molecules of the month

compound 49

orally bioavailable CD73 inhibitor

single agent, dose-dependent antitumor efficacy in mice

opt. of known CD73 inhibitor

J. Med. Chem., December 18, 2022

Calithera Biosciences, South San Fransisco, CA

compound 49 chemical structure orally bioavailable CD73 inhibitor - Calithera Biosciences, South San Fransisco, CA
3 mins read

What is it? Compound 49 is an orally available CD73 inhibitor with dose-dependent PK/PD and an immune-mediated antitumor mechanism of action. The molecule is highly potent in human plasma (0.38 nM), and despite having a high free fraction (42% unbound) and possessing several highly polar or charged groups, rings, hydrogen bond acceptors and donors, is orally available with a long half-life in rodents. Given the recently approved liquidation of Calithera, development will need to continue by a different company. Why do we care? Calithera is a Bay Area company that focused on programs for immuno-oncology and targeted oncology therapy, including an arginase program (partnered with Incyte) and an oral CD-73 inhibitor program (CB-703, partnered with Antengene). While the structure of…

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