Bayer Announces First-in-Class KEAP1 Activator VVD-130037 Enters Phase I Clinical Trial

On September 18, Bayer announced that VVD-130037 (BAY 3605349), a KEAP1 activator developed by its subsidiary Vividion Therapeutics, had officially initiated Phase I clinical trials and completed the first dosing in subjects. The trial aims to evaluate the safety, pharmacokinetics, pharmacodynamics, and preliminary efficacy of VVD-130037 (oral, once daily) in patients with advanced solid tumors.

VVD-130037 is a small molecule activator targeting Kelch-like ECH-associated protein 1 (KEAP1). KEAP1 is a subunit protein of the E3 ubiquitin ligase primarily expressed in the cytoplasm, responsible for regulating the levels of the downstream nuclear factor erythroid 2-related factor 2 (NRF2). After KEAP1 binds to NRF2, it promotes its ubiquitination and degradation. Studies have shown that activation of the KEAP1-NRF2 pathway enhances tumor cell proliferation by reprogramming metabolism, suppresses various stress responses, and promotes immune escape.

Vividion Therapeutics, Inc., acquired by Bayer in August 2021, is a biopharmaceutical company aimed at developing precision therapies for devastating cancers and immune diseases by targeting high-value, undruggable targets using novel discovery technologies.

Currently, Vividion Therapeutics' pipeline includes more than ten innovative small-molecule drugs in clinical development, targeting STAT3, NRF2, JAK1, and others.

Vividion Therapeutics Pipeline Products (Source: PharmaCube NextPharma Database)

Dr. Christian Rommel, Head of Research and Development at Bayer's Pharmaceuticals Division, said: "We are leveraging Vividion Therapeutics' innovative chemoproteomics technology to develop new therapies that have the potential to halt or reverse disease progression. For millions of patients and their families, cancer remains a devastating disease that requires novel treatment approaches to address the key drivers of tumor cell survival and growth. The initiation of Vividion's first clinical trial brings us one step closer to developing potentially meaningful new anticancer therapies for various types of cancer."

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