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PMID: 11959565 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, P.H.S.

Anti-human immunodeficiency virus interactions of SCH-C (SCH 351125), a CCR5 antagonist, with other antiretroviral agents in vitro.

Antimicrobial agents and chemotherapy ·Vol. 46 ·No. 5 ·2002-05-00 ·Pages 1336-9

Tremblay CL, Giguel F, Kollmann C, Guan Y, Chou TC, Baroudy BM, Hirsch MS

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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Article Info
Journal
Antimicrobial agents and chemotherapy
Abbr.
Antimicrob Agents Chemother
ISSN
0066-4804
Published
2002-05-00
Pages
1336-9
Language
English
Region
United States
NLM ID
0315061
PMCID
PMC127193
Subset
IM
Grants
NCI NIH HHS · CA12464 · United States
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