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.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"><tbody><tr><th colspan="2" class="infobox-above" style="background-color: #ddbbee">Gonadotropin-releasing hormone antagonist</th></tr><tr><td colspan="2" class="infobox-subheader"><i><a href="/wiki/Drug_class" title="Drug class">Drug class</a></i></td></tr><tr><td colspan="2" class="infobox-image"><span class="skin-invert-image" typeof="mw:File"><a href="/wiki/File:Cetrorelix.svg" class="mw-file-description"><img src="//upload.wikimedia.org/wikipedia/commons/thumb/8/8b/Cetrorelix.svg/250px-Cetrorelix.svg.png" decoding="async" width="250" height="83" class="mw-file-element" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/8/8b/Cetrorelix.svg/375px-Cetrorelix.svg.png 1.5x, //upload.wikimedia.org/wikipedia/commons/thumb/8/8b/Cetrorelix.svg/500px-Cetrorelix.svg.png 2x" data-file-width="512" data-file-height="171" /></a></span><div class="infobox-caption"><a href="/wiki/Cetrorelix" title="Cetrorelix">Cetrorelix</a>, one of the most widely used <abbr title="gonadotropin-releasing hormone">GnRH</abbr> antagonists.</div></td></tr><tr><th colspan="2" class="infobox-header" style="background: #e8e8e8;">Class identifiers</th></tr><tr><th scope="row" class="infobox-label"><a href="/wiki/Synonym" title="Synonym">Synonyms</a></th><td class="infobox-data">GnRH receptor antagonists; GnRH blockers; GnRH inhibitors; Antigonadotropins</td></tr><tr><th scope="row" class="infobox-label">Use</th><td class="infobox-data"><a href="/wiki/Infertility" title="Infertility">Infertility</a>; <a href="/wiki/Prostate_cancer" title="Prostate cancer">Prostate cancer</a>; <a href="/wiki/Precocious_puberty" title="Precocious puberty">Precocious puberty</a>; <a href="/wiki/Breast_cancer" title="Breast cancer">Breast cancer</a>; <a href="/wiki/Endometriosis" title="Endometriosis">Endometriosis</a>; <a href="/wiki/Uterine_fibroid" title="Uterine fibroid">Uterine fibroids</a>; <a href="/wiki/Transgender" title="Transgender">Transgender people</a></td></tr><tr><th scope="row" class="infobox-label"><a href="/wiki/Biological_target" title="Biological target">Biological target</a></th><td class="infobox-data"><a href="/wiki/GnRH_receptor" class="mw-redirect" title="GnRH receptor">GnRH receptor</a></td></tr><tr><th scope="row" class="infobox-label"><a href="/wiki/Chemical_classification" class="mw-redirect" title="Chemical classification">Chemical class</a></th><td class="infobox-data"><a href="/wiki/Peptide" title="Peptide">Peptides</a>; <a href="/wiki/Non-peptide" class="mw-redirect" title="Non-peptide">Non-peptides</a></td></tr><tr><th colspan="2" class="infobox-header" style="background: #e8e8e8;">Legal status</th></tr><tr><td colspan="2" class="infobox-below" style="background: #e8e8e8; text-align: center"><a href="https://www.wikidata.org/wiki/Q3618379" class="extiw" title="d:Q3618379">In Wikidata</a></td></tr></tbody></table> <p><b>Gonadotropin-releasing hormone antagonists</b> (<b>GnRH antagonists</b>) are a class of medications that <a href="/wiki/Receptor_antagonist" title="Receptor antagonist">antagonize</a> the <a href="/wiki/Gonadotropin-releasing_hormone_receptor" title="Gonadotropin-releasing hormone receptor">gonadotropin-releasing hormone receptor</a> (GnRH receptor) and thus the action of <a href="/wiki/Gonadotropin-releasing_hormone" title="Gonadotropin-releasing hormone">gonadotropin-releasing hormone</a> (GnRH). They are used in the treatment of <a href="/wiki/Prostate_cancer" title="Prostate cancer">prostate cancer</a>, <a href="/wiki/Endometriosis" title="Endometriosis">endometriosis</a>, <a href="/wiki/Uterine_fibroids" class="mw-redirect" title="Uterine fibroids">uterine fibroids</a>, <a href="/wiki/Female_infertility" title="Female infertility">female infertility</a> in <a href="/wiki/Assisted_reproduction" class="mw-redirect" title="Assisted reproduction">assisted reproduction</a>, and for other indications. </p><p>Some GnRH antagonists, such as <a href="/wiki/Cetrorelix" title="Cetrorelix">cetrorelix</a>, are similar in structure to natural GnRH (a <a href="/wiki/Hormone" title="Hormone">hormone</a> made by <a href="/wiki/GnRH_Neuron" class="mw-redirect" title="GnRH Neuron">neurons</a> in the hypothalamus) but that have an antagonistic effect, while other GnRH antagonists, such as <a href="/wiki/Elagolix" title="Elagolix">elagolix</a> and <a href="/wiki/Relugolix" title="Relugolix">relugolix</a>, are <a href="/wiki/Non-peptide" class="mw-redirect" title="Non-peptide">non-peptide</a> and <a href="/wiki/Small-molecule" class="mw-redirect" title="Small-molecule">small-molecule</a> compounds. GnRH antagonists <a href="/wiki/Competitive_inhibition" title="Competitive inhibition">compete with natural GnRH for binding</a> to GnRH receptors, thus decreasing or blocking GnRH action in the body. </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=Gonadotropin-releasing_hormone_antagonist&action=edit&section=1" title="Edit section: Medical uses"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <div class="mw-heading mw-heading3"><h3 id="Prostate_cancer">Prostate cancer</h3><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Gonadotropin-releasing_hormone_antagonist&action=edit&section=2" title="Edit section: Prostate cancer"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>Testosterone promotes growth of many prostate <a href="/wiki/Tumor" class="mw-redirect" title="Tumor">tumors</a> and therefore reducing circulating testosterone to very low (<a href="/wiki/Castration" title="Castration">castration</a>) levels is often the treatment goal in the management of men with advanced prostate cancer. GnRH antagonists are used to provide fast suppression of testosterone without the surge in testosterone levels that is seen when treating patients with GnRH agonists.<sup id="cite_ref-Van_Poppel_Nilsson_1-0" class="reference"><a href="#cite_note-Van_Poppel_Nilsson-1"><span class="cite-bracket">[</span>1<span class="cite-bracket">]</span></a></sup> In patients with advanced disease, this surge in testosterone can lead to a flare-up of the tumour, which can precipitate a range of clinical symptoms such as <a href="/wiki/Bone_pain" title="Bone pain">bone pain</a>, <a href="/wiki/Urethral_obstruction" class="mw-redirect" title="Urethral obstruction">urethral obstruction</a>, and <a href="/wiki/Spinal_cord_compression" title="Spinal cord compression">spinal cord compression</a>. Drug agencies have issued warnings regarding this phenomenon in the prescribing information for GnRH agonists. As testosterone surge does not occur with GnRH antagonists, there is no need for patients to receive an <a href="/wiki/Antiandrogen" title="Antiandrogen">antiandrogen</a> as flare protection during prostate cancer treatment. GnRH agonists also induce an increase in testosterone levels after each reinjection of the drug – a phenomenon that does not occur with GnRH antagonists. </p><p>The reduction in testosterone levels that occurs during GnRH antagonist therapy subsequently reduces the size of the prostate cancer. This in turn results in a reduction in <a href="/wiki/Prostate-specific_antigen" title="Prostate-specific antigen">prostate-specific antigen</a> (PSA) levels in the patient's blood and so measuring PSA levels is a way to monitor how patients with prostate cancer are responding to treatment. GnRH antagonists have an immediate onset of action leading to a fast and profound suppression of testosterone and are therefore especially valuable in the treatment of patients with prostate cancer, where fast control of disease is needed. </p><p>The GnRH antagonist <a href="/wiki/Abarelix" title="Abarelix">abarelix</a> was withdrawn from the United States market in 2005 and is now only marketed in Germany for use in patients with symptomatic prostate cancer. <a href="/wiki/Degarelix" title="Degarelix">Degarelix</a> is a GnRH antagonist that is approved for use in patients with advanced hormone-sensitive prostate cancer throughout Europe and also in the United States.