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Anticancer Agent "TASFYGO Tablets 35mg" (Tasurgratinib Succinate) Launches in Japan for Biliary Tract Cancer with FGFR2 Gene Fusion or Rearrangements

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Tablets 35mg&rdquo; (generic name: tasurgratinib succinate) in Japan for the treatment of patients with unresectable biliary tract cancer with FGFR2 gene fusions or rearrangements that progressed after cancer chemotherapy. The product received manufacturing and marketing approval in Japan on September 24, 2024, and was published in Japan&rsquo;s National Health Insurance Drug Price List today.<br><br><img style="display: block; margin-left: auto; margin-right: auto;" src="https://photos.acnnewswire.com/TASFYGO.jpg" alt="" width="380" height="214"></p> <p>Discovered in-house by Eisai&rsquo;s Tsukuba Research Laboratories, TASFYGO is an orally available novel tyrosine kinase inhibitor that demonstrates selective inhibitory activity against FGFR1, FGFR2 and FGFR3.</p> <p>The approval of TASFYGO in Japan is based on data such as the results of a multicenter, open-label, single- arm clinical phase II trial (Study 201) conducted by Eisai in Japan and China.1 A companion diagnostic test to detect FGFR2 gene fusions or rearrangements for the use of TASFYGO in biliary tract cancer, &ldquo;AmoyDx&reg; FGFR2 Break-apart FISH Probe Kit&rdquo; by Nihon Stery, Inc. (Headquarters: Tokyo) was approved in August 2024.(2)</p> <p>The estimated number of patients in Japan with biliary tract cancer is approximately 22,000,(3),(4) with approximately 25% of the five-year relative survival rate,(3) making it an intractable cancer with the second worst prognosis following pancreatic cancer. Since drug therapy options are limited in comparison with other cancers, it is a disease with significant unmet medical needs. FGFR2 gene fusions or rearrangements are observed in approximately 5-14% of intrahepatic cholangiocarcinoma, which accounts for 15-30% of biliary tract cancers.(5),(6),(7) FGFR genetic aberrations such as the gene fusions are known to be deeply involved in the proliferation, survival and migration of cancer cells as well as tumor angiogenesis and drug resistance. As these genetic aberrations in FGFRs have been observed in various other types of cancers as well as biliary tract cancer, there is growing interest in FGFRs as a promising target for cancer therapy.</p> <p>TASFYGO is produced at the Kawashima Industrial Park (Gifu Prefecture), using innovative Continuous Manufacturing and Real Time Release Testing, a manufacturing technology that ensures product quality within production processes. Continuous Manufacturing is a production method in which processing is carried out continuously from raw material input to formulation. By incorporating real-time quality monitoring technology, multiple manufacturing processes are integrated, enabling automatic production. This method allows for higher quality control compared to conventional processes that focus on product release testing, by utilizing data within the manufacturing process and reducing human-error through automation.</p> <p>Eisai aims to make continuous efforts to meet the diversified needs of and increase the benefits provided to patients with cancer, their families, and healthcare professionals, by delivering TASFYGO as a new treatment option for biliary tract cancer with FGFR2 gene fusions or rearrangements.</p> <p><strong>Product Information</strong></p> <p>Brand name: TASFYGO&reg; Tablets 35mg Generic name: Tasurgratinib succinate</p> <p>Indications: Unresectable biliary tract cancer with FGFR2 gene fusions or rearrangements that progressed after cancer chemotherapy</p> <p>Dosage and Administration: The usual adult dose of tasurgratinib is 140mg orally once daily under fasting conditions. The dose may be reduced appropriately according to the condition of the patient.