molecules of the month


oral FGFR1/2/3 kinase inhibitor

approved in oncology, 13.5 mg QD (14d+, 7d-)

from focused screen of ~20k cmpds and SBDD

Journal of Medicinal Chemistry

Incyte Corporation, Wilmington, US

Chemical structure of Pemigatinib Incyte FGFR1/2/3 kinase inhibitor
2 mins read

The Incyte FGFR1/2/3 kinase inhibitor, pemigatinib, is an oral kinase inhibitor that obtained an FDA accelerated approval in 2020 for adults with previously treated, unresectable locally advanced or metastatic cholangiocarcinoma (bile duct cancer) with FGFR2 fusion or other rearrangement as detected by an FDA-approved test. There were no FDA-approved drugs for second-line treatment of patients with unresectable or metastatic cholangiocarcinoma, and no treatments approved specifically for cholangiocarcinomas with an FGFR2 gene fusion or rearrangement. Pemigatinib was approved concurrently with a Foundation Medicine companion diagnostic assay for FGFR2 rearrangements. The molecule was approved primarily based on data from the Ph. II FIGHT-202 study (NCT02924376) of 107 patients (est. ORR of 36%), and took only 3 years from trial initiation to reach accelerated approval, serving as yet another example of the…

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