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TAK-220 is an investigational, orally bioavailable small-molecule antagonist of the C-C chemokine receptor type 5 (CCR5), developed by Takeda. It functions as an HIV-1 entry inhibitor by selectively blocking the CCR5 co-receptor, which prevents R5-tropic HIV-1 strains from binding to and entering host cells. Chemically a piperidine-4-carboxamide derivative, TAK-220 has shown potent nanomolar inhibitory activity against HIV-1 replication in peripheral blood mononuclear cells and synergistic potential with other antiretroviral drugs. While it progressed to Phase 1 clinical trials for the treatment of HIV-1 infection, its development appears to have been discontinued as it is no longer active in the company's pipeline.
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