On March 15, 2023 Vivace Therapeutics, Inc., a small molecule discovery and development company developing first-in-class therapies targeting the Hippo pathway, reported that the first clinical data for a cancer treatment targeting the Hippo pathway will be presented at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting 2023 (Press release, Vivace Therapeutics, MAR 15, 2023, View Source [SID1234628846]). Results from the company’s Phase 1 clinical study of its first-in-class transcriptional enhanced associate domain (TEAD) autopalmitoylation inhibitor, VT3989, will be presented by Timothy A. Yap, Ph.D., of the University of Texas, M.D. Anderson Cancer Center, during an oral plenary session at the conference. The AACR (Free AACR Whitepaper) conference is being held April 14-19, 2023, in Orange, Florida.
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The Phase 1 study (View Source) is a multi-center, open label trial designed to evaluate the safety, tolerability, pharmacokinetics (PK) and biological activity of VT3989 in patients with refractory metastatic solid tumors, including refractory pleural malignant mesothelioma. The study included both a dose escalation and a dose expansion phase, the latter of which also enrolled patients with neurofibromatosis 2 (NF2) mutant tumors.
Details of the oral presentation at the AACR (Free AACR Whitepaper) conference are as follows:
Presentation #CT006:
Title: First-in-Class, First-in-Human Phase 1 Trial of VT3989, an inhibitor of Yes-Associated Protein (YAP)/Transcriptional Enhancer Activator Domain (TEAD), in Patients (pts) with Advanced Solid Tumors Enriched for Malignant Mesothelioma and Other Tumors with Neurofibromatosis 2 (NF2) Mutations
Presenting Author: Timothy A. Yap, Ph.D., University of Texas, M.D. Anderson Cancer Center
Session: CTPL02: Hope for Rare Cancers: Novel Targeted and Immunotherapy Agents
Date/Time: Sunday, April 16, 2023, 3:30 – 3:45 p.m. Eastern
Location: W Hall A2-3
Vivace’s proprietary compounds, including lead development candidate VT3989, inhibit palmitoylation of members of the TEAD protein family, including both covalent and non-covalent inhibitors. Pre-clinical research and development activities have demonstrated that VT3989 is active as a monotherapy against tumors that rely upon dysfunction of the Hippo pathway, and in combination with other anti-cancer therapies in additional tumor types.