<sup id="cite_ref-2" class="reference"><a href="#cite_note-2"><span class="cite-bracket">[</span>2<span class="cite-bracket">]</span></a></sup> </p> <div class="mw-heading mw-heading3"><h3 id="Fertility_treatment">Fertility treatment</h3><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Gonadotropin-releasing_hormone_antagonist&action=edit&section=3" title="Edit section: Fertility treatment"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <style data-mw-deduplicate="TemplateStyles:r1236090951">.mw-parser-output .hatnote{font-style:italic}.mw-parser-output div.hatnote{padding-left:1.6em;margin-bottom:0.5em}.mw-parser-output .hatnote i{font-style:normal}.mw-parser-output .hatnote+link+.hatnote{margin-top:-0.5em}@media print{body.ns-0 .mw-parser-output .hatnote{display:none!important}}</style><div role="note" class="hatnote navigation-not-searchable">Further information: <a href="/wiki/Ovulation_suppression" class="mw-redirect" title="Ovulation suppression">Ovulation suppression</a></div> <p>GnRH antagonists are also used for short periods in the prevention of premature LH surge and endogenous <a href="/wiki/Ovulation" title="Ovulation">ovulation</a> in patients undergoing <a href="/wiki/Controlled_ovarian_hyperstimulation" title="Controlled ovarian hyperstimulation">ovarian hyperstimulation</a> with FSH in preparation for <a href="/wiki/In-vitro_fertilization" class="mw-redirect" title="In-vitro fertilization"><i>in-vitro</i> fertilization</a> (IVF).<sup id="cite_ref-3" class="reference"><a href="#cite_note-3"><span class="cite-bracket">[</span>3<span class="cite-bracket">]</span></a></sup><sup id="cite_ref-4" class="reference"><a href="#cite_note-4"><span class="cite-bracket">[</span>4<span class="cite-bracket">]</span></a></sup><sup id="cite_ref-5" class="reference"><a href="#cite_note-5"><span class="cite-bracket">[</span>5<span class="cite-bracket">]</span></a></sup> Typically they are administered in the mid-<a href="/wiki/Follicular_phase" title="Follicular phase">follicular phase</a> in stimulated cycles after administration of <a href="/wiki/Gonadotropins" class="mw-redirect" title="Gonadotropins">gonadotropins</a> and prior to the administration of hCG – which is given to stimulate ovulation. This protocol is likely beneficial in women expected to be hyper-responders, and probably also those expected to be poor responders to ovarian hyperstimulation.<sup id="cite_ref-6" class="reference"><a href="#cite_note-6"><span class="cite-bracket">[</span>6<span class="cite-bracket">]</span></a></sup> There is probably little or no difference between GnRH antagonist and GnRH agonist protocols in terms of live birth or risk of miscarriage but GnRH antagonists probably reduce the risk of ovarian hyperstimulation syndrome.<sup id="cite_ref-7" class="reference"><a href="#cite_note-7"><span class="cite-bracket">[</span>7<span class="cite-bracket">]</span></a></sup> The GnRH antagonists that are currently licensed for use in <a href="/wiki/Fertility_treatment" class="mw-redirect" title="Fertility treatment">fertility treatment</a> are cetrorelix and ganirelix. </p> <div class="mw-heading mw-heading3"><h3 id="Uterine_disorders">Uterine disorders</h3><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Gonadotropin-releasing_hormone_antagonist&action=edit&section=4" title="Edit section: Uterine disorders"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p><a href="/wiki/Elagolix" title="Elagolix">Elagolix</a> is indicated for the treatment of moderate to severe <a href="/wiki/Endometriosis" title="Endometriosis">endometriosis</a> pain and <a href="/wiki/Relugolix" title="Relugolix">relugolix</a> is indicated for the treatment of <a href="/wiki/Uterine_fibroid" title="Uterine fibroid">uterine fibroids</a>. </p> <div class="mw-heading mw-heading3"><h3 id="Other_uses">Other uses</h3><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Gonadotropin-releasing_hormone_antagonist&action=edit&section=5" title="Edit section: Other uses"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>GnRH antagonists are being investigated in the treatment of women with hormone-sensitive <a href="/wiki/Breast_cancer" title="Breast cancer">breast cancer</a>.<sup id="cite_ref-8" class="reference"><a href="#cite_note-8"><span class="cite-bracket">[</span>8<span class="cite-bracket">]</span></a></sup><sup id="cite_ref-9" class="reference"><a href="#cite_note-9"><span class="cite-bracket">[</span>9<span class="cite-bracket">]</span></a></sup> In men, they are being investigated in the treatment of <a href="/wiki/Benign_prostatic_hyperplasia" title="Benign prostatic hyperplasia">benign prostatic hyperplasia</a><sup id="cite_ref-10" class="reference"><a href="#cite_note-10"><span class="cite-bracket">[</span>10<span class="cite-bracket">]</span></a></sup> and also as potential <a href="/wiki/Contraceptive" class="mw-redirect" title="Contraceptive">contraceptive</a> agents.<sup id="cite_ref-11" class="reference"><a href="#cite_note-11"><span class="cite-bracket">[</span>11<span class="cite-bracket">]</span></a></sup> GnRH antagonists could be used as <a href="/wiki/Puberty_blocker" title="Puberty blocker">puberty blockers</a> in <a href="/wiki/Transgender_youth" title="Transgender youth">transgender youth</a> and to suppress <a href="/wiki/Sex_hormone" title="Sex hormone">sex hormone</a> levels in <a href="/wiki/Transgender" title="Transgender">transgender</a> adolescents and adults, but have not been studied in this context.<sup id="cite_ref-pmid28945902_12-0" class="reference"><a href="#cite_note-pmid28945902-12"><span class="cite-bracket">[</span>12<span class="cite-bracket">]</span></a></sup><sup id="cite_ref-pmid30256230_13-0" class="reference"><a href="#cite_note-pmid30256230-13"><span class="cite-bracket">[</span>13<span class="cite-bracket">]</span></a></sup><sup id="cite_ref-WiikAndersson2018_14-0" class="reference"><a href="#cite_note-WiikAndersson2018-14"><span class="cite-bracket">[</span>14<span class="cite-bracket">]</span></a></sup><sup id="cite_ref-Arasu2016_15-0" class="reference"><a href="#cite_note-Arasu2016-15"><span class="cite-bracket">[</span>15<span class="cite-bracket">]</span></a></sup> </p> <div class="mw-heading mw-heading3"><h3 id="Available_forms">Available forms</h3><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Gonadotropin-releasing_hormone_antagonist&action=edit&section=6" title="Edit section: Available forms"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <table class="wikitable sortable floatright" style="margin-left: auto; margin-right: auto; border: none;"> <caption class="nowrap">GnRH antagonists marketed for clinical or veterinary use </caption> <tbody><tr> <th>Name</th> <th>Brand/code name(s)</th> <th>Approved/intended