Abstract
SCH-C (SCH 351125) is a small-molecule antagonist of the human immunodeficiency virus type 1(HIV-1) coreceptor CCR5. It has in vitro activity against R5 viruses with 50% inhibitory concentrations ranging from 1.0 to 30.9 nM. We have studied anti-HIV-1 interactions of SCH-C with other antiretroviral agents in vitro. Synergistic interactions were seen with nucleoside reverse transcriptase inhibitors (zidovudine and lamivudine), nonnucleoside reverse transcriptase inhibitors (efavirenz), and protease inhibitors (indinavir) at all inhibitory concentrations evaluated. We have also studied antiviral interactions between the HIV-1 fusion inhibitor T-20 and SCH-C against a panel of R5 HIV-1 isolates. We found synergistic interactions against all the viruses tested, some of which harbored resistance mutations to reverse transcriptase and protease inhibitors. Anti-HIV-1 synergy was also observed between SCH-C and another R5 virus inhibitor, aminooxypentane-RANTES. These findings suggest that SCH-C may be a useful anti-HIV drug in combination regimens and that a combination of chemokine coreceptor/fusion inhibitors may be useful in the treatment of multidrug-resistant viruses.
MeSH Terms
Anti-HIV Agents/pharmacology
CCR5 Receptor Antagonists
Cyclic N-Oxides/pharmacology
Drug Interactions
Drug Resistance, Viral
HIV Infections/virology
HIV-1/drug effects
Humans
Inhibitory Concentration 50
Microbial Sensitivity Tests/methods
Oximes
Piperidines
Pyridines/pharmacology
Reverse Transcriptase Inhibitors/pharmacology
Chemicals
Anti-HIV Agents
CCR5 Receptor Antagonists
Cyclic N-Oxides
Oximes
Piperidines
Pyridines
Reverse Transcriptase Inhibitors
Ancriviroc
Authors & Affiliations
7 authors, click to expand affiliations / ORCID
Tremblay Cécile L
Massachusetts General Hospital, Infectious Diseases Unit, Harvard Medical School, Boston, Massachusetts 02114, USA.
Giguel Françoise
Kollmann Christopher
Guan Yongbiao
Chou Ting-Chao
Baroudy Bahige M
Hirsch Martin S
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