TAK-220 (TAK220) is a potent, specific, orally bioavailable CCR5 antagonist that blocks the binding of MIP-1α to CCR5 with IC50 of 1.4 nM.
TAK-220 shows no affinity for CCR1, CCR2b, CCR3, CCR4, or CCR7.
TAK-220 inhibits the replication of 6 CCR5-using (R5) HIV-1 clinical isolates in peripheral blood mononuclear cells (PBMCs) with mean EC90 of 13 nM.
TAK-220 selectively inhibits R5 HIV-1 replication by interfering with coreceptor-mediated entry of the virus into host cells; exhibits a good pharmacokinetic profile in monkeys.