uses</th> <th>Type</th> <th>Route(s)</th> <th>Launch/status<abbr title="(as of February 2018)">*</abbr></th> <th><abbr title="Google Search hits (February 2018)">Hits</abbr> </th></tr> <tr> <td><a href="/wiki/Abarelix" title="Abarelix">Abarelix</a></td> <td>Plenaxis</td> <td>Prostate cancer</td> <td>Peptide</td> <td><abbr title="Intramuscular injection">IM</abbr></td> <td>2003</td> <td>116,000 </td></tr> <tr> <td><a href="/wiki/Cetrorelix" title="Cetrorelix">Cetrorelix</a></td> <td>Cetrotide</td> <td>Female infertility (assisted reproduction)</td> <td>Peptide</td> <td><abbr title="Subcutaneous injection">SC</abbr></td> <td>2000</td> <td>134,000 </td></tr> <tr> <td><a href="/wiki/Degarelix" title="Degarelix">Degarelix</a></td> <td>Firmagon</td> <td>Prostate cancer</td> <td>Peptide</td> <td><abbr title="Subcutaneous injection">SC</abbr></td> <td>2008</td> <td>291,000 </td></tr> <tr> <td><a href="/wiki/Elagolix" title="Elagolix">Elagolix</a></td> <td>Orilissa</td> <td>Endometriosis; Uterine fibroids</td> <td>Non-peptide</td> <td>Oral</td> <td>2018</td> <td>126,000 </td></tr> <tr> <td><a href="/wiki/Ganirelix" title="Ganirelix">Ganirelix</a></td> <td>Orgalutran</td> <td>Female infertility (assisted reproduction)</td> <td>Peptide</td> <td><abbr title="Subcutaneous injection">SC</abbr></td> <td>2000</td> <td>134,000 </td></tr> <tr> <td><a href="/wiki/Linzagolix" title="Linzagolix">Linzagolix</a></td> <td>KLH-2109; OBE-2109</td> <td>Endometriosis; Uterine fibroids</td> <td>Non-peptide</td> <td>Oral</td> <td>Phase III<sup id="cite_ref-AdisInsight-KLH-2109_16-0" class="reference"><a href="#cite_note-AdisInsight-KLH-2109-16"><span class="cite-bracket">[</span>16<span class="cite-bracket">]</span></a></sup></td> <td>9,730 </td></tr> <tr> <td><a href="/wiki/Relugolix" title="Relugolix">Relugolix</a></td> <td>Relumina</td> <td>Uterine fibroids, prostate cancer</td> <td>Non-peptide</td> <td>Oral</td> <td>2019</td> <td>44,900 </td></tr> <tr class="sortbottom"> <td colspan="7" style="width: 1px; background-color:#eaecf0; text-align: center;"><b>Notes:</b> Launch/status = Launch year or developmental status (as of February 2018). Hits = Google Search hits (as of February 2018). </td></tr></tbody></table> <p>Currently approved GnRH antagonists include the <a href="/wiki/Peptide" title="Peptide">peptide</a> molecules <a href="/wiki/Abarelix" title="Abarelix">abarelix</a>, <a href="/wiki/Cetrorelix" title="Cetrorelix">cetrorelix</a>, <a href="/wiki/Degarelix" title="Degarelix">degarelix</a>, and <a href="/wiki/Ganirelix" title="Ganirelix">ganirelix</a> and the <a href="/wiki/Small-molecule" class="mw-redirect" title="Small-molecule">small-molecule</a> compounds <a href="/wiki/Elagolix" title="Elagolix">elagolix</a> and <a href="/wiki/Relugolix" title="Relugolix">relugolix</a>. GnRH antagonists are administered by <a href="/wiki/Subcutaneous_injection" class="mw-redirect" title="Subcutaneous injection">subcutaneous injection</a> (cetrorelix, degarelix, ganirelix), by <a href="/wiki/Intramuscular_injection" title="Intramuscular injection">intramuscular injection</a> (abarelix), or by <a href="/wiki/Oral_administration" title="Oral administration">oral administration</a> (elagolix, relugolix). </p><p>Another non-peptide and orally-active GnRH antagonist that is in development is <a href="/wiki/Linzagolix" title="Linzagolix">linzagolix</a>.<sup id="cite_ref-EzzatiCarr2015_17-0" class="reference"><a href="#cite_note-EzzatiCarr2015-17"><span class="cite-bracket">[</span>17<span class="cite-bracket">]</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=Gonadotropin-releasing_hormone_antagonist&action=edit&section=7" title="Edit section: Side effects"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>As with all hormonal therapies, GnRH antagonists are commonly associated with hormonal side effects such as <a href="/wiki/Hot_flushes" class="mw-redirect" title="Hot flushes">hot flushes</a>, <a href="/wiki/Headache" title="Headache">headache</a>, <a href="/wiki/Nausea" title="Nausea">nausea</a> and <a href="/wiki/Weight_gain" title="Weight gain">weight gain</a>.<sup id="cite_ref-Serono_18-0" class="reference"><a href="#cite_note-Serono-18"><span class="cite-bracket">[</span>18<span class="cite-bracket">]</span></a></sup><sup id="cite_ref-Degarelix_19-0" class="reference"><a href="#cite_note-Degarelix-19"><span class="cite-bracket">[</span>19<span class="cite-bracket">]</span></a></sup><sup id="cite_ref-Organon_20-0" class="reference"><a href="#cite_note-Organon-20"><span class="cite-bracket">[</span>20<span class="cite-bracket">]</span></a></sup> When used in fertility treatment they can also be associated with abdominal pain and ovarian hyperstimulation.<sup id="cite_ref-Serono_18-1" class="reference"><a href="#cite_note-Serono-18"><span class="cite-bracket">[</span>18<span class="cite-bracket">]</span></a></sup><sup id="cite_ref-Organon_20-1" class="reference"><a href="#cite_note-Organon-20"><span class="cite-bracket">[</span>20<span class="cite-bracket">]</span></a></sup> Subcutaneously administered agents are also associated with injection-site reactions<sup id="cite_ref-Degarelix_19-1" class="reference"><a href="#cite_note-Degarelix-19"><span class="cite-bracket">[</span>19<span class="cite-bracket">]</span></a></sup><sup id="cite_ref-21" class="reference"><a href="#cite_note-21"><span class="cite-bracket">[</span>21<span class="cite-bracket">]</span></a></sup> and <a href="/wiki/Abarelix" title="Abarelix">abarelix</a> (neither of these being GnRH agonists, but instead being antagonists) has been linked with immediate-onset systemic allergic reactions.<sup id="cite_ref-22" class="reference"><a href="#cite_note-22"><span class="cite-bracket">[</span>22<span class="cite-bracket">]</span></a></sup> </p> <div class="mw-heading mw-heading2"><h2 id="Pharmacology">Pharmacology</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Gonadotropin-releasing_hormone_antagonist&action=edit&section=8" title="Edit section: Pharmacology"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>GnRH antagonists competitively and reversibly bind to GnRH receptors in the <a href="/wiki/Pituitary_gland" title="Pituitary gland">pituitary gland</a>, blocking the release of <a href="/wiki/Luteinizing_hormone" title="Luteinizing hormone">luteinizing hormone</a> (LH) and <a href="/wiki/Follicle-stimulating_hormone" title="Follicle-stimulating hormone">follicle-stimulating hormone</a> (FSH) from the <a href="/wiki/Anterior_pituitary" title="Anterior pituitary">anterior pituitary</a>.<sup id="cite_ref-23" class="reference"><a href="#cite_note-23"><span class="cite-bracket">[</span>23<span class="cite-bracket">]</span></a></sup><sup id="cite_ref-24" class="reference"><a href="#cite_note-24"><span class="cite-bracket">[</span>24<span class="cite-bracket">]</span></a></sup> In men, the reduction in LH subsequently leads to rapid suppression of <a href="/wiki/Testosterone" title="Testosterone">testosterone</a> <a href="/wiki/Biosynthesis" title="Biosynthesis">production</a> in the <a href="/wiki/Testes" class="mw-redirect" title="Testes">testes</a>; in women it leads to suppression of <a href="/wiki/Estradiol" title="Estradiol">estradiol</a> and <a href="/wiki/Progesterone" title="Progesterone">progesterone</a> production from the <a href="/wiki/Ovaries" class="mw-redirect" title="Ovaries">ovaries</a>. GnRH antagonists are able to abolish <a href="/wiki/Gonad" title="Gonad">gonadal</a> sex hormone production and to suppress sex hormone levels into the <a href="/wiki/Castration" title="Castration">castrate</a> range, or by approximately 95%. </p><p>Unlike the GnRH agonists, which cause an initial stimulation of the <a href="/wiki/Hypothalamic%E2%80%93pituitary%E2%80%93gonadal_axis" title="Hypothalamic–pituitary–gonadal axis">hypothalamic–pituitary–gonadal axis</a> (HPG axis) that leads to a surge in testosterone or estrogen levels, GnRH antagonists have an immediate onset of action and rapidly reduce <a href="/wiki/Sex_hormone" title="Sex hormone">sex hormone</a> levels without an initial surge.