title: Switch from enfuvirtide to raltegravir lowers plasma concentrations of darunavir and tipranavir: a pharmacokinetic substudy of the EASIER-ANRS 138 trial.
abstract: We compared tipranavir and darunavir concentrations measured at steady state in 20 human immunodeficiency virus (HIV)-infected patients enrolled in the EASIER-ANRS 138 clinical trial who switched from enfuvirtide to raltegravir while maintaining the same background regimen. The geometric mean ratios of the observed predose concentration (C(trough)), maximum concentration of drug observed in plasma (C(max)), and area under the plasma concentration-time curve (AUC) before (day 0) and after (week 24) the switch were 0.49, 0.76, and 0.67 and 0.82, 0.68, and 0.64 for tipranavir and darunavir, respectively. The virologic consequences of these drug interactions have yet to be determined.
authors.affiliation: Department of Clinical Pharmacy, Bicêtre Hospital, Assistance Publique Hôpitaux de Paris, and University Paris 11, Le Kremlin-Bicêtre, France.
authors.forename: Lauriane
authors.initials: L
authors.lastname: Goldwirt
authors.forename: Joséphine
authors.initials: J
authors.lastname: Braun
authors.forename: Nathalie
authors.initials: N
authors.lastname: de Castro
authors.forename: Isabelle
authors.initials: I
authors.lastname: Charreau
authors.forename: Aurélie
authors.initials: A
authors.lastname: Barrail-Tran
authors.forename: Constance
authors.initials: C
authors.lastname: Delaugerre
authors.forename: François
authors.initials: F
authors.lastname: Raffi
authors.forename: Caroline
authors.initials: C
authors.lastname: Lascoux-Combe
authors.forename: Jean-Pierre
authors.initials: JP
authors.lastname: Aboulker
authors.forename: Anne-Marie
authors.initials: AM
authors.lastname: Taburet
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Molina
mesh_terms: D019380:Anti-HIV Agents / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D000069454:Darunavir; D000077560:Enfuvirtide; D005260:Female; D015700:HIV Envelope Protein gp41 / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D015658:HIV Infections / Q000097:blood / Q000188:drug therapy*; D006801:Humans; D008297:Male; D008875:Middle Aged; D010446:Peptide Fragments / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D011725:Pyridines / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D011753:Pyrones / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D019438:Ritonavir / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D013449:Sulfonamides / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use
chemical_list: D019380:Anti-HIV Agents; D015700:HIV Envelope Protein gp41; D010446:Peptide Fragments; D011725:Pyridines; D011753:Pyrones; D013449:Sulfonamides; D000077560:Enfuvirtide; D019438:Ritonavir; D000069454:Darunavir; C107201:tipranavir