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ancriviroc besylate

Development stage: Discontinued
Lead developer: Merck
Modality: Small Molecules
Administration: Oral

Overview

Ancriviroc (SCH 351125) is a small-molecule antagonist of the CCR5 coreceptor with activity against HIV-1. It functions as an orally bioavailable inhibitor of HIV-1 entry by blocking the CCR5 coreceptor. The compound has potent in vitro activity against R5 HIV-1 isolates with 50% inhibitory concentrations ranging from 0.4 to 30.9 nM. It has also shown activity in a SCID-hu Thy/Liv mouse model. Ancriviroc has good oral bioavailability (50-60%) in rodents and primates, with a serum half-life of 5-6 hours. It specifically inhibits HIV-1 infection mediated by CCR5 but has no effect on infection of CXCR4-expressing cells. The drug was developed by Schering-Plough but clinical development for HIV infection was discontinued.

Other names: Ancriviroc

Targets

CCR5 (C-C chemokine receptor type 5)

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