<sup id="cite_ref-Van_Poppel_Nilsson_1-1" class="reference"><a href="#cite_note-Van_Poppel_Nilsson-1"><span class="cite-bracket">[</span>1<span class="cite-bracket">]</span></a></sup><sup id="cite_ref-Gustofson_25-0" class="reference"><a href="#cite_note-Gustofson-25"><span class="cite-bracket">[</span>25<span class="cite-bracket">]</span></a></sup> </p> <div class="skin-invert-image"><div class="center" style="width:auto; margin-left:auto; margin-right:auto;"><style data-mw-deduplicate="TemplateStyles:r1248256098">@media all and (max-width:720px){.mw-parser-output .mod-gallery{width:100%!important}}.mw-parser-output .mod-gallery{display:table}.mw-parser-output .mod-gallery-default{background:transparent;margin-top:4px}.mw-parser-output .mod-gallery-center{margin-left:auto;margin-right:auto}.mw-parser-output .mod-gallery-left{float:left}.mw-parser-output .mod-gallery-right{float:right}.mw-parser-output .mod-gallery-none{float:none}.mw-parser-output .mod-gallery-collapsible{width:100%}.mw-parser-output .mod-gallery .title,.mw-parser-output .mod-gallery .main,.mw-parser-output .mod-gallery .footer{display:table-row}.mw-parser-output .mod-gallery .title>div{display:table-cell;padding:0 4px 4px;text-align:center;font-weight:bold}.mw-parser-output .mod-gallery 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4em}html.skin-theme-clientpref-night .mw-parser-output .navbar li a abbr{color:var(--color-base)!important}@media(prefers-color-scheme:dark){html.skin-theme-clientpref-os .mw-parser-output .navbar li a abbr{color:var(--color-base)!important}}@media print{.mw-parser-output .navbar{display:none!important}}</style><div class="navbar plainlinks hlist navbar-mini"><ul><li class="nv-view"><a href="/wiki/Template:Hormone_levels_with_gonadotropin-releasing_hormone_agonists_and_antagonists" title="Template:Hormone levels with gonadotropin-releasing hormone agonists and antagonists"><abbr title="View this template">v</abbr></a></li><li class="nv-talk"><a href="/wiki/Template_talk:Hormone_levels_with_gonadotropin-releasing_hormone_agonists_and_antagonists" title="Template talk:Hormone levels with gonadotropin-releasing hormone agonists and antagonists"><abbr title="Discuss this template">t</abbr></a></li><li class="nv-edit"><a href="/wiki/Special:EditPage/Template:Hormone_levels_with_gonadotropin-releasing_hormone_agonists_and_antagonists" title="Special:EditPage/Template:Hormone levels with gonadotropin-releasing hormone agonists and antagonists"><abbr title="Edit this template">e</abbr></a></li></ul></div> Hormone levels with <a href="/wiki/Gonadotropin-releasing_hormone_agonist" title="Gonadotropin-releasing hormone agonist">GnRH agonists</a> and <a class="mw-selflink selflink">antagonists</a></div></div><div class="main"><div><ul class="gallery mw-gallery-traditional nochecker bordered-images whitebg"> <li class="gallerybox" style="width: 335px"> <div class="thumb" style="width: 330px; height: 255px;"><span typeof="mw:File"><a href="/wiki/File:Testosterone_levels_in_men_with_prostate_cancer_treated_with_GnRH_agonists_and_antagonists.png" class="mw-file-description" title="Testosterone levels during the first month of androgen deprivation therapy in men with prostate cancer treated with subcutaneous injections of a GnRH antagonist (degarelix) or agonist (leuprorelin). Doses were 240 then 80 mg/month and 7.5 mg/month, respectively.[26]"><img alt="Testosterone levels during the first month of androgen deprivation therapy in men with prostate cancer treated with subcutaneous injections of a GnRH antagonist (degarelix) or agonist (leuprorelin). Doses were 240 then 80 mg/month and 7.5 mg/month, respectively.[26]" src="//upload.wikimedia.org/wikipedia/commons/thumb/f/f8/Testosterone_levels_in_men_with_prostate_cancer_treated_with_GnRH_agonists_and_antagonists.png/300px-Testosterone_levels_in_men_with_prostate_cancer_treated_with_GnRH_agonists_and_antagonists.png" decoding="async" width="300" height="203" class="mw-file-element" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/f/f8/Testosterone_levels_in_men_with_prostate_cancer_treated_with_GnRH_agonists_and_antagonists.png/450px-Testosterone_levels_in_men_with_prostate_cancer_treated_with_GnRH_agonists_and_antagonists.png 1.5x, //upload.wikimedia.org/wikipedia/commons/thumb/f/f8/Testosterone_levels_in_men_with_prostate_cancer_treated_with_GnRH_agonists_and_antagonists.png/600px-Testosterone_levels_in_men_with_prostate_cancer_treated_with_GnRH_agonists_and_antagonists.png 2x" data-file-width="1626" data-file-height="1101" /></a></span></div> <div class="gallerytext">Testosterone levels during the first month of androgen deprivation therapy in men with prostate cancer treated with subcutaneous injections of a GnRH antagonist (degarelix) or agonist (leuprorelin). Doses were 240 then 80 mg/month and 7.5 mg/month, respectively.<sup id="cite_ref-26" class="reference"><a href="#cite_note-26"><span class="cite-bracket">[</span>26<span class="cite-bracket">]</span></a></sup></div> </li> <li class="gallerybox" style="width: 335px"> <div class="thumb" style="width: 330px; height: 255px;"><span typeof="mw:File"><a href="/wiki/File:Testosterone_levels_in_long-term_androgen_deprivation_therapy_with_different_GnRH_agonists.png" class="mw-file-description" title="Testosterone levels in the long-term androgen deprivation therapy of men with prostate cancer by different GnRH agonists administered at 3 month intervals (goserelin, triptorelin and leuprorelin). Dotted line is the threshold for the castrate range.[27]"><img alt="Testosterone levels in the long-term androgen deprivation therapy of men with prostate cancer by different GnRH agonists administered at 3 month intervals (goserelin, triptorelin and leuprorelin). Dotted line is the threshold for the castrate range.[27]" src="//upload.wikimedia.org/wikipedia/commons/thumb/3/39/Testosterone_levels_in_long-term_androgen_deprivation_therapy_with_different_GnRH_agonists.png/300px-Testosterone_levels_in_long-term_androgen_deprivation_therapy_with_different_GnRH_agonists.png" decoding="async" width="300" height="202" class="mw-file-element" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/3/39/Testosterone_levels_in_long-term_androgen_deprivation_therapy_with_different_GnRH_agonists.png/450px-Testosterone_levels_in_long-term_androgen_deprivation_therapy_with_different_GnRH_agonists.png 1.5x, //upload.wikimedia.org/wikipedia/commons/thumb/3/39/Testosterone_levels_in_long-term_androgen_deprivation_therapy_with_different_GnRH_agonists.png/600px-Testosterone_levels_in_long-term_androgen_deprivation_therapy_with_different_GnRH_agonists.png 2x" data-file-width="1635" data-file-height="1101" /></a></span></div> <div class="gallerytext">Testosterone levels in the long-term androgen deprivation therapy of men with prostate cancer by different GnRH agonists administered at 3 month intervals (goserelin, triptorelin and leuprorelin). Dotted line is the threshold for the castrate range.