Human immunodeficiency virus (HIV) is an infection that attacks the body’s immune system, specifically the white blood cells called CD4 cells. HIV destroys these CD4 cells, weakening a person’s immunity against infections such as tuberculosis and some cancers.
WHO recommends that every person who may be at risk of HIV should access testing. People diagnosed with HIV should be offered and linked to antiretroviral treatment as soon as possible following diagnosis. If taken consistently, this treatment also prevents HIV transmission to others.
If the person’s CD4 cell count falls below 200, their immunity is severely compromised, leaving them more susceptible to infections. Someone with a CD4 count below 200 is described as having AIDS (acquired immunodeficiency syndrome).
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A potent, highly selective, and orally bioavailable CCR5 antagonist with Ki of 2.5 nM; display no affinity for muscarinic receptors (Ki>10 uM); inhibits HIV-1 entry into U-80 cells with IC50 of 0.8 nM, inhibits HIV-1 clinical isolates in PBMC with IC90 of 1-10 nM; exhibits excellent receptor selectivity and oral bioavailability in rats and monkeys.
A highly potent nonnucleoside inhibitor (NNRTI) of HIV-1 reverse trK7912:M7912anscriptase with IC50 of 0.4 nM for WT HIV-1 in cell-based assay; shows activity against a panel of single and double HIV-1 site-directed mutant (IC50=0.3-2 nM); orally active.
ABX464 (ABX-464, ABX 464) is a novel class of anti-HIV small molecule targeting Rev-mediated viral RNA biogenesis, shows dose dependent inhibition of HIV-1 replication in stimulated PBMCs with IC50 of 0.1-0.5 uM; ABX464 inhibits different HIV-1 clades, resistant viruses and did not select for resistance; increases the levels of spliced HIV RNA, influences REV-mediated HIV RNA biogenesis and export, and interacts with the CBC complex; inhibit viral replication in humanized mice.
Atazanavir is a highly potent HIV-1 protease inhibitor that exhibits potent anti-HIV activity EC50 of 2.6-5.3 nM and EC90 of 9-15 nM in cell culture; shows synergistic antiviral effects in HIV-infected PBMCs; used to treat and prevent HIV/AIDS.
Cobicistat is a pharmacoenhancer that acts as potent and selective inhibitor of human CYP3A with IC50 of 30-285 nM; more selective than RTV with much reduced inhibitory activity toward CYP2D6, CYP2C8, and CYP2C9.
Mavorixafor is a potent and selective antagonist of CXCR4 with IC50 of 13 nM in a CXCR4 125I-SDF inhibition binding assay; displays no significant activity (IC50>10 uM) for a series of other closely GPCRs (CCR1, CCR2b, CCR4, CCR5, CXCR1, and CXCR2); inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with IC50 of 2 nM and 26 nM, respectively, with noncytotoxic to cells (>23 uM); exhibits good PK profiles and excellent oral bioavailability; also inhibits CXCR4/SDF-1-mediated events in ALL cancer cells and transplant models.
INCB9471 (INCB 9471;INCB-9471) is a potent, selective and orally bioavailable CCR5 antagonist IC50 of 6.5 nM, Kd of 3.1 nM in human PBMCs; inhibits CCR5-mediated signaling events such as intracellular calcium mobilization, ERK phosphorylation, and CCR5 receptor internalization with IC50 values of 16, 3, and 1.5 nM, respectively; demonstrates anti-HIV-1 activity against R5 HIV-1 strains representing the major clades including A, B, C, D, E, F, G, and J with mean IC50 of 9 nM in PBMCs; also is a potent inhibitor of mutant HIV-1 variants that are resistant to other drugs including NRTIs, NNRTIs, PIs, and the fusion inhibitor T20.
Mavorixafor hydrochloride is a potent and selective antagonist of CXCR4 with IC50 of 13 nM in a CXCR4 125I-SDF inhibition binding assay; displays no significant activity (IC50>10 uM) for a series of other closely GPCRs (CCR1, CCR2b, CCR4, CCR5, CXCR1, and CXCR2); inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with IC50 of 2 nM and 26 nM, respectively, with noncytotoxic to cells (>23 uM); exhibits good PK profiles and excellent oral bioavailability; also inhibits CXCR4/SDF-1-mediated events in ALL cancer cells and transplant models.
MK-8591 (Islatravir, MK8591, EFdA) is a nucleoside analog that exhibits remarkable potency against wild-type and drug-resistant HIVs, inhibits HIV-1 reverse transcriptase with multiple mechanisms; also retains potent activity against multinucleoside-resistant HIV-2 mutants (EC50<11 nM).
NBD-11021 (NBD11021) is a small molecule, full antagonist of CD4 that blocks gp120-CD4 interaction; inhibits the CD4-dependent virus in a dose-dependent manner with IC50 of 2.4 uM; also weakly shows HIV-1 RT inhibition with IC50 of 43.4 uM; exhibits pan-neutralization activity against a panel of 56 Env-pseudotyped HIV-1 representing diverse subtypes of clinical isolates (IC50 as low as 270 nM).
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