fbpx

molecules of the month

MRTX1719

PRMT5 inhibitor

preclinical (MTAP-deleted cancers)

from fragment-based design + SBDD

J. Med. Chem.

Mirati Therapeutics

PRMT5 inhibitor - Mirati Therapeutics
2 mins read

MRTX1719 is PRMT5-MTA complex inhibitor for the treatment of MTAP-deleted cancers currently in IND-enabling studies. PRMT5 is a target of active interest with several molecules recently highlighted here. Inhibition of PRMT5 is expected to induce synthetic lethality in MTAP-deleted tumors – however, PRMT5 is also an essential gene for hematopoesis, and therefore most PRMT5 inhibitors also lead to dose-limiting cytopenias. MRTX1719, in contrast, inhibits PRMT5 cooperatively with MTA (methylthioadenosine), which is accumulated in MTAP-deleted cells. This mechanism of action may allow greater differentiation between MTAP-deleted tumor cells and healthy hematopoetic stem cells. The molecule is orally active in a preclinical model with once daily dosing. The molecule emerged from a fragment-based drug discovery campaign specifically focused on the PRMT5-MTA complex,…


request a trial

You don’t have time to read everything, but you can’t afford to fall behind.

Drug Hunter Premium is drug discovery, distilled, so you can quickly catch up and make informed decisions based on industry examples.

Get ahead now by requesting a trial.


already a member? log in: