MRTX9768 hydrochloride is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor. It inhibits SDMA and cell proliferation in HCT116 MTAP-del cells, showing marked selectivity over HCT116 MTAP-WT cells. This compound leads to sustained SDMA inhibition and demonstrates dose-dependent inhibition in MTAP-del tumors in vivo. It selectively targets MTAP/CDKN2A-deleted tumors, such as glioblastoma, and exhibits a favorable ADME profile.
- Potent and selective PRMT5-MTA complex inhibitor
- Orally active
- Targets MTAP/CDKN2A-deleted tumors
- Exhibits favorable ADME profile
- Leads to sustained SDMA inhibition
- Inhibits cell proliferation in HCT116 MTAP-del cells