MRTX9768

MRTX9768 is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor In Vitro MRTX9768 inhibits SDMA and cell proliferation in HCT116 MTAP-del cells (SDMA IC 50 3 nM; prolif. IC 50 11 nM) with marked selectivity over HCT116 MTAP-WT cells (SDMA IC 50 544 nM; prolif. IC 50 861 nM). MRTX9768 (0-250 nM) results in LU99 SDMA inhibition maintaining after 3-hr drug treatment followed by 4-day washout (exhibiting tight binding and prolonged PRMT5•MTA occupancy). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo In xenograft studies, oral administration of MRTX9768 demonstrates dose-dependent inhibition of SDMA in MTAP-del tumors, with less SDMA modulation observed in bone marrow . MRTX9768 selectively targets MTAP/CDKN2A-deleted tumors (such as glioblastoma). MRTX9768 (PO dose 30 mg/kg in CD-1 mouse and beagle dog, 10 mg/kg in cynomolgus monkey) has a favorable ADME profile (>50% bioavailability in mice and dogs, moderate to high clearance, No changes in RBC parameters when administered well above efficacious concentrations (1000 mg/kg)). MRTX9768 (100 mg/kg, orally, BID, 6/21 days) results in SDMA inhibition maintaining 3 days after dosing is stopped. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:PRMT5•MTA

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