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vopimetostat
- Development stage
- Phase 2
- Lead developer
- Tango Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Vopimetostat (TNG462) is an oral, once-daily, small molecule MTA-cooperative PRMT5 inhibitor developed by Tango Therapeutics. It is designed to selectively target cancer cells harboring a methylthioadenosine phosphorylase (MTAP) deletion, which occurs in approximately 10-15% of human cancers, including 35% of pancreatic cancers and 15% of lung cancers. By binding to the PRMT5-MTA complex that accumulates in MTAP-deleted cells, vopimetostat inhibits the methyltransferase activity of PRMT5, leading to synthetic lethality. It is currently being evaluated in Phase 1/2 clinical trials as a monotherapy and in combination with RAS(ON) inhibitors and standard chemotherapies for patients with MTAP-deleted solid tumors, specifically pancreatic ductal adenocarcinoma and non-small cell lung cancer.
- Other names
- vopimetostat
02
Targets
PRMT5 (Protein arginine N-methyltransferase 5)
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