
Compound Overview
KEAP1 functions as an E3 ligase responsible for stabilizing nuclear factor erythroid 2–related factor 2 (NRF2), a transcription factor that modulates the expression of genes involved in antioxidant, detoxification, and cytoprotective roles.1 Gain-of-function mutations in NRF2 or loss-of-function mutations in KEAP1 can promote malignant tumor growth and resistance to many standard-of-care therapies.2
KEAP1-NRF2 inhibitor (BAY 3605349)*† is a selective, small-molecule activator of KEAP1 that allosterically enhances the ability of this E3 ligase to degrade its natural cellular target, NRF2.1,3 KEAP1-NRF2 inhibitor (BAY 3605349) is currently being evaluated in a phase I clinical trial enrolling patients with advanced solid tumors.4
*Previously known as VVD-130037.
†Managed by Vividion Therapeutics.
Clinical Trial
Tumor Type(s) | Phase | Status | Description | NCT Number |
|---|---|---|---|---|
Lung Cancer, Solid Tumors, Head and Neck Cancer | I | Now Enrolling | A Phase 1, Open-label, Multicenter, First-in-Human Study to Evaluate the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Preliminary Anti-tumor Activity of VVD-130037, a Kelch-like ECH Associated Protein 1 (KEAP1) Activator, in Participants With Advanced Solid Tumors |
Bayer’s Oncology Pipeline Brochure
Explore a comprehensive overview of Bayer's oncology pipeline, including investigational compounds, clinical trials, and areas of research.
The ongoing clinical trials listed on this website represent a comprehensive overview of Bayer's clinical pipeline in Oncology, including Bayer-sponsored research and collaborative research with academic centers, cooperative groups, and other global institutions.
