Vivace Therapeutics is advancing VT3989, a first-in-class, once-daily, orally bioavailable small-molecule inhibitor targeting the Hippo–YAP/TEAD pathway, a key oncogenic signal transduction pathway activated in some tumors.
VT3989 inhibits TEAD auto-palmitoylation, blocking interaction with YAP and TAZ, directly disrupting YAP–TEAD oncogenic transcriptional activity.
The Hippo–YAP/TEAD pathway regulates cell growth and survival but is frequently dysregulated in some cancers due to mutations, genetic rearrangements and impaired expression of the signaling pathway proteins.
YAP/TEAD activity is strongly associated with resistance to targeted therapies and disease relapse, making it a compelling target for both monotherapy and combination strategies with other targeted agents (e.g. RAS, EGFR and PRMT5 inhibitors).
VT3989 positions Vivace at the forefront of a new class of inhibitors with significant therapeutic potential for patients with high unmet medical need.
