molecules of the month


oral pan-TEAD auto-palmitoylation inhibitor

tumor regression at 3 mg/kg QD

from 160k compound cell-based HTS

Mol. Cancer. Ther., Apr. 13, 2021

Vivace Therapeutics, San Mateo, CA

1 min read

The Vivace Therapeutics pan-TEAD transcription factor inhibitor, VT-104, binds to a lipid pocket on TEAD, preventing its auto-palmitoylation, similar to a previously highlighted TEAD inhibitor. In contrast to previously published TEAD inhibitors, VT104 has high oral bioavailability (78%) and a long half-life (24 h) in mice, and demonstrates in vivo tumor regression at a low daily dose of 3 mg/kg. Interestingly in the paper, the authors refer to anNF2 mutant tumor being “lost” due to the difficulty in growing the tumors - these things happen in real life drug discovery.

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