Pemetinib/Pemetinib is the first generation of targeted drugs

Pemetinib/Pemigatinib (Pemigatinib) is the first targeted therapy approved for FGFR2-altered cholangiocarcinoma (CCA).It is mainly suitable for the treatment of adult patients with unresectable locally advanced or metastatic CCA who have previously received FGFR2 fusion or other rearrangement therapy and have been detected in trials approved by the U.S. Food and Drug Administration (FDA). On the same day as pemetinib was approved, the FDA also approved a companion diagnostic (FoundationOne CDxFoundation Medicine) to identify patients with CCA and FGFR2 fusions and rearrangements who may benefit from pemetinib treatment. FoundationOne CDx Genomic Profiling Analysis has previously been approved as an adjunctive diagnostic test for many other types of cancer.

Judging from the development process and clinical application of pemetinib, it is an innovative drug. It targets FGFR2, a gene that is commonly mutated in many cancers. Pemetinib is a potent and selective small molecule kinase inhibitor that targets FGFR1, FGFR2 and FGFR3. Constitutive FGFR signaling can lead to cancer cell proliferation. Pemetinib inhibits phosphorylation and signaling of the FGFR1, 2, and 3 pathways, thereby reducing the proliferation of cancer cells with FGFR alterations. Pemetinib shows antitumor activity in human tumor xenograft models with alterations in FGFR1, FGFR2, and FGFR3.

In addition, pemetinib/pemetinib has also shown good efficacy and safety in clinical trials. In some studies, it has significantly prolonged patient survival and progression-free survival, has been associated with lower toxicity, and improved patients' quality of life. By inhibiting the activity of FGFR2, pemetinib can prevent the proliferation and spread of cancer cells, thereby achieving the purpose of treating cancer. Although there is currently no clear data indicating which generation of targeted drug it is.