Drug intelligence / Profile preview

MRTX1719

Development stage
Phase 2
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

MRTX1719 is a small molecule investigational drug that acts as a potent and selective inhibitor of the PRMT5•MTA complex. It is designed to exploit synthetic lethality in cancers with homozygous deletion of the MTAP gene (MTAP-deleted cancers). By selectively binding to and inhibiting PRMT5 activity in MTAP-deficient cells, MRTX1719 disrupts protein arginine methylation processes critical for tumor cell survival. Preclinical studies have shown that daily oral administration of MRTX1719 leads to dose-dependent inhibition of PRMT5-dependent symmetric dimethylarginine protein modification and correlates with antitumor activity in MTAP-deleted tumor models. The drug is being developed primarily for advanced solid tumors harboring MTAP deletions, including non-small cell lung cancer, mesothelioma, neurilemmoma, pancreatic cancer, glioblastoma, and other solid tumors[2][3][4][6].

Other names
PRMT5-MTA inhibitorPRMT-5-MTA inhibitorPRMT 5-MTA inhibitorPRMT5•MTA complex inhibitormethylthioadenosine-cooperative PRMT5 inhibitor
02

Targets

PRMT5 (Protein arginine N-methyltransferase 5)

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