MRTX9768 / BMS - LARVOL DELTA

[VIRTUAL] Fragment based discovery of MRTX9768, a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors (AACR 2021) - "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. In summary, we have used a fragment-based approach to discover a new class of orally active PRMT5•MTA inhibitors that demonstrate selective antitumor activity in MTAP-del tumor cells while sparing MTAP-WT cells."

Late-breaking abstract • Synthetic lethality • Lung Cancer • Mesothelioma • Oncology • Solid Tumor • CDKN2A • MTAP • PRMT5

Mirati Therapeutics Presents Preclinical Data on Novel Approach to PRMT5 Inhibition that Selectively Targets the PRMT5/MTA Complex in MTAP-Deleted Cancer Models (PRNewswire) - "Mirati Therapeutics...announced initial preclinical results evaluating its investigational synthetic lethal PRMT5 inhibitor in methylthioadenosine phosphorylase (MTAP)-deleted cancer models. Mirati's internally discovered PRMT5 compound is the first to specifically target the PRMT5/methylthioadenosine (MTA) complex...The results were presented today during a late-breaking minisymposium at the 2021 American Association for Cancer Research (AACR) Virtual Annual Meeting...The Mirati PRMT5 compound is advancing toward an Investigational New Drug (IND) filing in the first half of 2022."

IND • Preclinical • Oncology

Mirati Therapeutics to Present Late-Breaking Data That Advance the Understanding of Synthetic Lethal PRMT5 Inhibitors in MTAP-Deleted Cancers at AACR 2021 (PRNewswire) - “Mirati Therapeutics, Inc…announced it will present initial preclinical data on the Company's synthetic lethal PRMT5 inhibitor during a late-breaking mini symposium at the American Association for Cancer Research (AACR) Virtual Annual Meeting taking place April 10-15, 2021…Title: Fragment based discovery of MRTX9768, a synthetic lethal-based inhibitor designed to bind the PRMT5/MTA complex and selectively target MTAP/CDKN2A-deleted tumors.”

Preclinical • Oncology