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Vivace Therapeutics Presents New Preclinical Data Highlighting Strong Synergistic Activity for Combination of VT3989 and Osimertinib at American Association for Cancer Research (AACR) Annual Meeting 2022


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Vivace Therapeutics, Inc.

Apr 11, 2022, 07:30 ET

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Combination Treatment Demonstrates Enhanced Efficacy and Delayed Tumor Growth as Compared to Osimertinib Alone in EGFR Mutant Non-Small Cell Lung Cancer Models

VT3989, a First-in-Class TEAD Autopalmitoylation Inhibitor, Currently Being Evaluated in Phase 1 Clinical Trials

SAN MATEO, Calif. , April 11, 2022 /PRNewswire/ -- Vivace Therapeutics, Inc., a small molecule discovery and development company developing first-in-class therapies targeting the Hippo pathway, today announced that new preclinical data on the company's transcriptional enhanced associate domain (TEAD) autopalmitoylation inhibitor, VT3989, were reported at the American Association for Cancer Research (AACR) Annual Meeting 2022. Presented findings demonstrated that the combination of VT3989 and osimertinib (Tagrisso®), an epidermal growth factor receptor (EGFR) inhibitor, possessed enhanced anti-tumor activity and delayed tumor growth as compared to osimertinib alone in preclinical EGFR mutant tumor models. The AACR conference is being held April 8-13, 2022, in New Orleans, Louisiana.

Data reported in the poster presentation demonstrated that VT3989 exhibits strong synergistic activity with osimertinib.  This was highlighted by the ability of the combination to enhance the blocking of tumor growth in EGFR mutant, non-small cell lung cancer (NSCLC) cell-line derived xenograft models, including the HCC827 model that is already known to be particularly sensitive to osimertinib. Furthermore, the combination of VT3989 and osimertinib significantly increased the life span of mice in an NCI-H1975 NSCLC CDX model as compared to osimertinib monotherapy.

Additionally, researchers showed similar synergistic activity in blocking tumor regrowth in human patient-derived xenograft models of EGFR mutant NSCLC. Of note, data demonstrated that TEAD inhibition achieved with VT3989 significantly delayed the re-emergence of tumor mass after osimertinib treatment resulted in non-palpable tumors. This finding offers evidence that EGFR mutant NSCLC relies upon dysfunction in the Hippo pathway to survive treatment with osimertinib,  and can thus be targeted with TEAD inhibition.

"The exciting new data presented at AACR not only support previous research highlighting the potency and selectivity of VT3989 as a TEAD inhibitor and its single agent anti-tumor activity in mesothelioma models, the findings also begin to build a compelling strategy around a synergistic combination treatment approach featuring VT3989 and EGFR inhibitors such as osimertinib," said Tracy Tang, Ph.D., vice president of biology at Vivace Therapeutics and lead author on the AACR poster presentation. "We are eager to continue our pioneering research into the Hippo pathway and how addressing dysfunction in that pathway may pave the way for first-in-class cancer therapies capable of addressing the unmet needs of patients."

Vivace's proprietary compounds inhibit palmitoylation of members of the TEAD protein family, including both covalent and non-covalent inhibitors. The company's clinical candidate, VT3989, is currently in Phase 1 clinical trials. Pre-clinical research and development activities have demonstrated that the clinical candidate 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.

The poster presented is available at the company's website www.vivacetherapeutics.com.

About Vivace Therapeutics, Inc.
Vivace Therapeutics is a small molecule drug discovery and development company focused on targeting the Hippo pathway. The company is pursuing a first-in-class approach to treat human carcinomas of high unmet medical need. Based in San Francisco Bay Area, the company has raised $70 million to date, and is funded by leading biotechnology investors, including Canaan Partners, WuXi Healthcare Ventures, Cenova Capital, Sequoia Capital China, Boxer Capital and RA Capital Mangement. For more information, please visit www.vivacetherapeutics.com.

Tagrisso® is a registered trademark of the AstraZeneca group of companies. 

Contact information

Sofie Qiao, Ph.D.
President and CEO
[email protected]
650.666.2753

Tim Brons
Vida Strategic Partners (media)
646-319-8981
[email protected]

SOURCE Vivace Therapeutics, Inc.

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