About PEMAZYRE — 2 of 3
PEMAZYRE is the first approved, molecularly targeted treatment for FGFR2 fusion-positive CCA
Pemigatinib is a potent inhibitor of FGFR1, 2 and 31,27
- Pemigatinib is a kinase inhibitor of FGFR1, 2 and 3. It inhibits FGFR phosphorylation and signalling and decreases cell viability in cells expressing FGFR genetic alterations, including point mutations, amplifications, and fusions or rearrangements1
- FGFR2 fusions are strong oncogenic drivers and are the most common FGFR alteration, occurring almost exclusively in 10–16% of iCCA1
Adapted from PEMAZYRE® (pemigatinib) Swissmedic Professorial Information, June 2021; ref. 1.
- PEMAZYRE® (pemigatinib) Swissmedic Professional Information, June 2021; https://www.swissmedicinfo.ch/ (accessed 02 December 2021).
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- Bañales JM, et al. Expert consensus document: Cholangiocarcinoma: Current knowledge and future perspectives consensus statement from the European Network for the Study of Cholangiocarcinoma (ENS-CCA). Nat Rev Gastroenterol Hepatol. 2016;13:261–80.
- Bertuccio P, et al. A comparison of trends in mortality from primary liver cancer and intrahepatic cholangiocarcinoma in Europe. Ann Oncol. 2013;24:1667–74.
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- Valle JW, et al. Biliary cancer: ESMO Clinical Practice Guidelines for diagnosis, treatment and follow-up. Ann Oncol. 2016;27(suppl 5):v28–v37.
- Lamarca A, et al. Advanced intrahepatic cholangiocarcinoma: Post hoc analysis of the ABC-01, -02, and -03 clinical trials. J Natl Cancer Inst. 2020;112:200–10.
- Valle JW, et al. Cisplatin plus gemcitabine versus gemcitabine for biliary tract cancer. N Engl J Med. 2010;362:1273–81.
- Lamarca A, et al. Second-line FOLFOX chemotherapy versus active symptom control for advanced biliary tract cancer (ABC-06): A phase 3, open-label, randomised, controlled trial. Lancet Oncol. 2021;22:690–701.
- Lowery MA, et al. Comprehensive molecular profiling of intrahepatic and extrahepatic cholangiocarcinomas: potential targets for intervention. Clin Cancer Res. 2018;24:4154–61.
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- Churi CR, et al. Mutation profiling in cholangiocarcinoma: Prognostic and therapeutic implications. PLoS One. 2014;9:e115383.
- Arai Y, et al. Fibroblast growth factor receptor 2 tyrosine kinase fusions define a unique molecular subtype of cholangiocarcinoma. Hepatology. 2014;59:1427–34.
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- Silverman IM, et al. Clinicogenomic analysis of FGFR2-rearranged cholangiocarcinoma identifies correlates of response and mechanisms of resistance to pemigatinib. Cancer Discov. 2021;11:326–39.
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All references are available upon request
Abbreviated Prescribing Information
▼ This medicinal product is subject to additional monitorings. For further information, see product information Pemazyre on www.swissmedicinfo.ch.PEMAZYRE (pemigatinib), tablets of 13.5 mg, 9 mg, 4.5 mg. I: : As monotherapy for the treatment of adults with locally advanced, unresectable or metastatic cholangiocarcinoma with a fibroblast growth factor receptor 2 (FGFR2) fusion or rearrangement that have progressed after at least one line of systemic therapy. P: Treatment should be initiated by a physician experienced in the diagnosis and treatment of patients with biliary tract cancer. FGFR2 fusion positivity status must be confirmed prior to initiation of therapy. Pemazyre 13.5 mg is taken orally once per day for 14 days, followed by 7 days off therapy. For dose adjustments due to adverse reactions, see www.swissmedicinfo.ch.For patients with severe hepatic or renal impairment, the dose should be reduced to the next lower strength. CI: : Hypersensitivity to the active substance or to any of the excipients. Concomitant use with St John’s wort. W/P: Pemazyre is associated with hyper- and hypophosphatemia, serous retinal detachment, dry eye and blood creatinine increase. Pemazyre can cause fetal harm. Women of childbearing potential should be advised not to become pregnant and men not to father a child during treatment. IA: Concomitant administration with proton pump inhibitors, strong CYP3A4 inhibitors or inducers should be avoided. Administration should be separated by at least 6 hours before or after administration of P-gp substrates with a narrow therapeutic index. Close clinical surveillance is recommended when co-administered with CYP2B6 substrates. UE: The most common adverse reactions (≥ 30%) were hyperphosphatemia, alopecia, diarrhea, nail toxicity, fatigue, nausea, dysgeusia, stomatitis, constipation and dry mouth. The most common serious adverse reactions were hyponatremia and increased blood creatinine. For further information on UE, see www.swissmedicinfo.ch. Dispensing cat.: A. Revision date: June 2021. Marketing authorisation holder: Incyte Biosciences International Sàrl, CH-1110 Morges. Refer to www.swissmedicinfo.ch for detailed information.
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