title: Rezolsta® (Darunavir/Cobicistat): First Boosted Protease Inhibitor Co-formulated with Cobicistat.
abstract: Rezolsta® (darunavir/cobicistat) is the first boosted protease inhibitor in a fixed-dose combination to be approved for the treatment of HIV infection. It contains darunavir, a protease inhibitor with a well-known safety and efficacy profile, and the new pharmacokinetic enhancer cobicistat. The convenience of this combination makes boosted darunavir easier to take, thus improving adherence. Exposure to darunavir is equivalent when it is administered with cobicistat or with ritonavir. Darunavir/cobicistat-based antiretroviral therapy has shown considerable efficacy and good tolerability in several clinical trials. Data from the single-arm, open-label, phase III GS-US-216-130 trial showed virological efficacy rates comparable to those from ARTEMIS and ODIN. Darunavir/cobicistat was well tolerated; most adverse events were mild and consisted of gastrointestinal disturbances. Cobicistat inhibits transporters of creatinine in kidney tubules, thus causing a minimal and reversible reduction in estimated glomerular filtration rate. Like ritonavir, cobicistat is a strong CYP3A4 inhibitor and, as such, shares most of its drug interactions. However, inhibition by cobicistat seems to be more specific than with ritonavir, and cobicistat has no inducer effect; therefore, differences in its drug interaction profile may be observed.
authors.affiliation: Infectious Diseases Department, Hospital Universitari Vall d'Hebron, Barcelona, Spain.|Universitat Autònoma de Barcelona, Barcelona, Spain.
authors.forename: Adrián
authors.initials: A
authors.lastname: Curran
authors.affiliation: HIV Unit, IdiPAZ Hospital Universitario La Paz, Madrid, Spain.
authors.forename: Ignacio
authors.initials: I
authors.lastname: Pérez-Valero
authors.affiliation: Fundación Lluita contra la SIDA, Hospital Universitari Germans Trias i Pujol, Badalona, Spain.|Universitat Autònoma de Barcelona, Barcelona, Spain.
authors.forename: José
authors.initials: J
authors.lastname: Moltó
mesh_terms: D002986:Clinical Trials as Topic; D000069547:Cobicistat / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000069454:Darunavir / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D004338:Drug Combinations; D064420:Drug-Related Side Effects and Adverse Reactions; D015658:HIV Infections / Q000188:drug therapy; D017320:HIV Protease Inhibitors / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D006801:Humans; D055118:Medication Adherence; D016896:Treatment Outcome
chemical_list: D004338:Drug Combinations; D017320:HIV Protease Inhibitors; D000069547:Cobicistat; D000069454:Darunavir