What is the mechanism of action of pemetinib? How does it work?

Pemigatinib is a kinase inhibitor used to treat fibroblast growth factor receptor 2 (fgfr 2) Adult patients with previously treated unresectable locally advanced or metastatic cholangiocarcinoma with fusion or other rearrangement. This indication received accelerated approval based on overall response rate and duration of response. Continued approval for this indication may be contingent upon verification and characterization of clinical benefit in confirmatory trials. Pemetinibis indicated for the treatment of adults with FGFR1rearranged relapsed or refractory myeloid /lymphoid neoplasms (MLNs).

Pemetinib is a small molecule kinase inhibitor targeting FGFR1, 2 and 3 with IC50 values less than 2 nM. Pemetinibinhibits FGFR4 in vitro at concentrations that are approximately 100 times higher than those that inhibit FGFR1, 2, and 3. Pemetinib inhibits FGFR1-3phosphorylation and signaling and reduces cell viability of cancer cell lines through activation of FGFRamplification and fusion, resulting in constitutive activation of FGFR signaling. Constitutive FGFR signaling supports the proliferation and survival of malignant cells. Pemetinib showed antitumor activity in mouse xenograft models of human tumors in which alterations in FGFR1, FGFR2 or FGFR3 resulted in constitutive FGFR activation, including expression of oncogenic FGF Xenograft model of cholangiocarcinoma patients with R2-Transformer-2βhomolog (TRA2b) fusion protein and carrying FGFR1Translocation (FGFR1OP2-FGFR1)KG1 leukemia model. There are generic drugs in Laos, and they are all officially marketed generic drugs with government approval. The retail price of Lucius Pharmaceuticals in Laos is around 1000 yuan for 4.5mg*14 tablets. If you want to get more high-quality information, you can contact Yaode, and Yaode will do its best to help you learn more about high-quality overseas drugs.

xa0

xa0