333994-00-6

TAK-220 is an orally bioavailable antagonist of chemokine (C-C motif) receptor 5 (CCR5). It binds to CCR5 (IC₅₀ = 3.5 nM for the human receptor in CHO cells), but not CCR1, CCR2b, CCR3, CCR4, or CCR7. TAK-220 inhibits the binding of chemokine (C-C motif) ligand 5 (CCL5) and CCL3 to CCR5 (IC₅₀s = 3.5 and 1.4 nM, respectively) but does not inhibit binding of CCL4. It inhibits HIV-1 envelope-mediated membrane fusion in a macrophage (M-tropic) R5, but not in a T cell (T-tropic) X4, strain of HIV-1 (IC₅₀s = 0.42 and >1,000 nM, respectively). TAK-220 inhibits the replication of six strains of R5 HIV-1 clinical isolates (EC₉₀ overall mean = 13 nM) and the R5 JR-FL laboratory-adapted strain (EC₅₀ = 0.6 nM), but not of X4 HIV-1 clinical isolates or the X4 IIIB laboratory-adapted strain (EC₅₀s = >10,000 nM for both), in human peripheral blood mononuclear cells (PBMCs).

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