</i>. <b>12</b> (1). American Association for Cancer Research (AACR): 204–219. <a href="/wiki/Doi_(identifier)" class="mw-redirect" title="Doi (identifier)">doi</a>:<a rel="nofollow" class="external text" href="https://doi.org/10.1158%2F2159-8290.cd-21-0072">10.1158/2159-8290.cd-21-0072</a>. <a href="/wiki/PMC_(identifier)" class="mw-redirect" title="PMC (identifier)">PMC</a>&#160;<span class="id-lock-free" title="Freely accessible"><a rel="nofollow" class="external text" href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9762331">9762331</a></span>. <a href="/wiki/PMID_(identifier)" class="mw-redirect" title="PMID (identifier)">PMID</a>&#160;<a rel="nofollow" class="external text" href="https://pubmed.ncbi.nlm.nih.gov/34544753">34544753</a>.</cite><span title="ctx_ver=Z39.88-2004&amp;rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&amp;rft.genre=article&amp;rft.jtitle=Cancer+Discovery&amp;rft.atitle=RTK-Dependent+Inducible+Degradation+of+Mutant+PI3K%CE%B1+Drives+GDC-0077+%28Inavolisib%29+Efficacy&amp;rft.volume=12&amp;rft.issue=1&amp;rft.pages=204-219&amp;rft.date=2022-01&amp;rft_id=https%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fpmc%2Farticles%2FPMC9762331%23id-name%3DPMC&amp;rft_id=info%3Apmid%2F34544753&amp;rft_id=info%3Adoi%2F10.1158%2F2159-8290.cd-21-0072&amp;rft.aulast=Song&amp;rft.aufirst=KW&amp;rft.au=Edgar%2C+KA&amp;rft.au=Hanan%2C+EJ&amp;rft.au=Hafner%2C+M&amp;rft.au=Oeh%2C+J&amp;rft.au=Merchant%2C+M&amp;rft.au=Sampath%2C+D&amp;rft.au=Nannini%2C+MA&amp;rft.au=Hong%2C+R&amp;rft.au=Phu%2C+L&amp;rft.au=Forrest%2C+WF&amp;rft.au=Stawiski%2C+E&amp;rft.au=Schmidt%2C+S&amp;rft.au=Endres%2C+N&amp;rft.au=Guan%2C+J&amp;rft.au=Wallin%2C+JJ&amp;rft.au=Cheong%2C+J&amp;rft.au=Plise%2C+EG&amp;rft.au=Lewis+Phillips%2C+GD&amp;rft.au=Salphati%2C+L&amp;rft.au=Heffron%2C+TP&amp;rft.au=Olivero%2C+AG&amp;rft.au=Malek%2C+S&amp;rft.au=Staben%2C+ST&amp;rft.au=Kirkpatrick%2C+DS&amp;rft.au=Dey%2C+A&amp;rft.au=Friedman%2C+LS&amp;rft_id=https%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fpmc%2Farticles%2FPMC9762331&amp;rfr_id=info%3Asid%2Fen.wikipedia.org%3AInavolisib" class="Z3988"></span></span> </li> <li id="cite_note-Novel_Drug_Approvals_for_2024-19"><span class="mw-cite-backlink"><b><a href="#cite_ref-Novel_Drug_Approvals_for_2024_19-0">^</a></b></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1238218222"><cite class="citation web cs1"><a rel="nofollow" class="external text" href="https://www.fda.gov/drugs/novel-drug-approvals-fda/novel-drug-approvals-2024">"Novel Drug Approvals for 2024"</a>. <i>U.S. <a href="/wiki/Food_and_Drug_Administration" title="Food and Drug Administration">Food and Drug Administration</a> (FDA)</i>. 1 October 2024<span class="reference-accessdate">. Retrieved <span class="nowrap">29 November</span> 2024</span>.</cite><span title="ctx_ver=Z39.88-2004&amp;rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&amp;rft.genre=unknown&amp;rft.jtitle=U.S.+Food+and+Drug+Administration+%28FDA%29&amp;rft.atitle=Novel+Drug+Approvals+for+2024&amp;rft.date=2024-10-01&amp;rft_id=https%3A%2F%2Fwww.fda.gov%2Fdrugs%2Fnovel-drug-approvals-fda%2Fnovel-drug-approvals-2024&amp;rfr_id=info%3Asid%2Fen.wikipedia.org%3AInavolisib" class="Z3988"></span></span> </li> <li id="cite_note-20"><span class="mw-cite-backlink"><b><a href="#cite_ref-20">^</a></b></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1238218222"><cite class="citation pressrelease cs1"><a rel="nofollow" class="external text" href="https://www.businesswire.com/news/home/20241008295168/en/FDA-Approves-Genentech%E2%80%99s-Itovebi-a-Targeted-Treatment-for-Advanced-Hormone-Receptor-Positive-HER2-Negative-Breast-Cancer-With-a-PIK3CA-Mutation">"FDA Approves Genentech's Itovebi, a Targeted Treatment for Advanced Hormone Receptor-Positive, HER2-Negative Breast Cancer With a PIK3CA Mutation"</a> (Press release). 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Retrieved <span class="nowrap">11 October</span> 2024</span> &#8211; via Business Wire.