<sup id="cite_ref-27" class="reference"><a href="#cite_note-27"><span class="cite-bracket">[</span>27<span class="cite-bracket">]</span></a></sup></div> </li> </ul></div></div></div></div></div> <div class="mw-heading mw-heading2"><h2 id="Chemistry">Chemistry</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Gonadotropin-releasing_hormone_antagonist&action=edit&section=9" title="Edit section: Chemistry"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>GnRH antagonists include <a href="/wiki/Peptide" title="Peptide">peptides</a> such as <a href="/wiki/Cetrorelix" title="Cetrorelix">cetrorelix</a> and <a href="/wiki/Non-peptide" class="mw-redirect" title="Non-peptide">non-peptide</a> and <a href="/wiki/Small-molecule" class="mw-redirect" title="Small-molecule">small-molecule</a> compounds such as <a href="/wiki/Elagolix" title="Elagolix">elagolix</a>. Peptide GnRH antagonists are <a href="/wiki/GnRH_analogue" class="mw-redirect" title="GnRH analogue">GnRH analogues</a>. </p> <table class="wikitable mw-collapsible mw-collapsed" style="margin-left: auto; margin-right: auto; border: none;"> <caption class="nowrap">Chemical structures of peptide GnRH antagonists </caption> <tbody><tr> <th>Compound</th> <th>Amino acid sequence</th> <th>Marketed </th></tr> <tr> <td><a href="/wiki/Cetrorelix" title="Cetrorelix">Cetrorelix</a></td> <td>Ac-<span style="font-size:85%;">D</span>-Nal-<span style="font-size:85%;">D</span>-Cpa-<span style="font-size:85%;">D</span>-Pal-Ser-Tyr-<span style="font-size:85%;">D</span>-Cit-Leu-Arg-Pro-<span style="font-size:85%;">D</span>-Ala-NH<sub>2</sub></td> <td>Yes </td></tr> <tr> <td><a href="/wiki/Abarelix" title="Abarelix">Abarelix</a></td> <td>Ac-<span style="font-size:85%;">D</span>-Nal-<span style="font-size:85%;">D</span>-Cpa-<span style="font-size:85%;">D</span>-Pal-Ser-<i>N</i>-MeTyr-<span style="font-size:85%;">D</span>-Asn-Leu-Lys(iPr)-Pro-<span style="font-size:85%;">D</span>-Ala-NH<sub>2</sub></td> <td>Yes </td></tr> <tr> <td><a href="/wiki/Ganirelix" title="Ganirelix">Ganirelix</a></td> <td>Ac-<span style="font-size:85%;">D</span>-Nal-<span style="font-size:85%;">D</span>-Cpa-<span style="font-size:85%;">D</span>-Pal-Ser-Tyr-<span style="font-size:85%;">D</span>-hArg(Et)<sub>2</sub>-Leu-hArg(Et)<sub>2</sub>-Pro-<span style="font-size:85%;">D</span>-Ala-NH<sub>2</sub></td> <td>Yes </td></tr> <tr> <td><a href="/wiki/Degarelix" title="Degarelix">Degarelix</a></td> <td>Ac-<span style="font-size:85%;">D</span>-Nal-<span style="font-size:85%;">D</span>-Cpa-<span style="font-size:85%;">D</span>-Pal-Ser-Aph(Hor)-<span style="font-size:85%;">D</span>-Aph(Cba)-Leu-Lys(iPr)-Pro-<span style="font-size:85%;">D</span>-Ala-NH<sub>2</sub></td> <td>Yes </td></tr> <tr> <td><a href="/w/index.php?title=Teverelix&action=edit&redlink=1" class="new" title="Teverelix (page does not exist)">Teverelix</a></td> <td>Ac-<span style="font-size:85%;">D</span>-Nal-<span style="font-size:85%;">D</span>-Cpa-<span style="font-size:85%;">D</span>-Pal-Ser-Tyr-<span style="font-size:85%;">D</span>-hCit-Leu-Lys(iPr)-Pro-<span style="font-size:85%;">D</span>-Ala-NH<sub>2</sub></td> <td>No </td></tr> <tr> <td><a href="/wiki/Ozarelix" title="Ozarelix">Ozarelix</a></td> <td>Ac-<span style="font-size:85%;">D</span>-Nal-<span style="font-size:85%;">D</span>-Cpa-<span style="font-size:85%;">D</span>-Pal-Ser-<i>N</i>-MeTyr-<span style="font-size:85%;">D</span>-hCit-Nle-Arg-Pro-<span style="font-size:85%;">D</span>-Ala-NH<sub>2</sub></td> <td>No </td></tr> <tr> <td><a href="/w/index.php?title=Ornirelix&action=edit&redlink=1" class="new" title="Ornirelix (page does not exist)">Ornirelix</a></td> <td>Ac-<span style="font-size:85%;">D</span>-Nal-<span style="font-size:85%;">D</span>-Cpa-<span style="font-size:85%;">D</span>-Pal-Ser-Lys(Pic)-<span style="font-size:85%;">D</span>-Orn(6Anic)-Leu-Lys(iPr)-Pro-<span style="font-size:85%;">D</span>-Ala-NH<sub>2</sub></td> <td>No </td></tr> <tr> <td><a href="/w/index.php?title=Iturelix&action=edit&redlink=1" class="new" title="Iturelix (page does not exist)">Iturelix</a></td> <td>Ac-<span style="font-size:85%;">D</span>-Nal-<span style="font-size:85%;">D</span>-Cpa-<span style="font-size:85%;">D</span>-Pal-Ser-Lys(Nic)-<span style="font-size:85%;">D</span>-Lys(Nic)-Leu-Lys(iPr)-Pro-<span style="font-size:85%;">D</span>-Ala-NH<sub>2</sub></td> <td>No </td></tr> <tr> <td><a href="/wiki/Acyline" title="Acyline">Acyline</a></td> <td>Ac-<span style="font-size:85%;">D</span>-Nal-<span style="font-size:85%;">D</span>-Cpa-<span style="font-size:85%;">D</span>-Pal-Ser-Aph(Ac)-<span style="font-size:85%;">D</span>-Aph(Ac)-Leu-Lys(iPr)-Pro-<span style="font-size:85%;">D</span>-Ala-NH<sub>2</sub></td> <td>No </td></tr> <tr> <td><a href="/w/index.php?title=Azaline_B&action=edit&redlink=1" class="new" title="Azaline B (page does not exist)">Azaline B</a></td> <td>Ac-<span style="font-size:85%;">D</span>-Nal-<span style="font-size:85%;">D</span>-Cpa-<span style="font-size:85%;">D</span>-Pal-Ser-Aph(Atz)-<span style="font-size:85%;">D</span>-Aph(Atz)-Leu-Lys(iPr)-Pro-<span style="font-size:85%;">D</span>-Ala-NH<sub>2</sub></td> <td>No </td></tr> <tr class="sortbottom"> <td colspan="3" style="width: 1px; background-color:#eaecf0; text-align: center;"><b>Sources:</b> <sup id="cite_ref-pmid19939192_28-0" class="reference"><a href="#cite_note-pmid19939192-28"><span class="cite-bracket">[</span>28<span class="cite-bracket">]</span></a></sup> </td></tr></tbody></table> <div class="mw-heading mw-heading2"><h2 id="See_also">See also</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Gonadotropin-releasing_hormone_antagonist&action=edit&section=10" title="Edit section: See also"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <ul><li><a href="/wiki/Gonadotropin-releasing_hormone_modulator" title="Gonadotropin-releasing hormone modulator">Gonadotropin-releasing hormone modulator</a></li> <li><a href="/wiki/Gonadotropin-releasing_hormone_agonist" title="Gonadotropin-releasing hormone agonist">Gonadotropin-releasing hormone agonist</a></li></ul> <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=Gonadotropin-releasing_hormone_antagonist&action=edit&section=11" 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-Van_Poppel_Nilsson-1"><span class="mw-cite-backlink">^ <a href="#cite_ref-Van_Poppel_Nilsson_1-0"><sup><i><b>a</b></i></sup></a> <a href="#cite_ref-Van_Poppel_Nilsson_1-1"><sup><i><b>b</b></i></sup></a></span> <span class="reference-text">Van Poppel H, Nilsson S (June 2008). 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rel="nofollow" class="external text" href="https://api.semanticscholar.org/CorpusID:11906496">11906496</a>.