MRTX9768 is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor. It inhibits SDMA and cell proliferation in HCT116 MTAP-del cells with marked selectivity over HCT116 MTAP-WT cells. This compound selectively targets MTAP/CDKN2A-deleted tumors, such as glioblastoma, and exhibits a favorable ADME profile.
- Potent and selective PRMT5-MTA complex inhibitor
- Inhibits SDMA and cell proliferation in MTAP-del cells
- Demonstrates dose-dependent inhibition of SDMA in MTAP-del tumors
- Selectively targets MTAP/CDKN2A-deleted tumors, including glioblastoma
- Favorable ADME profile with high bioavailability and moderate to high clearance