Abstract |
Highly active antiretroviral therapy has revolutionized the care of patients with HIV infection, but treatment is often complicated by the development of antiretroviral resistance. CCR5 inhibitors are a novel class of antiretroviral agents that block the CCR5 receptor, thereby preventing HIV-1 recognition and entry into CD4+ macrophages and T-cells. Schering-Plough Corp is developing vicriviroc, a CCR5 inhibitor that has demonstrated good oral bioavailability, has a long half-life that allows once daily dosing, and is primarily metabolized by cytochrome P450 CYP3A4. In vitro and clinical data suggest that vicriviroc has excellent antiviral potency with minimal toxicity. Phase I and II clinical trials demonstrated promising efficacy results when vicriviroc is administered to patients infected with CCR5-tropic HIV-1. At the time of publication, phase III trials were ongoing or planned to investigate the efficacy and safety of vicriviroc in antiretroviral-naïve and -experienced patients infected with HIV-1.
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Authors | Olga M Klibanov |
Journal | Current opinion in investigational drugs (London, England : 2000)
(Curr Opin Investig Drugs)
Vol. 10
Issue 8
Pg. 845-59
(Aug 2009)
ISSN: 2040-3429 [Electronic] England |
PMID | 19649929
(Publication Type: Journal Article, Review)
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Chemical References |
- Anti-HIV Agents
- CCR5 Receptor Antagonists
- Piperazines
- Pyrimidines
- vicriviroc
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Topics |
- Animals
- Anti-HIV Agents
(adverse effects, pharmacology, therapeutic use)
- CCR5 Receptor Antagonists
- Clinical Trials as Topic
- Drug Resistance, Viral
- HIV Infections
(drug therapy)
- HIV-1
- Humans
- Piperazines
(adverse effects, pharmacology, therapeutic use)
- Pyrimidines
(adverse effects, pharmacology, therapeutic use)
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