</cite><span title="ctx_ver=Z39.88-2004&amp;rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Abook&amp;rft.genre=unknown&amp;rft.btitle=FDA+Approves+Genentech%27s+Itovebi%2C+a+Targeted+Treatment+for+Advanced+Hormone+Receptor-Positive%2C+HER2-Negative+Breast+Cancer+With+a+PIK3CA+Mutation&amp;rft.pub=Genentech&amp;rft.date=2024-10-10&amp;rft_id=https%3A%2F%2Fwww.businesswire.com%2Fnews%2Fhome%2F20241008295168%2Fen%2FFDA-Approves-Genentech%25E2%2580%2599s-Itovebi-a-Targeted-Treatment-for-Advanced-Hormone-Receptor-Positive-HER2-Negative-Breast-Cancer-With-a-PIK3CA-Mutation&amp;rfr_id=info%3Asid%2Fen.wikipedia.org%3AInavolisib" class="Z3988"></span></span> </li> <li id="cite_note-21"><span class="mw-cite-backlink"><b><a href="#cite_ref-21">^</a></b></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1238218222"><cite class="citation pressrelease cs1"><a rel="nofollow" class="external text" href="https://www.businesswire.com/news/home/20241011935278/en/U.S.-Food-and-Drug-Administration-Approves-FoundationOne%C2%AELiquid-CDx-as-a-Companion-Diagnostic-for-Itovebi%E2%84%A2-inavolisib-to-Identify-Patients-with-Hormone-Receptor-Positive-HER2-Negative-Breast-Cancer-with-a-PIK3CA-Mutation">"U.S. Food and Drug Administration Approves FoundationOne Liquid CDx as a Companion Diagnostic for Itovebi (inavolisib) to Identify Patients with Hormone Receptor-Positive, HER2-Negative Breast Cancer with a PIK3CA Mutation"</a> (Press release). Foundation Medicine. 11 October 2024<span class="reference-accessdate">. Retrieved <span class="nowrap">11 October</span> 2024</span> &#8211; via Business Wire.</cite><span title="ctx_ver=Z39.88-2004&amp;rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Abook&amp;rft.genre=unknown&amp;rft.btitle=U.S.+Food+and+Drug+Administration+Approves+FoundationOne+Liquid+CDx+as+a+Companion+Diagnostic+for+Itovebi+%28inavolisib%29+to+Identify+Patients+with+Hormone+Receptor-Positive%2C+HER2-Negative+Breast+Cancer+with+a+PIK3CA+Mutation&amp;rft.pub=Foundation+Medicine&amp;rft.date=2024-10-11&amp;rft_id=https%3A%2F%2Fwww.businesswire.com%2Fnews%2Fhome%2F20241011935278%2Fen%2FU.S.-Food-and-Drug-Administration-Approves-FoundationOne%25C2%25AELiquid-CDx-as-a-Companion-Diagnostic-for-Itovebi%25E2%2584%25A2-inavolisib-to-Identify-Patients-with-Hormone-Receptor-Positive-HER2-Negative-Breast-Cancer-with-a-PIK3CA-Mutation&amp;rfr_id=info%3Asid%2Fen.wikipedia.org%3AInavolisib" class="Z3988"></span></span> </li> <li id="cite_note-22"><span class="mw-cite-backlink"><b><a href="#cite_ref-22">^</a></b></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1238218222"><cite class="citation web cs1"><a rel="nofollow" class="external text" href="https://www.onclive.com/view/fda-approves-inavolisib-plus-palbociclib-fulvestrant-for-endocrine-resistant-pik3ca-mutated-hr-her2-advanced-breast-cancer">"FDA Approves Inavolisib Plus Palbociclib/Fulvestrant for Endocrine-Resistant, PIK3CA-Mutated, HR+, HER2– Advanced Breast Cancer"</a>. <i>OncLive</i>. 10 October 2024<span class="reference-accessdate">. Retrieved <span class="nowrap">11 October</span> 2024</span>.</cite><span title="ctx_ver=Z39.88-2004&amp;rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&amp;rft.genre=unknown&amp;rft.jtitle=OncLive&amp;rft.atitle=FDA+Approves+Inavolisib+Plus+Palbociclib%2FFulvestrant+for+Endocrine-Resistant%2C+PIK3CA-Mutated%2C+HR%2B%2C+HER2%E2%80%93+Advanced+Breast+Cancer&amp;rft.date=2024-10-10&amp;rft_id=https%3A%2F%2Fwww.onclive.com%2Fview%2Ffda-approves-inavolisib-plus-palbociclib-fulvestrant-for-endocrine-resistant-pik3ca-mutated-hr-her2-advanced-breast-cancer&amp;rfr_id=info%3Asid%2Fen.wikipedia.org%3AInavolisib" class="Z3988"></span></span> </li> <li id="cite_note-23"><span class="mw-cite-backlink"><b><a href="#cite_ref-23">^</a></b></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1238218222"><cite id="CITEREFWorld_Health_Organization2020" class="citation journal cs1"><a href="/wiki/World_Health_Organization" title="World Health Organization">World Health Organization</a> (2020). 