Investigators from John Byrd’s Lab at University of Cincinnati Presented Non-Clinical Summary Data for The Best-in-Class Selective BCL2 Inhibitor Clinical Candidate Developed by Eilean Therapeutics in Collaboration with ChemDiv

On December 13, 2023 ChemDiv Inc., dedicated to partnering in discovery and development of breakthrough therapies based on its unique chem-bio platforms, reported the presentation of non-clinical summary data for the best-in-class selective BCL2 inhibitor clinical candidate at the 65th ASH (Free ASH Whitepaper) Annual Meeting and Exposition in San Diego, CA (Press release, ChemDiv, DEC 13, 2023, View Source [SID1234638543]).

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"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.