</cite><span title="ctx_ver=Z39.88-2004&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&rft.genre=article&rft.jtitle=Expert+Opin+Ther+Pat&rft.atitle=Luteinizing+hormone-releasing+hormone+antagonists&rft.volume=19&rft.issue=12&rft.pages=1771-85&rft.date=2009-12&rft_id=https%3A%2F%2Fapi.semanticscholar.org%2FCorpusID%3A11906496%23id-name%3DS2CID&rft_id=info%3Apmid%2F19939192&rft_id=info%3Adoi%2F10.1517%2F13543770903410237&rft.aulast=Mezo&rft.aufirst=G&rft.au=Manea%2C+M&rft_id=http%3A%2F%2Fnbn-resolving.de%2Furn%3Anbn%3Ade%3Absz%3A352-opus-108412&rfr_id=info%3Asid%2Fen.wikipedia.org%3AGonadotropin-releasing+hormone+antagonist" 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 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href="mw-data:TemplateStyles:r1239400231"><div class="navbar plainlinks hlist navbar-mini"><ul><li class="nv-view"><a href="/wiki/Template:GnRH_and_gonadotropins" title="Template:GnRH and gonadotropins"><abbr title="View this template">v</abbr></a></li><li class="nv-talk"><a href="/wiki/Template_talk:GnRH_and_gonadotropins" title="Template talk:GnRH and gonadotropins"><abbr title="Discuss this template">t</abbr></a></li><li class="nv-edit"><a href="/wiki/Special:EditPage/Template:GnRH_and_gonadotropins" title="Special:EditPage/Template:GnRH and gonadotropins"><abbr title="Edit this template">e</abbr></a></li></ul></div><div id="GnRHTooltip_Gonadotropin-releasing_hormone_and_gonadotropins" style="font-size:114%;margin:0 4em"><a href="/wiki/Gonadotropin-releasing_hormone" title="Gonadotropin-releasing hormone"><abbr title="Gonadotropin-releasing hormone">GnRH</abbr></a><span class="sr-only" style="border: 0; clip: rect(0, 0, 0, 0); clip-path: polygon(0px 0px, 0px 0px, 0px 0px); height: 1px; margin: -1px; overflow: hidden; padding: 0; position: absolute; width: 1px; white-space: nowrap;">Tooltip Gonadotropin-releasing hormone</span> and <a href="/wiki/Gonadotropin" title="Gonadotropin">gonadotropins</a></div></th></tr><tr><th scope="row" class="navbox-group" style="width:1%;text-align:center;"><a href="/wiki/Gonadotropin-releasing_hormone_modulator" title="Gonadotropin-releasing hormone modulator"><abbr title="Gonadotropin-releasing hormone">GnRH</abbr> modulators</a><br />(incl. <a href="/wiki/Gonadotropin-releasing_hormone_analogue" class="mw-redirect" title="Gonadotropin-releasing hormone analogue">analogues</a>)</th><td class="navbox-list-with-group navbox-list navbox-odd hlist" style="width:100%;padding:0;background:#DDDDFF;"><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:9em;;text-align:center;"><a href="/wiki/Gonadotropin-releasing_hormone_agonist" title="Gonadotropin-releasing hormone agonist">Agonists</a></th><td class="navbox-list-with-group navbox-list navbox-odd" style="padding:0"><div style="padding:0 0.25em"> <ul><li><i>Peptide:</i> <a href="/wiki/Azagly-nafarelin" title="Azagly-nafarelin">Azagly-nafarelin</a></li> <li><a href="/wiki/Buserelin" title="Buserelin">Buserelin</a></li> <li><a href="/wiki/Deslorelin" title="Deslorelin">Deslorelin</a></li> <li><a href="/wiki/Fertirelin" title="Fertirelin">Fertirelin</a></li> <li><a href="/wiki/Gonadorelin" title="Gonadorelin">Gonadorelin</a></li> <li><a href="/wiki/Goserelin" title="Goserelin">Goserelin</a></li> <li><a href="/wiki/Histrelin" title="Histrelin">Histrelin</a></li> <li><a href="/wiki/Lecirelin" title="Lecirelin">Lecirelin</a></li> <li><a href="/wiki/Leuprorelin" title="Leuprorelin">Leuprorelin (leuprolide)</a></li> <li><a href="/wiki/Nafarelin" title="Nafarelin">Nafarelin</a></li> <li><a href="/wiki/Peforelin" title="Peforelin">Peforelin</a></li> <li><a href="/wiki/Triptorelin" title="Triptorelin">Triptorelin</a></li></ul> </div></td></tr><tr><th scope="row" class="navbox-group" style="width:9em;;text-align:center;"><a class="mw-selflink selflink">Antagonists</a></th><td class="navbox-list-with-group navbox-list navbox-even" style="padding:0"><div style="padding:0 0.25em"> <ul><li><i>Peptide:</i> <a href="/wiki/Abarelix" title="Abarelix">Abarelix</a></li> <li><a href="/wiki/Cetrorelix" title="Cetrorelix">Cetrorelix</a></li> <li><a href="/wiki/Degarelix" title="Degarelix">Degarelix</a></li> <li><a href="/wiki/Ganirelix" title="Ganirelix">Ganirelix</a></li></ul> <ul><li><i>Non-peptide:</i> <a href="/wiki/Elagolix" title="Elagolix">Elagolix</a></li> <li><a href="/wiki/Linzagolix" title="Linzagolix">Linzagolix</a><sup>†</sup></li> <li><a href="/wiki/Relugolix" title="Relugolix">Relugolix</a> (<a href="/wiki/Relugolix/estradiol/norethisterone_acetate" title="Relugolix/estradiol/norethisterone acetate">+estradiol/norethisterone acetate</a>)</li></ul> </div></td></tr></tbody></table><div></div></td></tr><tr><th scope="row" class="navbox-group" style="width:1%;text-align:center;"><a href="/wiki/Gonadotropin" title="Gonadotropin">Gonadotropins</a></th><td class="navbox-list-with-group navbox-list navbox-odd hlist" style="width:100%;padding:0;background:#DDDDFF;"><div style="padding:0 0.25em"></div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Preparations" scope="row" class="navbox-group" style="width:9em;;text-align:center;"><a href="/wiki/Gonadotropin_preparation" class="mw-redirect" title="Gonadotropin preparation">Preparations</a></th><td class="navbox-list-with-group navbox-list navbox-odd" style="padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Follicle-stimulating_hormone" title="Follicle-stimulating hormone">Follicle-stimulating hormone</a></li> <li><a href="/wiki/Human_chorionic_gonadotropin" title="Human chorionic gonadotropin">Human chorionic gonadotropin</a></li> <li><a href="/wiki/Luteinizing_hormone" title="Luteinizing hormone">Luteinizing hormone</a></li> <li><a href="/wiki/Menotropin" title="Menotropin">Menotropin</a></li> <li><a href="/wiki/Urofollitropin" title="Urofollitropin">Urofollitropin</a></li></ul> </div></td></tr></tbody></table><div></div></td></tr><tr><th scope="row" class="navbox-group" style="width:1%;text-align:center;">Others<br />(indirect)</th><td class="navbox-list-with-group navbox-list navbox-odd hlist" style="width:100%;padding:0;background:#DDDDFF;"><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:8em;;text-align:center;"><a href="/wiki/Progonadotropin" title="Progonadotropin">Progonadotropins</a></th><td class="navbox-list-with-group navbox-list navbox-even" style="padding:0"><div style="padding:0 0.25em"> <ul><li><i>Sex steroid antagonists (via disinhibition of the <a href="/wiki/Hypothalamic-pituitary-gonadal_axis" class="mw-redirect" title="Hypothalamic-pituitary-gonadal axis"><abbr title="hypothalamic–pituitary–gonadal">HPG</abbr> axis</a>):</i> <a href="/wiki/Antiandrogen" title="Antiandrogen">Antiandrogens</a> (e.g., <a href="/wiki/Flutamide" title="Flutamide">flutamide</a>, <a href="/wiki/Bicalutamide" title="Bicalutamide">bicalutamide</a>, <a href="/wiki/Enzalutamide" title="Enzalutamide">enzalutamide</a>)</li> <li><a href="/wiki/Antiestrogen" title="Antiestrogen">Antiestrogens</a>/<a href="/wiki/Selective_estrogen_receptor_modulators" class="mw-redirect" title="Selective estrogen receptor modulators"><abbr title="Selective estrogen receptor modulators">SERMs</abbr></a><span class="sr-only" style="border: 0; clip: rect(0, 0, 0, 0); clip-path: polygon(0px 0px, 0px 0px, 0px 0px); height: 1px; margin: -1px; overflow: hidden; padding: 0; position: absolute; width: 1px; white-space: nowrap;">Tooltip Selective estrogen receptor modulators</span> (e.g., <a href="/wiki/Tamoxifen" title="Tamoxifen">tamoxifen</a>, <a href="/wiki/Clomifene" title="Clomifene">clomifene</a>, <a href="/wiki/Enclomifene" title="Enclomifene">enclomifene</a>)</li> <li><a href="/wiki/Aromatase_inhibitor" title="Aromatase inhibitor">Aromatase inhibitors</a> (e.g., <a href="/wiki/Anastrozole" title="Anastrozole">anastrozole</a>)</li> <li><a href="/wiki/GnRH_agonist" class="mw-redirect" title="GnRH agonist"><abbr title="gonadotropin-releasing hormone">GnRH</abbr> agonists</a> (e.g., <a