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title="ctx_ver=Z39.88-2004&amp;rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&amp;rft.genre=article&amp;rft.jtitle=Cancer+Discovery&amp;rft.atitle=Precision+Targeting+of+Mutant+PI3K%CE%B1+in+Cancer+by+Selective+Degradation&amp;rft.volume=12&amp;rft.issue=1&amp;rft.pages=20-22&amp;rft.date=2022-01&amp;rft_id=https%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fpmc%2Farticles%2FPMC7612218%23id-name%3DPMC&amp;rft_id=info%3Apmid%2F35022207&amp;rft_id=info%3Adoi%2F10.1158%2F2159-8290.cd-21-1411&amp;rft.aulast=Vanhaesebroeck&amp;rft.aufirst=B&amp;rft.au=Burke%2C+JE&amp;rft.au=Madsen%2C+RR&amp;rft_id=https%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fpmc%2Farticles%2FPMC7612218&amp;rfr_id=info%3Asid%2Fen.wikipedia.org%3AInavolisib" class="Z3988"></span></span> </li> </ol></div></div> <div class="mw-heading mw-heading2"><h2 id="External_links">External links</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inavolisib&amp;action=edit&amp;section=13" title="Edit section: External links"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <ul><li>Clinical trial number <i><a rel="nofollow" class="external text" href="https://www.clinicaltrials.gov/show/NCT04191499">NCT04191499</a></i> for "A Study Evaluating the Efficacy and Safety of Inavolisib + Palbociclib + Fulvestrant vs Placebo + Palbociclib + Fulvestrant in Patients With PIK3CA-Mutant, Hormone Receptor-Positive, Her2-Negative, Locally Advanced or Metastatic Breast Cancer (INAVO120)" at <a href="/wiki/ClinicalTrials.gov" title="ClinicalTrials.gov">ClinicalTrials.gov</a></li></ul> <div class="navbox-styles"><style data-mw-deduplicate="TemplateStyles:r1129693374">.mw-parser-output .hlist dl,.mw-parser-output .hlist ol,.mw-parser-output .hlist ul{margin:0;padding:0}.mw-parser-output .hlist dd,.mw-parser-output .hlist dt,.mw-parser-output .hlist li{margin:0;display:inline}.mw-parser-output .hlist.inline,.mw-parser-output .hlist.inline dl,.mw-parser-output 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class="navbox-group" style="width:1%"><a href="/wiki/Cancer_immunotherapy" title="Cancer immunotherapy">CI</a> <a href="/wiki/Monoclonal_antibody_therapy" title="Monoclonal antibody therapy">monoclonal antibodies</a> ("-mab")</th><td class="navbox-list-with-group navbox-list navbox-odd hlist" style="width:100%;padding:0"><div style="padding:0 0.25em"></div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th scope="row" class="navbox-group" style="width:1%"><a href="/wiki/Receptor_tyrosine_kinase" title="Receptor tyrosine kinase">Receptor tyrosine kinase</a></th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/ErbB" title="ErbB">ErbB</a>: <i><a href="/wiki/Epidermal_growth_factor_receptor" title="Epidermal growth factor receptor">HER1/EGFR</a></i> (<a href="/wiki/Cetuximab" title="Cetuximab">Cetuximab</a></li> <li><a href="/wiki/Panitumumab" title="Panitumumab">Panitumumab</a>)</li> <li><i><a href="/wiki/HER2/neu" class="mw-redirect" title="HER2/neu">HER2/neu</a></i> (<a href="/wiki/Pertuzumab" title="Pertuzumab">Pertuzumab</a></li> <li><a href="/wiki/Trastuzumab" title="Trastuzumab">Trastuzumab</a> (<a href="/wiki/Trastuzumab/hyaluronidase" title="Trastuzumab/hyaluronidase">+hyaluronidase</a>)</li> <li><a href="/wiki/Trastuzumab_emtansine" title="Trastuzumab emtansine">Trastuzumab emtansine</a></li> <li><a href="/wiki/Trastuzumab_deruxtecan" title="Trastuzumab deruxtecan">Trastuzumab deruxtecan</a></li> <li><a href="/wiki/Zanidatamab" title="Zanidatamab">Zanidatamab</a> )</li></ul> </div></td></tr><tr><th scope="row" class="navbox-group" style="width:1%">Others for solid tumors</th><td class="navbox-list-with-group navbox-list navbox-even" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><i><a href="/wiki/EpCAM" class="mw-redirect" title="EpCAM">EpCAM</a></i> (<a href="/wiki/Catumaxomab" title="Catumaxomab">Catumaxomab</a></li> <li><a href="/wiki/Edrecolomab" title="Edrecolomab">Edrecolomab</a>)</li> <li><i><a href="/wiki/Vascular_endothelial_growth_factor_A" title="Vascular endothelial growth factor A">VEGF-A</a></i> (<a