BAY 3605349 / Bayer - LARVOL DELTA

A First-in-Human (FIH) Study to Evaluate the Safety and Tolerability of VVD-130037 in Participants With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=290 | Recruiting | Sponsor: Vividion Therapeutics, Inc. | Trial primary completion date: Dec 2027 ➔ Aug 2030 | Trial completion date: Dec 2027 ➔ Feb 2031

First-in-human • Trial completion date • Trial primary completion date • Oncology • Solid Tumor

Vividion Publishes Discovery of First-in-Class KEAP1 Activator, Supporting Ongoing Clinical Program in Oncology (Businesswire) - "The article...establishes NRF2 degradation via KEAP1 activation as a promising therapeutic approach for NRF2-activated cancers, including non-small cell lung cancer, esophageal squamous cell carcinoma, and head and neck squamous cell carcinoma....In preclinical models, these KEAP1 activators led to robust suppression of NRF2 signaling and showed meaningful antitumor activity across several tumor types with NRF2 pathway activation....Research provides foundational mechanistic insights underlying Vividion’s Phase I KEAP1 activator, VVD-037."

Preclinical • Esophageal Squamous Cell Carcinoma • Non Small Cell Lung Cancer • Squamous Cell Carcinoma of Head and Neck

Translational pharmacokinetic/pharmacodynamic (PK/PD) modeling for VVD-130037, a novel, first-in-class covalent small molecule Kelch-like ECH-associated protein 1 (KEAP1) activator (AACR 2025) - "A translational PK/PD model is developed for VVD-130037; supporting efficacious doses during clinical development."

PK/PD data • Oncology • KEAP1

A First-in-Human (FIH) Study to Evaluate the Safety and Tolerability of VVD-130037 in Participants With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=280 | Recruiting | Sponsor: Vividion Therapeutics, Inc. | N=80 ➔ 280

Enrollment change • Oncology • Solid Tumor

Discovery of VVD-130037: A first-in-class covalent allosteric KEAP1 activator for the treatment of NRF2-activated cancers (ACS-Fall 2024) - "We will describe the identification of these molecules and the elucidation of their mechanism of action and associated structural biology. Optimization of both the intrinsic efficacy for KEAP1 activation/NRF2 degradation and pharmacokinetic properties resulted in a lead molecule, VVD-130037, which is currently being evaluated in patients with advanced solid tumors."

Oncology • Solid Tumor • KEAP1