title: Vicriviroc, a CCR5 receptor antagonist for the potential treatment of HIV infection.
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.
authors: Wingate University School of Pharmacy, Wingate, NC 28174-0159, USA. o.klibanov@wingate.edu
authors: Olga M
authors: OM
authors: Klibanov
mesh_terms: D000818:Animals; D019380:Anti-HIV Agents / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D065100:CCR5 Receptor Antagonists; D002986:Clinical Trials as Topic; D024882:Drug Resistance, Viral; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1; D006801:Humans; D010879:Piperazines / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D011743:Pyrimidines / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*
chemical_list: D019380:Anti-HIV Agents; D065100:CCR5 Receptor Antagonists; D010879:Piperazines; D011743:Pyrimidines; C486781:vicriviroc