molecules of the month

lirafugratinib (RLY-4008)

oral covalent FGFR2 inhibitor

Ph. II for cholangiocarcinoma

from rational design with MD simulations

Cancer Discov., June 4, 2023

Relay Therapeutics Inc., Cambridge MA

lirafubratinib, FGFR2, oral covalent FGFR2 inhibitor, Ph. II for cholangiocarcinoma, from rational design with MD simulations, Cancer Discov., June 4, 2023, RELAY THERAPEUTICS INC., CAMBRIDGE, MA
8 mins read

The First Isoform-Selective FGFR2 Inhibitor The FGFR family of receptors are well-validated targets in cancer, and several pan-FGFR inhibitors that have strong activity against FGFR1-4 have reached approval including pemigatinib, infigratinib, futibatinib, and erdafitinib. While specific FGFRs like FGFR2 can drive cancers like cholangiocarcinoma, broad inhibition of FGFRs leads to significant off-target toxicities, such as hyperphosphatemia from FGFR1 inhibition or diarrhea from FGFR4 inhibition. Due to the 88-96% sequence similarity of the FGFR2 and FGFR1/3/4 kinase domains, however, an FGFR2-specific inhibitor has until recently been elusive. Relay Therapeutics captured industry attention when they announced their discovery of an FGFR2 isoform-selective inhibitor using an approach involving molecular dynamics simulations (“Dynamo” platform), leading many to wonder how they were able to accomplish…

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