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aplaviroc

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

Overview

Aplaviroc is a small molecule CCR5 entry inhibitor developed by GlaxoSmithKline for the treatment of HIV infection. It belongs to the class of spiro-diketo-piperazine derivatives and acts as a noncompetitive allosteric antagonist of the C-C chemokine receptor type 5 (CCR5), thereby blocking HIV entry into host cells. Unlike other CCR5 antagonists, aplaviroc preserves some natural chemokine ligand binding to CCR5. Despite promising preclinical and early clinical results, development was discontinued in October 2005 due to concerns about liver toxicity and insufficient efficacy in some patients[1][2][6][8].

Targets

CCR5 (C-C chemokine receptor type 5)

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