Bayer's First-in-Class AhR Inhibitor BAY 2416964 Granted IND Approval in China for Advanced Solid Tumors

On December 17, according to the public announcement by the Center for Drug Evaluation (CDE) of China’s National Medical Products Administration, Bayer’s BAY 2416964 tablets, submitted as a Class 1 chemical drug, received implicit approval for two clinical trials and are intended for development in the treatment of advanced malignant solid tumors. Publicly available information indicates that BAY 2416964 is a highly selective aryl hydrocarbon receptor (AhR) inhibitor currently in the early stages of global development.

Screenshot source: CDE official website

Aryl hydrocarbon receptor (AhR) is a protein found in immune cells that modulates immune responses based on integrated signals such as gut microbiota and amino acid metabolism. Due to its high expression in various tumors and its immunomodulatory properties, AhR-targeting modulators are considered a novel class of immunotherapies. Furthermore, these therapies hold promise for combination with other drug classes to enhance therapeutic efficacy.

Public information indicates that BAY 2416964 is a potent, selective, and cross-reactive AhR inhibitor capable of exerting diverse antitumor immunomodulatory effects. It blocks CYP1A1 transcription mediated by various AhR agonistic ligands, directly interacts with AhR, and inhibits ligand-induced translocation of AhR to the nucleus. Studies have demonstrated that BAY 2416964 exerts inhibitory effects in specific tumor models across different doses and dosing frequencies.

According to the ClinicalTrials.gov website, Bayer is currently conducting a human dose-finding study of BAY 2416964 in patients with advanced cancer. This is an open-label, Phase I, first-in-human dose-escalation and expansion study designed to evaluate the safety, tolerability, maximum tolerated dose, pharmacokinetics, pharmacodynamics, and tumor response profile of the AhR inhibitor BAY 2416964. The study was initiated in August 2019 and is scheduled for completion in 2023.

Image source: ClinicalTrials.gov website

In China, Bayer submitted the clinical trial application for BAY 2416964 tablets this October, which was accepted by the Center for Drug Evaluation (CDE). This marks the first approval for clinical trials of this product in China, indicating that this candidate drug is poised to commence clinical studies in patients with advanced malignant tumors in the country.

We hope that the subsequent clinical development of this product will proceed smoothly, bringing a new treatment option to cancer patients as soon as possible.

References:

[1] Center for Drug Evaluation, National Medical Products Administration of China. Retrieved Dec 17, 2020, from http://www.cde.org.cn/news.do?method=changePage&pageName=service&frameStr=20#

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