SAN DIEGO, Dec. 13, 2023 /PRNewswire/ — ChemDiv Inc., dedicated to partnering in discovery and development of breakthrough therapies based on its unique chem-bio platforms, announces the presentation of non-clinical summary data for the best-in-class selective BCL2 inhibitor clinical candidate at the 65th ASH Annual Meeting and Exposition in San Diego, CA.
“A Novel Selective BCL2 Inhibitor with Limited Immune Suppression and Improved Safety Compared to Venetoclax” was presented by collaborators from University of Cincinnati (Ohio), Molsoft LLC, Expert Systems Inc of San Diego California, and Eilean Therapeutics LLC of Dover, Delaware. The presentation highlighted best-in-class potency and selectivity against BCL2, a key pro-survival protein that is overexpressed in many cancers. This clinical candidate demonstrated an equivalent in vivo anti-tumor efficacy as venetoclax in both B cell and myeloid malignancy cell lines and in vivo models. Compared to venetoclax, the candidate exhibits significantly less suppression of non-malignant immune cell populations, a result that signals superior selectivity and improved safety profile.
In collaboration with rational design groups of Molsoft and Expert Systems, John Byrd’s lab at University of Cincinnati, ChemDiv deployed a fragment-based approach to completely redesign a binding interface comparing to venetoclax and venetoclax-like molecules to achieve differentiated pharmacology according to the target product profile. The 4600-fold selectivity for BCL2 over BCL-xl; high oral bioavailability, short half-life and low interaction with CYP3A of the resulting clinical candidate translated in best-in-class safety, tolerability and developable pharmacology advantages delivered to partners at Eilean Therapeutics LLC.
About ChemDiv Inc.
ChemDiv is dedicated to partnering in discovery and development of breakthrough therapies based on its unique chem-bio platforms: molecular glues, stabilizers and degraders; covalent and non-covalent binders; bifunctional molecules for synergistic effect and synthetic lethality. Over the past 32 years ChemDiv has successfully completed hundreds of lead, candidate and new drug programs to treat cancer, neurological, infectious, cardiometabolic and immune diseases with pharma, biotech and academic partners around the globe. Learn more at www.chemdiv.com
About Expert Systems
Expert Systems is a global target to clinic accelerator. It deploys a comprehensive hybrid AI/ML based platform, covering all aspects of preclinical drug discovery and early development, from target identification and virtual screening, to non-clinical and clinical pharmacology, including chemical liability assessment and toxicology. Expert Systems uses proprietary and public databases and software tools to evaluate the intellectual property landscape and provide competitive intelligence to de-risk candidate selection for fast transition from in silico to first-time-in-man. Expert Systems sets up seed & series A companies, organizes and manages R&D programs for financial investors and strategic partners in North America, Europe and Australia. Learn more at www.expertsystems.inc
About Eilean Therapeutics
Eilean Therapeutics is a small molecule oncology company that is committed to defeating cancer and improving lives of cancer patients. Eilean develops differentiated best-in-class molecules that target fundamental biological pathways with resistant mutations and escape mechanisms in hematologic malignancies. Learn more at www.eileanther.com
Media contact:
Ronald Demuth
CEO of ChemDiv,
[email protected]
SOURCE ChemDiv