href="/wiki/Bevacizumab" title="Bevacizumab">Bevacizumab</a>)</li></ul> </div></td></tr><tr><th scope="row" class="navbox-group" style="width:1%"><a href="/wiki/Leukemia" title="Leukemia">Leukemia</a>/<a href="/wiki/Lymphoma" title="Lymphoma">lymphoma</a></th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Lymphatic_system" title="Lymphatic system">lymphoid</a>: <i><a href="/wiki/CD3_(immunology)" title="CD3 (immunology)">CD3</a></i> (<a href="/wiki/Glofitamab" title="Glofitamab">Glofitamab</a>, <a href="/wiki/Elranatamab" title="Elranatamab">Elranatamab</a>, <a href="/wiki/Mosunetuzumab" title="Mosunetuzumab">Mosunetuzumab</a>), <i><a href="/wiki/CD20" title="CD20">CD20</a></i> (<a href="/wiki/Glofitamab" title="Glofitamab">Glofitamab</a></li> <li><a href="/wiki/Ibritumomab_tiuxetan" title="Ibritumomab tiuxetan">Ibritumomab</a></li> <li><a href="/wiki/Mosunetuzumab" title="Mosunetuzumab">Mosunetuzumab</a></li> <li><a href="/wiki/Obinutuzumab" title="Obinutuzumab">Obinutuzumab</a></li> <li><a href="/wiki/Ofatumumab" title="Ofatumumab">Ofatumumab</a></li> <li><a href="/wiki/Rituximab" title="Rituximab">Rituximab</a></li> <li><a href="/wiki/Tositumomab" title="Tositumomab">Tositumomab</a>), <i><a href="/wiki/CD30" title="CD30">CD30</a></i> (<a href="/wiki/Brentuximab_vedotin" title="Brentuximab vedotin">Brentuximab</a>), <i><a href="/wiki/CD52" title="CD52">CD52</a></i> (<a href="/wiki/Alemtuzumab" title="Alemtuzumab">Alemtuzumab</a>)</li></ul> <ul><li><a href="/wiki/Myeloid" class="mw-redirect" title="Myeloid">myeloid</a>: <i><a href="/wiki/CD33" title="CD33">CD33</a></i> (<a href="/wiki/Gemtuzumab_ozogamicin" title="Gemtuzumab ozogamicin">Gemtuzumab ozogamicin</a>)</li></ul> </div></td></tr><tr><th scope="row" class="navbox-group" style="width:1%">Other</th><td class="navbox-list-with-group navbox-list navbox-even" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Amivantamab" title="Amivantamab">Amivantamab</a></li> <li><a href="/wiki/Atezolizumab" title="Atezolizumab">Atezolizumab</a> (<a href="/wiki/Atezolizumab/hyaluronidase" title="Atezolizumab/hyaluronidase">+hyaluronidase</a>)</li> <li><a href="/wiki/Avelumab" title="Avelumab">Avelumab</a></li> <li><a href="/wiki/Axatilimab" title="Axatilimab">Axatilimab</a></li> <li><a href="/wiki/Belantamab_mafodotin" title="Belantamab mafodotin">Belantamab mafodotin</a></li> <li><a href="/wiki/Bermekimab" title="Bermekimab">Bermekimab</a></li> <li><a href="/wiki/Blinatumomab" title="Blinatumomab">Blinatumomab</a></li> <li><a href="/wiki/Cemiplimab" title="Cemiplimab">Cemiplimab</a></li> <li><a href="/wiki/Daratumumab" title="Daratumumab">Daratumumab</a></li> <li><a href="/wiki/Dinutuximab_beta" class="mw-redirect" title="Dinutuximab beta">Dinutuximab beta</a></li> <li><a href="/wiki/Dostarlimab" title="Dostarlimab">Dostarlimab</a></li> <li><a href="/wiki/Durvalumab" title="Durvalumab">Durvalumab</a></li> <li><a href="/wiki/Elotuzumab" title="Elotuzumab">Elotuzumab</a></li> <li><a href="/wiki/Enfortumab_vedotin" title="Enfortumab vedotin">Enfortumab vedotin</a></li> <li><a href="/wiki/Epcoritamab" title="Epcoritamab">Epcoritamab</a></li> <li><a href="/wiki/Inotuzumab_ozogamicin" title="Inotuzumab ozogamicin">Inotuzumab ozogamicin</a></li> <li><a href="/wiki/Ipilimumab" title="Ipilimumab">Ipilimumab</a></li> <li><a href="/wiki/Isatuximab" title="Isatuximab">Isatuximab</a></li> <li><a href="/wiki/Loncastuximab_tesirine" title="Loncastuximab tesirine">Loncastuximab tesirine</a></li> <li><a href="/wiki/Mirvetuximab_soravtansine" title="Mirvetuximab soravtansine">Mirvetuximab soravtansine</a></li> <li><a href="/wiki/Mogamulizumab" title="Mogamulizumab">Mogamulizumab</a></li> <li><a href="/wiki/Moxetumomab_pasudotox" title="Moxetumomab pasudotox">Moxetumomab pasudotox</a></li> <li><a href="/wiki/Naxitamab" title="Naxitamab">Naxitamab</a></li> <li><a href="/wiki/Necitumumab" title="Necitumumab">Necitumumab</a></li> <li><a href="/wiki/Nivolumab" title="Nivolumab">Nivolumab</a></li> <li><a href="/wiki/Olaratumab" title="Olaratumab">Olaratumab</a></li> <li><a