Ensem Therapeutics has partnered with BeiGene to advance ETX-197, now known as BG-68501, into clinical trials. BG-68501 is a potent inhibitor of the cyclin-dependent kinase 2 (CDK2), an enzyme involved in the uncontrolled growth of solid tumors.
This achievement is a testament to the power of Ensem’s Kinetic Ensemble® platform, which leverages artificial intelligence (AI) and machine learning to uncover previously hidden binding pockets in target proteins. BG-68501 is the first clinical-stage compound to emerge from this platform, demonstrating its potential for revolutionizing drug discovery.
Shengfang Jin, CEO of Ensem, emphasized the difficulty in targeting CDK2 in cancer treatment. However, the company’s novel approach allows for identifying “cryptic sites” that are not easily identified in traditional protein structures. By targeting these sites, BG-68501 can potentially inhibit CDK2 hyperactivity, a key driver in numerous cancer types.
BeiGene has initiated a Phase 1 clinical trial to evaluate BG-68501 in advanced solid tumors. The trial will assess the safety and efficacy of the drug in various cancer types, including breast, ovarian, and lung cancer.
Ensem’s successful completion of the preclinical development and rapid advancement of BG-68501 into clinical trials highlights the efficiency of its platform. With multiple early-stage programs underway, the company anticipates nominating two additional development candidates in 2024.
Jon Napitupulu is Director of Media Relations at The Clinical Trial Vanguard. Jon, a computer data scientist, focuses on the latest clinical trial industry news and trends.
