title: [Maraviroc efficacy in clinical studies on the development of the molecule].
abstract: Maraviroc is the first co-receptor antagonist to be approved for use in HIV infected patient. In a phase II trial, in which the drug was administered as a single therapy, the most suitable maintenance dose was 300 mg, once or twice per day. The MOTIVATE double blind, placebo-compared studies, were carried out on patients infected by HIV-1 with R5 tropism and resistant to drugs from three families of retrovirals. Maraviroc two times per day achieved < 50 copies/mL in 45.5% of the patients compared to 16.7% in the placebo group (p < 0.001). The CD4+ lymphocyte count had a mean of 63 cells/mm(3) higher with Maraviroc. The drug was shown to be superior in all patient groups regardless of the baseline viral load, the baseline CD4+ lymphocyte count or the number of accompanying active drugs. In the study on patients infected by HIV with X4/dual/mixed tropism, Maraviroc, was not virologically effective, but did produce a CD4 increase higher than the placebo. Maraviroc was compared with Efavirenz in the study on patients with no previous treatment and with R5-tropic virus. At 48 weeks, the percentage of patients with a viral load of <50 copies/mL was 69.3% in the group that received Efavirenz and 65.3% in the Maraviroc group. In conclusion, Maraviroc has demonstrated its increased efficacy in patients with CCR5-tropic virus and a long history of antiretroviral use and failure, and in patients with no previous treatment.
authors.affiliation: Servicio de Enfermedades Infecciosas, Hospital Ramón y Cajal, Madrid, España. smoreno.hrc@salud.madrid.org
authors.forename: Santiago
authors.initials: S
authors.lastname: Moreno
authors.forename: Beatriz
authors.initials: B
authors.lastname: Hernández
authors.forename: Carolina
authors.initials: C
authors.lastname: Gutiérrez
authors.forename: Enrique
authors.initials: E
authors.lastname: Delsol
mesh_terms: D000480:Alkynes; D019380:Anti-HIV Agents / Q000494:pharmacology / Q000627:therapeutic use; D048588:Benzoxazines / Q000627:therapeutic use; D065100:CCR5 Receptor Antagonists; D018791:CD4 Lymphocyte Count; D017322:Clinical Trials, Phase II as Topic / Q000706:statistics & numerical data; D017326:Clinical Trials, Phase III as Topic / Q000706:statistics & numerical data; D017327:Clinical Trials, Phase IV as Topic / Q000706:statistics & numerical data; D003510:Cyclohexanes / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D003521:Cyclopropanes; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D004334:Drug Administration Schedule; D015195:Drug Design; D024921:Drug Resistance, Multiple, Viral; D006678:HIV / Q000502:physiology; D023581:HIV Fusion Inhibitors / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D015658:HIV Infections / Q000188:drug therapy*; D006801:Humans; D000077592:Maraviroc; D015337:Multicenter Studies as Topic; D016879:Salvage Therapy; D016896:Treatment Outcome; D014230:Triazoles / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D054299:env Gene Products, Human Immunodeficiency Virus / Q000737:chemistry / Q000502:physiology
chemical_list: D000480:Alkynes; D019380:Anti-HIV Agents; D048588:Benzoxazines; D065100:CCR5 Receptor Antagonists; D003510:Cyclohexanes; D003521:Cyclopropanes; D023581:HIV Fusion Inhibitors; D014230:Triazoles; D054299:env Gene Products, Human Immunodeficiency Virus; C098320:efavirenz; D000077592:Maraviroc