href="/wiki/Gonadotropin-releasing_hormone" title="Gonadotropin-releasing hormone"><abbr title="gonadotropin-releasing hormone">GnRH</abbr></a><span class="sr-only" style="border: 0; clip: rect(0, 0, 0, 0); clip-path: polygon(0px 0px, 0px 0px, 0px 0px); height: 1px; margin: -1px; overflow: hidden; padding: 0; position: absolute; width: 1px; white-space: nowrap;">Tooltip gonadotropin-releasing hormone</span>)</li></ul> </div></td></tr><tr><th scope="row" class="navbox-group" style="width:8em;;text-align:center;"><a href="/wiki/Antigonadotropin" title="Antigonadotropin">Antigonadotropins</a></th><td class="navbox-list-with-group navbox-list navbox-odd" style="padding:0"><div style="padding:0 0.25em"> <ul><li><i>Sex steroid agonists (via negative feedback on the <a href="/wiki/Hypothalamic-pituitary-gonadal_axis" class="mw-redirect" title="Hypothalamic-pituitary-gonadal axis"><abbr title="hypothalamic–pituitary–gonadal">HPG</abbr> axis</a>):</i> <a href="/wiki/Androgen" title="Androgen">Androgens</a>/<a href="/wiki/Anabolic_steroid" title="Anabolic steroid">anabolic steroids</a> (e.g., <a href="/wiki/Testosterone_(medication)" title="Testosterone (medication)">testosterone</a>, <a href="/wiki/Nandrolone_ester" class="mw-redirect" title="Nandrolone ester">nandrolone esters</a>, <a href="/wiki/Oxandrolone" title="Oxandrolone">oxandrolone</a>)</li> <li><a href="/wiki/D2_receptor" class="mw-redirect" title="D2 receptor">D<sub>2</sub> receptor</a> <a href="/wiki/Dopamine_antagonist" title="Dopamine antagonist">antagonists</a> (<a href="/wiki/Prolactin_releaser" class="mw-redirect" title="Prolactin releaser">prolactin releasers</a>) (incl., <a href="/wiki/Domperidone" title="Domperidone">domperidone</a>, <a href="/wiki/Metoclopramide" title="Metoclopramide">metoclopramide</a>, <a href="/wiki/Risperidone" title="Risperidone">risperidone</a>, <a href="/wiki/Haloperidol" title="Haloperidol">haloperidol</a>, <a href="/wiki/Chlorpromazine" title="Chlorpromazine">chlorpromazine</a>, <a href="/wiki/Sulpiride" title="Sulpiride">sulpiride</a>)</li> <li><a href="/wiki/Estrogen_(medication)" title="Estrogen (medication)">Estrogens</a> (incl., <a href="/wiki/Bifluranol" title="Bifluranol">bifluranol</a>, <a href="/wiki/Estradiol_(medication)" title="Estradiol (medication)">estradiol</a>, <a href="/wiki/Estradiol_ester" class="mw-redirect" title="Estradiol ester">estradiol esters</a>, <a href="/wiki/Ethinylestradiol" title="Ethinylestradiol">ethinylestradiol</a>, <a href="/wiki/Diethylstilbestrol" title="Diethylstilbestrol">diethylstilbestrol</a>, <a href="/wiki/Paroxypropione" title="Paroxypropione">paroxypropione</a>)</li> <li><a href="/wiki/Progestogen" title="Progestogen">Progestogens</a> (incl. <a href="/wiki/Progestin" class="mw-redirect" title="Progestin">progestins</a>, e.g., <a href="/wiki/Chlormadinone_acetate" title="Chlormadinone acetate">chlormadinone acetate</a>, <a href="/wiki/Cyproterone_acetate" title="Cyproterone acetate">cyproterone acetate</a>, <a href="/wiki/Hydroxyprogesterone_caproate" title="Hydroxyprogesterone caproate">hydroxyprogesterone caproate</a>, <a href="/wiki/Gestonorone_caproate" title="Gestonorone caproate">gestonorone caproate</a>, <a href="/wiki/Medroxyprogesterone_acetate" title="Medroxyprogesterone acetate">medroxyprogesterone acetate</a>, <a href="/wiki/Megestrol_acetate" title="Megestrol acetate">megestrol acetate</a>)</li></ul> <ul><li><i>Others (mixed or unknown mechanism of action):</i> <a href="/wiki/Danazol" title="Danazol">Danazol</a></li> <li><a href="/wiki/Gestrinone" title="Gestrinone">Gestrinone</a></li> <li><a href="/wiki/Metallibure" title="Metallibure">Metallibure</a></li></ul> </div></td></tr></tbody></table><div></div></td></tr><tr><td colspan="2" class="navbox-list navbox-even hlist" style="width:100%;padding:0;background:#DDDDFF;"><div style="padding:0 0.25em"><div class="hlist"> <ul><li><sup>#</sup><a href="/wiki/WHO_Model_List_of_Essential_Medicines" title="WHO Model List of Essential Medicines">WHO-EM</a></li> <li><sup>‡</sup><a href="/wiki/List_of_withdrawn_drugs" title="List of withdrawn drugs">Withdrawn</a> from market</li> <li><a href="/wiki/Clinical_trial" title="Clinical trial">Clinical trials</a>: <ul><li><sup>†</sup><a href="/wiki/Phases_of_clinical_research#Phase_III" title="Phases of clinical research">Phase III</a></li> <li><sup>§</sup>Never to phase III</li></ul></li></ul> </div> <dl><dt>See also</dt> <dd><a href="/wiki/Template:GnRH_and_gonadotropin_receptor_modulators" title="Template:GnRH and gonadotropin receptor modulators"><abbr title="gonadotropin-releasing hormone">GnRH</abbr> and gonadotropin receptor modulators</a></dd> <dd><a href="/wiki/Template:Androgens_and_antiandrogens" title="Template:Androgens and antiandrogens">Androgens and antiandrogens</a></dd> <dd><a href="/wiki/Template:Estrogens_and_antiestrogens" title="Template:Estrogens and antiestrogens">Estrogens and antiestrogens</a></dd> <dd><a href="/wiki/Template:Progestogens_and_antiprogestogens" title="Template:Progestogens and antiprogestogens">Progestogens and antiprogestogens</a></dd></dl></div></td></tr></tbody></table></div> <div class="navbox-styles"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1129693374"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1236075235"></div><div role="navigation" class="navbox" aria-labelledby="GnRHTooltip_Gonadotropin-releasing_hormone_receptor_and_gonadotropin_receptor_modulators" style="padding:3px"><table class="nowraplinks hlist mw-collapsible mw-collapsed navbox-inner" style="border-spacing:0;background:transparent;color:inherit"><tbody><tr><th scope="col" class="navbox-title" colspan="2"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1129693374"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1239400231"><div class="navbar plainlinks hlist navbar-mini"><ul><li class="nv-view"><a href="/wiki/Template:GnRH_and_gonadotropin_receptor_modulators" title="Template:GnRH and gonadotropin receptor modulators"><abbr title="View this template">v</abbr></a></li><li class="nv-talk"><a href="/wiki/Template_talk:GnRH_and_gonadotropin_receptor_modulators" title="Template talk:GnRH and gonadotropin receptor modulators"><abbr title="Discuss this template">t</abbr></a></li><li class="nv-edit"><a href="/wiki/Special:EditPage/Template:GnRH_and_gonadotropin_receptor_modulators" title="Special:EditPage/Template:GnRH and gonadotropin receptor modulators"><abbr title="Edit this template">e</abbr></a></li></ul></div><div id="GnRHTooltip_Gonadotropin-releasing_hormone_receptor_and_gonadotropin_receptor_modulators" style="font-size:114%;margin:0 4em"><a href="/wiki/Gonadotropin-releasing_hormone_receptor" title="Gonadotropin-releasing hormone receptor"><abbr title="Gonadotropin-releasing hormone receptor">GnRH</abbr></a><span class="sr-only" style="border: 0; clip: rect(0, 0, 0, 0); clip-path: polygon(0px 0px, 0px 0px, 0px 0px); height: 1px; margin: -1px; overflow: hidden; padding: 0; position: absolute; width: 1px; white-space: nowrap;">Tooltip Gonadotropin-releasing hormone receptor</span> and <a href="/wiki/Gonadotropin_receptor" title="Gonadotropin receptor">gonadotropin receptor</a> <a href="/wiki/Receptor_modulator" title="Receptor modulator">modulators</a></div></th></tr><tr><th scope="row" class="navbox-group" style="width:1%;text-align:center;"><a href="/wiki/Gonadotropin-releasing_hormone_receptor" title="Gonadotropin-releasing hormone receptor"><abbr