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Association details:
| Biomarker: | MTAP deletion |
|---|---|
| Cancer: | Colorectal Cancer |
| Drug: | MRTX9768 (PRMT5 inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
LB003 - Fragment based discovery of MRTX9768, a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors
Published date:
04/09/2021
Excerpt:
MRTX9768, a potent inhibitor of SDMA and cell proliferation in HCT116 MTAP-del cells (SDMA IC50 3 nM; prolif. IC50 11 nM) with marked selectivity over HCT116 MTAP-WT cells (SDMA IC50 544 nM; prolif. IC50 861 nM)....PRMT5•MTA inhibitors that demonstrate selective antitumor activity in MTAP-del tumor cells while sparing MTAP-WT cells.