href="/wiki/Oportuzumab_monatox" title="Oportuzumab monatox">Oportuzumab monatox</a></li> <li><a href="/wiki/Pembrolizumab" title="Pembrolizumab">Pembrolizumab</a></li> <li><a href="/wiki/Polatuzumab_vedotin" title="Polatuzumab vedotin">Polatuzumab vedotin</a></li> <li><a href="/w/index.php?title=Prolgolimab&amp;action=edit&amp;redlink=1" class="new" title="Prolgolimab (page does not exist)">Prolgolimab</a></li> <li><a href="/wiki/Ramucirumab" title="Ramucirumab">Ramucirumab</a></li> <li><a href="/wiki/Retifanlimab" title="Retifanlimab">Retifanlimab</a></li> <li><a href="/w/index.php?title=Sabatolimab&amp;action=edit&amp;redlink=1" class="new" title="Sabatolimab (page does not exist)">Sabatolimab</a></li> <li><a href="/wiki/Sacituzumab_govitecan" title="Sacituzumab govitecan">Sacituzumab govitecan</a></li> <li><a href="/wiki/Serplulimab" title="Serplulimab">Serplulimab</a></li> <li><a href="/wiki/Sugemalimab" title="Sugemalimab">Sugemalimab</a></li> <li><a href="/wiki/Tafasitamab" title="Tafasitamab">Tafasitamab</a></li> <li><a href="/wiki/Talquetamab" title="Talquetamab">Talquetamab</a></li> <li><a href="/wiki/Tarlatamab" title="Tarlatamab">Tarlatamab</a></li> <li><a href="/wiki/Teclistamab" title="Teclistamab">Teclistamab</a></li> <li><a href="/wiki/Tislelizumab" title="Tislelizumab">Tislelizumab</a></li> <li><a href="/wiki/Tisotumab_vedotin" title="Tisotumab vedotin">Tisotumab vedotin</a></li> <li><a href="/wiki/Toripalimab" title="Toripalimab">Toripalimab</a></li> <li><a href="/wiki/Tremelimumab" title="Tremelimumab">Tremelimumab</a></li> <li><a href="/wiki/Zolbetuximab" title="Zolbetuximab">Zolbetuximab</a></li></ul> </div></td></tr></tbody></table><div></div></td></tr><tr><th scope="row" class="navbox-group" style="width:1%"><a href="/wiki/Tyrosine_kinase_inhibitor" title="Tyrosine kinase inhibitor">Tyrosine kinase inhibitors</a> ("-nib")</th><td class="navbox-list-with-group navbox-list navbox-odd hlist" style="width:100%;padding:0"><div style="padding:0 0.25em"></div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th scope="row" class="navbox-group" style="width:1%"><a href="/wiki/Receptor_tyrosine_kinase" title="Receptor tyrosine kinase">Receptor tyrosine kinase</a></th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/ErbB" title="ErbB">ErbB</a>: <i><a href="/wiki/Epidermal_growth_factor_receptor" title="Epidermal growth factor receptor">HER1/EGFR</a></i> (<a href="/wiki/Afatinib" title="Afatinib">Afatinib</a></li> <li><a href="/wiki/Aumolertinib" title="Aumolertinib">Aumolertinib</a></li> <li><a href="/wiki/Brigatinib" title="Brigatinib">Brigatinib</a></li> <li><a href="/wiki/Dacomitinib" title="Dacomitinib">Dacomitinib</a></li> <li><a href="/wiki/Erlotinib" title="Erlotinib">Erlotinib</a></li> <li><a href="/wiki/Gefitinib" title="Gefitinib">Gefitinib</a></li> <li><a href="/wiki/Icotinib" title="Icotinib">Icotinib</a></li> <li><a href="/wiki/Lazertinib" title="Lazertinib">Lazertinib</a></li> <li><a href="/wiki/Mobocertinib" title="Mobocertinib">Mobocertinib</a></li> <li><a href="/wiki/Olmutinib" title="Olmutinib">Olmutinib</a></li> <li><a href="/wiki/Osimertinib" title="Osimertinib">Osimertinib</a></li> <li><a href="/wiki/Rociletinib" title="Rociletinib">Rociletinib</a></li> <li><a href="/wiki/Vandetanib" title="Vandetanib">Vandetanib</a>)</li></ul> <ul><li><i>HER1/EGFR and <a href="/wiki/HER2/neu" class="mw-redirect" title="HER2/neu">HER2/neu</a></i> <ul><li><a href="/wiki/Lapatinib" title="Lapatinib">Lapatinib</a></li> <li><a href="/wiki/Neratinib" title="Neratinib">Neratinib</a></li> <li><a href="/wiki/Tucatinib" title="Tucatinib">Tucatinib</a></li></ul></li></ul> <ul><li><i><a href="/wiki/BRAF_(gene)" title="BRAF (gene)">BRAF</a></i> <ul><li><a href="/wiki/Dabrafenib" title="Dabrafenib">Dabrafenib</a></li> <li><a href="/wiki/Encorafenib" title="Encorafenib">Encorafenib</a></li> <li><a href="/wiki/Vemurafenib" title="Vemurafenib">Vemurafenib</a></li></ul></li></ul> <ul><li><a href="/wiki/RTK_class_III" title="RTK class III">RTK class III</a>: <i><a