培米替尼的适应症有哪些？

Indications of pemetinib

Pemetinib, developed by the American company Incyte, is an FGFR1/2/3 inhibitor. (Specification: 4.5, 9, 13.5 mg) was approved by the US FDA for accelerated approval on April 20, 2020, for adult patients with previously treated unresectable locally advanced or metastatic cholangiocarcinoma associated with FGFR2 gene fusion or other rearrangements. Pemetinib is the first small molecule drug approved by the US FDA for the treatment of cholangiocarcinoma.

In March 2021, pemetinib was conditionally approved for marketing in Europe and launched in Japan in the same month, both for the treatment of cholangiocarcinoma. Pemetinib tablets were domestically administered by Innovent Biologics (Suzhou) Co., Ltd. in accordance with the Drug Registration Classification Class 5.1. The drug's marketing application was submitted in July 2021. In April 2022, it was approved for marketing by China's NMPA (trade name: Dabotan). It is used for the treatment of adult patients with advanced, metastatic or unresectable cholangiocarcinoma who have received at least one systemic treatment in the past and have been confirmed to have FGFR2 fusion or rearrangement. In addition, pemetinib is in phase II clinical trial research for other indications such as solid tumors, myeloproliferative diseases, endometrial cancer, hematological tumors, etc. in the United States, Europe, South Korea, Japan and other countries or regions.

Pemetinib mechanism of action

Pemetinib can inhibit the binding of FGFR1/2/3 to ligands, that is, inhibit the FGFR signaling pathway, thereby inhibiting the proliferation of tumor cells overexpressing FGFR1/2/3. Pemetinib inhibits the abnormal activation of the FGFR2 signaling pathway by inhibiting the binding of FGFR2 receptors to FGFR ligands, thereby inhibiting the occurrence, development and progression of cholangiocarcinoma.

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