</p> <p>National Health Insurance (NHI) Drug Price: TASFYGO Tablets 35 mg: &yen; 15,378.70 (per 1 tablet) Packaging: TASFYGO Tablets 35 mg: 56 tablets (14 tablet PTP sheet X 4)</p> <p><strong>About &ldquo;TASFYGO&reg; Tablets 35mg&rdquo; (tasurgratinib succinate, Development Code: E7090)</strong></p> <p>Discovered in-house by Eisai&rsquo;s Tsukuba Research Laboratories, TASFYGO is an orally available novel tyrosine kinase inhibitor that demonstrates selective inhibitory activity against fibroblast growth factor receptors (FGFR) FGFR1, FGFR2 and FGFR3. Distinct from prior known FGFR inhibitors, TASFYGO has a basic structure which lacks the dimethoxyphenyl moiety, and in a kinetic interaction analysis study, it was observed that TASFYGO demonstrates antitumor activities due to inhibition of kinase activity with a binding mode (Type V) that exhibits rapid and potent binding as well as high selectivity to FGFR.(8),(9)</p> <p>In non-clinical studies for biliary tract cancer, NIH/3T3 cells expressing FGFR2-AHCYL1, FGFR2-KCTD1, FGFR2-BICC1 or FGFR2-TXLNA as FGFR2-fusion genes, provided by the National Cancer Center Japan, were used. The antitumor activity of TASFYGO against FGFR2 gene fusion-positive cancers was confirmed in these models by evaluating its effect on anchorage-independent growth and subcutaneously transplanted tumor growth in mice.(9)</p> <p>A Phase I clinical trial is underway in Japan in patients with estrogen receptor-positive and HER2-negative breast cancer.</p> <p><strong>About Real Time Release Testing</strong></p> <p>Real Time Release Testing is a quality control approach that ensures the quality of final products based on data from within the manufacturing process. Applying Real Time Release Testing requires a quality design approach based on Quality by Design (QbD), an advanced development method for manufacturing processes. QbD is a development method that emphasizes process control based on profound understanding of manufacturing processes, rather than conventional quality assurance methods which mainly focus on product release testing.</p> <p>Eisai integrates Process Analytical Technology (PAT) into QbD to achieve a higher level of quality control by managing critical attributes of pharmaceuticals within the production process.</p> <p>(1) Furuse J. et al. Pivotal single-arm, phase 2 trial of tasurgratinib for patients with fibroblast growth factor receptor&nbsp;(FGFR)-2 gene fusion-positive cholangiocarcinoma (CCA). 2024 ASCO Gastrointestinal Cancers Symposium; Abstract No. 471. <a href="https://ascopubs.org/doi/pdf/10.1200/JCO.2024.42.3_suppl.471">https://ascopubs.org/doi/pdf/10.1200/JCO.2024.42.3_suppl.471</a><br>(2) AmoyDx&reg; FGFR2 Break-apart FISH Probe Kit Approved as Companion Diagnostic for Eisai&rsquo;s Tasurgratinib in Japan. Available at: https://www.amoydiagnostics.com/about/press-releases/245 Last accessed: September 2024.<br>(3) Latest statistics, Cancer Information Service, National Cancer Center, Japan. (Japanese only)<br>(4) The 23rd Follow-up Survey Reports for Primary Liver Cancer Cases in Japan (2014-2015), 2023. (Japanese only)<br>(5) Arai Y. et al., Fibroblast growth factor receptor 2 tyrosine kinase fusions define a unique molecular subtype of cholangiocarcinoma, Hepatology, 2014, 59, 1427-1434.<br>(6) Maruki Y. et al., Molecular detection and clinicopathological characteristics of advanced/recurrent biliary tract carcinomas harboring the FGFR2 rearrangements: a prospective observational study (PRELUDE Study), J Gastroenterol. 2021; 56(3), 250-260.<br>(7) Tsujie M. et al., Fibroblast growth factor receptor 2 (FGFR2) fusions in Japanese patients with intrahepatic cholangiocarcinoma, Jpn J Clin Oncol. 2021; 51(6): 911-917.<br>(8) Miyano SW. et al., E7090, a Novel Selective Inhibitor of Fibroblast Growth Factor Receptors, Displays Potent Antitumor Activity and Prolongs Survival in Preclinical Models, Molecular Cancer Therapeutics, 2016, 15, 2630-2639.<br>(9) Kawano S. et al., Antitumor Activity of Tasurgratinib as an Orally Available FGFR1-3 Inhibitor in Cholangiocarcinoma Models With FGFR2-fusion, Anticancer Research, 2024, 44, 2393-2406.</p> <p>Media Inquiries:<br>Public Relations Department, Eisai Co., Ltd.<br>+81-(0)3-3817-5120</p></span></div> <div align="justify"><span id="MainContent_CompanyName" class="bodytext"></span></div> <div align="justify"><span id="MainContent_CompanyBoiler" class="bodytext"></span></div> <div align="justify"><span id="MainContent_Contact" class="bodytext"></span></div> <div align="justify"><span id="MainContent_Source" class="note">Source: Eisai<BR />Sectors: Healthcare & Pharm <BR /><BR /></span></div> <div align="justify"><span id="MainContent_Copyright" class="bodytext"><p>Copyright 漏2024 JCN Newswire. 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