href="/wiki/CD117" class="mw-redirect" title="CD117">C-kit</a> and <a href="/wiki/Platelet-derived_growth_factor_receptor" title="Platelet-derived growth factor receptor">PDGFR</a></i> (<a href="/wiki/Avapritinib" title="Avapritinib">Avapritinib</a></li> <li><a href="/wiki/Axitinib" title="Axitinib">Axitinib</a></li> <li><a href="/wiki/Masitinib" title="Masitinib">Masitinib</a></li> <li><a href="/wiki/Pazopanib" title="Pazopanib">Pazopanib</a></li> <li><a href="/wiki/Ripretinib" title="Ripretinib">Ripretinib</a></li> <li><a href="/wiki/Sorafenib" title="Sorafenib">Sorafenib</a></li> <li><a href="/wiki/Sunitinib" title="Sunitinib">Sunitinib</a></li> <li><a href="/wiki/Toceranib" title="Toceranib">Toceranib</a>)</li> <li><i><a href="/wiki/CD135" title="CD135">FLT3</a></i> (<a href="/wiki/Lestaurtinib" title="Lestaurtinib">Lestaurtinib</a>, <a href="/wiki/Gilteritinib" title="Gilteritinib">Gilteritinib</a> (AXL, ALK, LTK))</li></ul> <ul><li><i><a href="/wiki/VEGF_receptors" class="mw-redirect" title="VEGF receptors">VEGFR</a></i> <ul><li><a href="/wiki/Axitinib" title="Axitinib">Axitinib</a></li> <li><a href="/wiki/Cediranib" title="Cediranib">Cediranib</a></li> <li><a href="/wiki/Fruquintinib" title="Fruquintinib">Fruquintinib</a></li> <li><a href="/wiki/Lenvatinib" title="Lenvatinib">Lenvatinib</a></li> <li><a href="/wiki/Nintedanib" title="Nintedanib">Nintedanib</a></li> <li><a href="/wiki/Pazopanib" title="Pazopanib">Pazopanib</a></li> <li><a href="/wiki/Regorafenib" title="Regorafenib">Regorafenib</a></li> <li><a href="/wiki/Semaxanib" title="Semaxanib">Semaxanib</a></li> <li><a href="/wiki/Sorafenib" title="Sorafenib">Sorafenib</a></li> <li><a href="/wiki/Sunitinib" title="Sunitinib">Sunitinib</a></li> <li><a href="/wiki/Tivozanib" title="Tivozanib">Tivozanib</a></li> <li><a href="/wiki/Toceranib" title="Toceranib">Toceranib</a></li> <li><a href="/wiki/Vandetanib" title="Vandetanib">Vandetanib</a></li></ul></li></ul> <ul><li><i><a href="/wiki/Anaplastic_lymphoma_kinase" title="Anaplastic lymphoma kinase">ALK</a></i> <ul><li><a href="/wiki/Alectinib" title="Alectinib">Alectinib</a></li> <li><a href="/wiki/Brigatinib" title="Brigatinib">Brigatinib</a></li> <li><a href="/wiki/Ceritinib" title="Ceritinib">Ceritinib</a></li> <li><a href="/wiki/Crizotinib" title="Crizotinib">Crizotinib</a></li> <li><a href="/wiki/Lorlatinib" title="Lorlatinib">Lorlatinib</a></li></ul></li></ul> <ul><li><i><a href="/wiki/RET_proto-oncogene" title="RET proto-oncogene">RET</a> inhibitors:</i> <a href="/wiki/Entrectinib" title="Entrectinib">Entrectinib</a> (ALK, ROS1, NTRK), <a href="/wiki/Futibatinib" title="Futibatinib">Futibatinib</a> (FGFR2), <a href="/wiki/Infigratinib" title="Infigratinib">Infigratinib</a>, <a href="/wiki/Larotrectinib" title="Larotrectinib">Larotrectinib</a> (NTRK), <a href="/wiki/Pemigatinib" title="Pemigatinib">Pemigatinib</a> (FGFR), <a href="/wiki/Pralsetinib" title="Pralsetinib">Pralsetinib</a>, <a href="/wiki/Repotrectinib" title="Repotrectinib">Repotrectinib</a> (ROS1, TRK, ALK), <a href="/wiki/Selpercatinib" title="Selpercatinib">Selpercatinib</a> (VEGFR, FGFR), <a href="/wiki/Vandetanib" title="Vandetanib">Vandetanib</a> (VEGFR, EGFR).</li></ul> <ul><li><i><a href="/wiki/C-Met" class="mw-redirect" title="C-Met">c-MET</a> inhibitors:</i> <a href="/wiki/Cabozantinib" title="Cabozantinib">Cabozantinib</a> (VEGFR), <a href="/wiki/Capmatinib" title="Capmatinib">Capmatinib</a>, <a href="/wiki/Crizotinib" title="Crizotinib">Crizotinib</a> (ALK)</li></ul> </div></td></tr><tr><th scope="row" class="navbox-group" style="width:1%"><a href="/wiki/Non-receptor_tyrosine_kinase" title="Non-receptor tyrosine kinase">Non-receptor</a></th><td class="navbox-list-with-group navbox-list navbox-even" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><i><a href="/wiki/Bcr-abl_fusion_protein" class="mw-redirect" title="Bcr-abl fusion protein">bcr-abl</a></i> <ul><li><a href="/wiki/Asciminib" title="Asciminib">Asciminib</a></li> <li><a href="/wiki/Bosutinib" title="Bosutinib">Bosutinib</a></li> <li><a