Entos Presents Preclinical Data on its First Clinical Candidate

LA JOLLA, CA – Entos, Inc presents a poster today at the annual meeting of the American Association for Cancer Research (AACR) that highlights the preclinical data for the company’s first clinical candidate, ENT-H1, generated using its proprietary AI-driven drug discovery platform.

ENT-H1 is a highly differentiated irreversible HER2 inhibitor that exhibits over 1000-fold selectivity against EGFR. It potently targets all known oncogenic forms of HER2, including the recalcitrant exon-20 mutations. ENT-H1 has favorable pharmacokinetic (PK) and safety profiles, enabling once-daily dosing and significant efficacy in multiple HER2-driven tumor models. In these studies, ENT-H1 has consistently outperformed benchmark tyrosine kinase inhibitors and antibody-drug conjugates, positioning it as a potential best-in-class HER2-targeting agent. Unique among known HER2 inhibitors, ENT-H1 shows preferential tumor enrichment, a phenomenon that has been observed across tumor types and anatomic sites. This property is exquisitely linked to HER2 expression, resulting in target engagement with antibody-like precision. Additionally, ENT-H1 has also shown high brain penetrance in brain PK evaluations, and superior efficacy in an intracranial tumor model, outperforming both tucatinib and trastuzumab deruxtecan.

“ENT-H1 is the first clinical candidate delivered from our state-of-the-art AI-driven chemistry platform. This highly differentiated molecule was discovered just eight months into the project, highlighting a key strength of our platform in the integration of physics-informed AI with high-throughput experimentation to explore novel chemical space and rapidly achieve desired optimization outcomes. We are well-positioned to file the IND by the end of 2023 and, with the enthusiastic support of clinical investigators, to bring this promising treatment to patients in need.”
- Tom Miller, Entos co-founder and CEO

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About Entos

Entos is disrupting the therapeutics landscape with its cutting-edge generative AI drug discovery platform. Headquartered in La Jolla, CA, the Entos team unites pioneering AI experts and seasoned drug hunters with strong track records of success in delivering clinically validated breakthrough treatments. Entos stands alone in providing concrete demonstration of a fully AI-enabled platform to deliver high quality, differentiated drugs to clinic with unprecedented speed and across multiple target classes and mechanisms of action.  The Entos team is advancing an internal pipeline of clinical assets to address urgent unmet patient need in oncology.  Learn more about the Entos team, platform, and pipeline at www.entos.ai.

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