title="Gonadotropin-releasing hormone receptor">GnRH</abbr></a><span class="sr-only" style="border: 0; clip: rect(0, 0, 0, 0); clip-path: polygon(0px 0px, 0px 0px, 0px 0px); height: 1px; margin: -1px; overflow: hidden; padding: 0; position: absolute; width: 1px; white-space: nowrap;">Tooltip Gonadotropin-releasing hormone receptor</span></th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><i>Agonists:</i> <i>Peptides:</i> <a href="/w/index.php?title=Alarelin&action=edit&redlink=1" class="new" title="Alarelin (page does not exist)">Alarelin</a></li> <li><a href="/w/index.php?title=Avorelin&action=edit&redlink=1" class="new" title="Avorelin (page does not exist)">Avorelin</a></li> <li><a href="/wiki/Azagly-nafarelin" title="Azagly-nafarelin">Azagly-nafarelin</a></li> <li><a href="/wiki/Buserelin" title="Buserelin">Buserelin</a></li> <li><a href="/wiki/Deslorelin" title="Deslorelin">Deslorelin</a></li> <li><a href="/wiki/Fertirelin" title="Fertirelin">Fertirelin</a></li> <li><a href="/wiki/Gonadotropin-releasing_hormone" title="Gonadotropin-releasing hormone">GnRH</a></li> <li><a href="/wiki/Gonadorelin" title="Gonadorelin">Gonadorelin</a></li> <li><a href="/wiki/Goserelin" title="Goserelin">Goserelin</a></li> <li><a href="/wiki/Histrelin" title="Histrelin">Histrelin</a></li> <li><a href="/wiki/Leuprorelin" title="Leuprorelin">Leuprorelin (leuprolide)</a></li> <li><a href="/w/index.php?title=Lutrelin&action=edit&redlink=1" class="new" title="Lutrelin (page does not exist)">Lutrelin</a></li> <li><a href="/wiki/Nafarelin" title="Nafarelin">Nafarelin</a></li> <li><a href="/wiki/Peforelin" title="Peforelin">Peforelin</a></li> <li><a href="/w/index.php?title=Salmon_GnRH&action=edit&redlink=1" class="new" title="Salmon GnRH (page does not exist)">Salmon GnRH</a></li> <li><a href="/wiki/Triptorelin" title="Triptorelin">Triptorelin</a></li> <li><a href="/w/index.php?title=Zoptarelin&action=edit&redlink=1" class="new" title="Zoptarelin (page does not exist)">Zoptarelin</a></li> <li><a href="/wiki/Zoptarelin_doxorubicin" title="Zoptarelin doxorubicin">Zoptarelin doxorubicin</a></li></ul> <ul><li><i>Antagonists:</i> <i>Peptides:</i> <a href="/wiki/Abarelix" title="Abarelix">Abarelix</a></li> <li><a href="/wiki/Acyline" title="Acyline">Acyline</a></li> <li><a href="/w/index.php?title=Azaline_B&action=edit&redlink=1" class="new" title="Azaline B (page does not exist)">Azaline B</a></li> <li><a href="/wiki/Cetrorelix" title="Cetrorelix">Cetrorelix</a></li> <li><a href="/wiki/Degarelix" title="Degarelix">Degarelix</a></li> <li><a href="/w/index.php?title=Detirelix&action=edit&redlink=1" class="new" title="Detirelix (page does not exist)">Detirelix</a></li> <li><a href="/wiki/Ganirelix" title="Ganirelix">Ganirelix</a></li> <li><a href="/w/index.php?title=Iturelix&action=edit&redlink=1" class="new" title="Iturelix (page does not exist)">Iturelix (antide)</a></li> <li><a href="/w/index.php?title=LXT-101&action=edit&redlink=1" class="new" title="LXT-101 (page does not exist)">LXT-101</a></li> <li><a href="/w/index.php?title=Ornirelix&action=edit&redlink=1" class="new" title="Ornirelix (page does not exist)">Ornirelix (ornitide)</a></li> <li><a href="/wiki/Ozarelix" title="Ozarelix">Ozarelix</a></li> <li><a href="/w/index.php?title=Prazarelix&action=edit&redlink=1" class="new" title="Prazarelix (page does not exist)">Prazarelix</a></li> <li><a href="/w/index.php?title=Ramorelix&action=edit&redlink=1" class="new" title="Ramorelix (page does not exist)">Ramorelix</a></li> <li><a href="/w/index.php?title=Teverelix&action=edit&redlink=1" class="new" title="Teverelix (page does not exist)">Teverelix (antarelix)</a>; <i>Non-peptides:</i> <a href="/wiki/Elagolix" title="Elagolix">Elagolix</a></li> <li><a href="/wiki/Linzagolix" title="Linzagolix">Linzagolix</a></li> <li><a href="/wiki/Opigolix" title="Opigolix">Opigolix</a></li> <li><a href="/wiki/Relugolix" title="Relugolix">Relugolix</a></li> <li><a href="/wiki/Sufugolix" title="Sufugolix">Sufugolix</a></li></ul> </div></td></tr><tr><th scope="row" class="navbox-group" style="width:1%;text-align:center;"><a href="/wiki/Gonadotropin_receptor" title="Gonadotropin receptor">Gonadotropin</a></th><td class="navbox-list-with-group navbox-list navbox-odd" 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%;text-align:center;"><a href="/wiki/Luteinizing_hormone/choriogonadotropin_receptor" title="Luteinizing hormone/choriogonadotropin receptor"><abbr title="Luteinizing hormone/choriogonadotropin receptor">LH/hCG</abbr></a><span class="sr-only" style="border: 0; clip: rect(0, 0, 0, 0); clip-path: polygon(0px 0px, 0px 0px, 0px 0px); height: 1px; margin: -1px; overflow: hidden; padding: 0; position: absolute; width: 1px; white-space: nowrap;">Tooltip Luteinizing hormone/choriogonadotropin receptor</span></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>Agonists:</i> <i>Peptides:</i> <a href="/wiki/Choriogonadotropin_alfa" class="mw-redirect" title="Choriogonadotropin alfa">Choriogonadotropin alfa</a></li> <li><a href="/wiki/Human_chorionic_gonadotropin" title="Human chorionic gonadotropin">Human chorionic gonadotropin</a></li> <li><a href="/wiki/Luteinizing_hormone" title="Luteinizing hormone">Luteinizing hormone</a></li> <li><a href="/wiki/Lutropin_alfa" class="mw-redirect" title="Lutropin alfa">Lutropin alfa</a></li> <li><a href="/wiki/Menotropin" title="Menotropin">Menotropin (human menopausal gonadotropin)</a></li></ul> </div></td></tr><tr><th scope="row" class="navbox-group" style="width:1%;text-align:center;"><a href="/wiki/Follicle-stimulating_hormone_receptor" title="Follicle-stimulating hormone receptor"><abbr title="Follicle-stimulating hormone receptor">FSH</abbr></a><span class="sr-only" style="border: 0; clip: rect(0, 0, 0, 0); clip-path: polygon(0px 0px, 0px 0px, 0px 0px); height: 1px; margin: -1px; overflow: hidden; padding: 0; position: absolute; width: 1px; white-space: nowrap;">Tooltip Follicle-stimulating hormone receptor</span></th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><i>Agonists:</i> <i>Peptides:</i> <a href="/wiki/Corifollitropin_alfa" class="mw-redirect" title="Corifollitropin alfa">Corifollitropin alfa</a></li> <li><a href="/wiki/Follicle-stimulating_hormone" title="Follicle-stimulating hormone">Follicle-stimulating hormone</a></li> <li><a href="/wiki/Follitropin_alfa" class="mw-redirect" title="Follitropin alfa">Follitropin alfa</a></li> <li><a href="/wiki/Follitropin_beta" class="mw-redirect" title="Follitropin beta">Follitropin beta</a></li> <li><a href="/w/index.php?title=Follitropin_epsilon&action=edit&redlink=1" class="new" title="Follitropin epsilon (page does not exist)">Follitropin epsilon</a></li> <li><a href="/wiki/Menotropin" title="Menotropin">Menotropin (human menopausal gonadotropin)</a></li> <li><a href="/wiki/Urofollitropin" title="Urofollitropin">Urofollitropin</a></li> <li><a href="/w/index.php?title=Varfollitropin_alfa&action=edit&redlink=1" class="new" title="Varfollitropin alfa (page does not exist)">Varfollitropin alfa</a></li></ul> <ul><li><i><abbr title="negative allosteric modulators">NAMs</abbr>:</i> <i>Non-peptides:</i> <a href="/w/index.php?title=ADX-61623&action=edit&redlink=1" class="new" title="ADX-61623 (page does not exist)">ADX-61623</a></li></ul> </div></td></tr></tbody></table><div></div></td></tr></tbody></table></div>    </div><noscript><img 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