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Sep. 18, 2021

VT-104: An Oral Pan-TEAD Auto-Palmitoylation Inhibitor

VT-104

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

drughunter.com
Drug Hunter Team

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 [...]

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