href="/wiki/Dasatinib" title="Dasatinib">Dasatinib</a></li> <li><a href="/wiki/Imatinib" title="Imatinib">Imatinib</a></li> <li><a href="/wiki/Nilotinib" title="Nilotinib">Nilotinib</a></li> <li><a href="/wiki/Ponatinib" title="Ponatinib">Ponatinib</a></li> <li><a href="/wiki/Radotinib" title="Radotinib">Radotinib</a></li></ul></li></ul> <ul><li><i><a href="/wiki/Src_(gene)" class="mw-redirect" title="Src (gene)">Src</a></i> (<a href="/wiki/Bosutinib" title="Bosutinib">Bosutinib</a></li> <li><a href="/wiki/Dasatinib" title="Dasatinib">Dasatinib</a>)</li></ul> <ul><li><i><a href="/wiki/Janus_kinase" title="Janus kinase">Janus kinase</a> (JAK)</i> <ul><li><a href="/wiki/Baricitinib" title="Baricitinib">Baricitinib</a></li> <li><a href="/wiki/Fedratinib" title="Fedratinib">Fedratinib</a></li> <li><a href="/wiki/Filgotinib" title="Filgotinib">Filgotinib</a></li> <li><a href="/wiki/Lestaurtinib" title="Lestaurtinib">Lestaurtinib</a></li> <li><a href="/wiki/Momelotinib" title="Momelotinib">Momelotinib</a></li> <li><a href="/wiki/Pacritinib" title="Pacritinib">Pacritinib</a></li> <li><a href="/wiki/Ruxolitinib" title="Ruxolitinib">Ruxolitinib</a></li></ul></li></ul> <ul><li><i><a href="/wiki/Mitogen-activated_protein_kinase_kinase" title="Mitogen-activated protein kinase kinase">MAP2K</a> (MEK)</i> <ul><li><a href="/wiki/Binimetinib" title="Binimetinib">Binimetinib</a></li> <li><a href="/wiki/Cobimetinib" title="Cobimetinib">Cobimetinib</a></li> <li><a href="/wiki/Selumetinib" title="Selumetinib">Selumetinib</a></li> <li><a href="/wiki/Trametinib" title="Trametinib">Trametinib</a></li></ul></li></ul> <ul><li><i><a href="/wiki/EML4" title="EML4">EML4</a>-<a href="/wiki/Anaplastic_lymphoma_kinase" title="Anaplastic lymphoma kinase">ALK</a></i> <ul><li><a href="/wiki/Crizotinib" title="Crizotinib">Crizotinib</a></li> <li><a href="/wiki/Entrectinib" title="Entrectinib">Entrectinib</a></li> <li><a href="/wiki/Lorlatinib" title="Lorlatinib">Lorlatinib</a></li></ul></li></ul> <ul><li><i><a href="/wiki/Bruton%27s_tyrosine_kinase" title="Bruton&#39;s tyrosine kinase">Bruton's</a> (BTK)</i> <ul><li><a href="/wiki/Acalabrutinib" title="Acalabrutinib">Acalabrutinib</a></li> <li><a href="/wiki/Ibrutinib" title="Ibrutinib">Ibrutinib</a></li> <li><a href="/wiki/Orelabrutinib" title="Orelabrutinib">Orelabrutinib</a></li> <li><a href="/wiki/Pirtobrutinib" title="Pirtobrutinib">Pirtobrutinib</a></li> <li><a href="/wiki/Zanubrutinib" title="Zanubrutinib">Zanubrutinib</a></li></ul></li></ul> </div></td></tr></tbody></table><div></div></td></tr><tr><th scope="row" class="navbox-group" style="width:1%">Other</th><td class="navbox-list-with-group navbox-list navbox-odd hlist" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><i><a href="/wiki/Fusion_protein" title="Fusion protein">fusion protein</a> against <a href="/wiki/Vascular_endothelial_growth_factor" title="Vascular endothelial growth factor">VEGF</a></i> (<a href="/wiki/Aflibercept" title="Aflibercept">Aflibercept</a>)</li></ul> <ul><li><i><a href="/wiki/Proapoptotic" class="mw-redirect" title="Proapoptotic">proapoptotic</a> peptide against <a href="/wiki/ANXA2" class="mw-redirect" title="ANXA2">ANXA2</a> and <a href="/wiki/Prohibitin" title="Prohibitin">prohibitin</a></i> (<a href="/wiki/Adipotide" class="mw-redirect" title="Adipotide">Adipotide</a>)</li></ul> <ul><li><i><a href="/wiki/Exotoxin" title="Exotoxin">exotoxin</a> against <a href="/wiki/Interleukin_2" title="Interleukin 2">IL-2</a></i> (<a href="/wiki/Denileukin_diftitox" title="Denileukin diftitox">Denileukin diftitox</a>)</li></ul> <ul><li><i><a href="/wiki/MTOR_inhibitor" class="mw-redirect" title="MTOR inhibitor">mTOR inhibitors</a></i> <ul><li><a href="/wiki/Everolimus" title="Everolimus">Everolimus</a></li> <li><a href="/wiki/Ridaforolimus" title="Ridaforolimus">Ridaforolimus</a></li> <li><a href="/wiki/Sirolimus" title="Sirolimus">Sirolimus</a></li> <li><a href="/wiki/Temsirolimus" title="Temsirolimus">Temsirolimus</a></li></ul></li></ul> <ul><li><i><a href="/wiki/Hedgehog_signaling_pathway" title="Hedgehog