molecules of the month


PD-L1 inhibitor via induced internalization

oral activity (10 mpk QD) in humanized model

from biochemical HTRF screening

Nat. Comm., Feb. 22, 2021

Arbutus Biopharma Inc, Warminster, P

Chemical structure of molecule ARB-272572 inhibitor
1 min read

7. The Arbutus PD-L1 inhibitor ARB-272572 is a preclinical molecule that potently induces PD-L1 dimerization and internalization and demonstrates oral activity (10 mg/kg QD) in a humanized mouse model. Biologic PD-1/PD-L1 inhibitors have had incredible success as cancer immunotherapy agents, and there has been significant accompanying interest in small molecule inhibitors. Given the crowdedness of the field, however, the Arbutus team also makes the case that small molecule PD-L1 inhibitors could be useful in alternate settings such as chronic hepatitis B, and demonstrate activity in an in vitro HBV assay as well.

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