molecules of the month


potent, oral CD73 nucleotidase inhibitor

oral activity in vivo, available in higher species

from SBDD of known ligand

J. Med. Chem., Sep. 24, 2020

ORIC Pharma, South San Francisco, CA

Structure of OP-5244, a potent and orally active inhibitor of CD73
1 min read

OP-5244 is a potent (250 pM), orally bioavailable inhibitor of the nucleotidase CD73, in contrast to the previously highlighted IV inhibitor in July. I thought it was remarkable that the ORIC team was able to identify an orally available, low clearance, and permeable compound with phosphonic acid motif and four other hydrogen bond donors (incl. 3 free hydroxyl groups). The authors label OP-5244 a tool compound, but it will be interesting to see if an oral candidate emerges against the backdrop of CD73 antibodies in development.

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