signaling pathway">hedgehog</a> inhibitors</i> <ul><li><a href="/wiki/Glasdegib" title="Glasdegib">Glasdegib</a></li> <li><a href="/wiki/Sonidegib" title="Sonidegib">Sonidegib</a></li> <li><a href="/wiki/Vismodegib" title="Vismodegib">Vismodegib</a></li></ul></li></ul> <ul><li><i><a href="/wiki/CDK_inhibitor" title="CDK inhibitor">CDK inhibitors</a></i> <ul><li><a href="/wiki/Abemaciclib" title="Abemaciclib">Abemaciclib</a></li> <li><a href="/wiki/Dalpiciclib" title="Dalpiciclib">Dalpiciclib</a></li> <li><a href="/wiki/Palbociclib" title="Palbociclib">Palbociclib</a></li> <li><a href="/wiki/Ribociclib" title="Ribociclib">Ribociclib</a></li> <li><a href="/wiki/Trilaciclib" title="Trilaciclib">Trilaciclib</a></li></ul></li></ul> <ul><li><i><a href="/wiki/KRAS" title="KRAS">KRAS</a> inhibitors</i> <ul><li><a href="/wiki/Adagrasib" title="Adagrasib">Adagrasib</a></li> <li><a href="/wiki/Sotorasib" title="Sotorasib">Sotorasib</a></li></ul></li></ul> <ul><li><i><a href="/wiki/Pi3K_inhibitor" class="mw-redirect" title="Pi3K inhibitor">Pi3K inhibitors</a></i> <ul><li><a href="/wiki/Alpelisib" title="Alpelisib">Alpelisib</a></li> <li><a href="/wiki/Copanlisib" title="Copanlisib">Copanlisib</a></li> <li><a href="/wiki/Duvelisib" title="Duvelisib">Duvelisib</a></li> <li><a href="/wiki/Idelalisib" title="Idelalisib">Idelalisib</a></li> <li><a class="mw-selflink selflink">Inavolisib</a></li> <li><a href="/wiki/Parsaclisib" title="Parsaclisib">Parsaclisib</a></li></ul></li></ul> <ul><li><i><a href="/wiki/MEN1" title="MEN1">Menin</a> inhibitors</i> <ul><li><a href="/wiki/Revumenib" title="Revumenib">Revumenib</a></li></ul></li></ul> <ul><li><i><a href="/wiki/Fibroblast_growth_factor_receptor" title="Fibroblast growth factor receptor">Fibroblast growth factor receptor</a></i> (FGFR) inhibitors</li> <li><a href="/wiki/Erdafitinib" title="Erdafitinib">Erdafitinib</a></li> <li><a href="/wiki/Futibatinib" title="Futibatinib">Futibatinib</a></li> <li><a href="/wiki/Infigratinib" title="Infigratinib">Infigratinib</a></li> <li><a href="/wiki/Pemigatinib" title="Pemigatinib">Pemigatinib</a></li></ul> <ul><li><a href="/wiki/Cabozantinib" title="Cabozantinib">Cabozantinib</a></li> <li><a href="/wiki/Capmatinib" title="Capmatinib">Capmatinib</a></li> <li><a href="/wiki/Entrectinib" title="Entrectinib">Entrectinib</a></li> <li><a href="/wiki/Gilteritinib" title="Gilteritinib">Gilteritinib</a></li> <li><a href="/wiki/Larotrectinib" title="Larotrectinib">Larotrectinib</a></li> <li><a href="/wiki/Lenvatinib" title="Lenvatinib">Lenvatinib</a></li> <li><a href="/wiki/Masitinib" title="Masitinib">Masitinib</a></li> <li><a href="/wiki/Midostaurin" title="Midostaurin">Midostaurin</a></li> <li><a href="/wiki/Nintedanib" title="Nintedanib">Nintedanib</a></li> <li><a href="/wiki/Odronextamab" title="Odronextamab">Odronextamab</a></li> <li><a href="/wiki/Pazopanib" title="Pazopanib">Pazopanib</a></li> <li><a href="/wiki/Pexidartinib" title="Pexidartinib">Pexidartinib</a></li> <li><a href="/wiki/Quizartinib" title="Quizartinib">Quizartinib</a></li> <li><a href="/wiki/Regorafenib" title="Regorafenib">Regorafenib</a></li> <li><a href="/wiki/Ripretinib" title="Ripretinib">Ripretinib</a></li> <li><a href="/wiki/Sorafenib" title="Sorafenib">Sorafenib</a></li> <li><a href="/wiki/Sunitinib" title="Sunitinib">Sunitinib</a></li> <li><a href="/wiki/Tebentafusp" title="Tebentafusp">Tebentafusp</a></li> <li><a href="/wiki/Tepotinib" title="Tepotinib">Tepotinib</a></li> <li><a href="/wiki/Vandetanib" title="Vandetanib">Vandetanib</a></li> <li><a href="/wiki/Venetoclax" title="Venetoclax">Venetoclax</a></li></ul> </div></td></tr></tbody></table></div> <style data-mw-deduplicate="TemplateStyles:r1130092004">.mw-parser-output .portal-bar{font-size:88%;font-weight:bold;display:flex;justify-content:center;align-items:baseline}.mw-parser-output .portal-bar-bordered{padding:0 2em;background-color:#fdfdfd;border:1px solid #a2a9b1;clear:both;margin:1em auto 0}.mw-parser-output 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