title: Penetration of enfuvirtide, tenofovir, efavirenz, and protease inhibitors in the genital tract of HIV-1-infected men.
abstract: One likely mechanism of virological failure is poor antiretroviral drug diffusion in sites of viral replication such as the genital tract. We measured antiretroviral drug concentrations in blood and semen in 13 HIV-infected men failing treatment. Enfuvirtide did not cross the blood-testis barrier, whereas tenofovir accumulated in semen. Unlike indinavir, semen concentrations of lopinavir, amprenavir, saquinavir and efavirenz were ineffective. These are worrying findings, because suboptimal semen drug concentrations may enhance the risk of sexually transmitted drug-resistant HIV variants.
authors.affiliation: Laboratoire de Virologie, EA MRT 3620 Université René Descartes, France.
authors.forename: Jade
authors.initials: J
authors.lastname: Ghosn
authors.forename: Marie-Laure
authors.initials: ML
authors.lastname: Chaix
authors.forename: Gilles
authors.initials: G
authors.lastname: Peytavin
authors.forename: Elisabeth
authors.initials: E
authors.lastname: Rey
authors.forename: Jean-Louis
authors.initials: JL
authors.lastname: Bresson
authors.forename: Cécile
authors.initials: C
authors.lastname: Goujard
authors.forename: Christine
authors.initials: C
authors.lastname: Katlama
authors.forename: Jean-Paul
authors.initials: JP
authors.lastname: Viard
authors.forename: Jean-Marc
authors.initials: JM
authors.lastname: Tréluyer
authors.forename: Christine
authors.initials: C
authors.lastname: Rouzioux
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D000328:Adult; D000480:Alkynes; D019380:Anti-HIV Agents / Q000493:pharmacokinetics*; D048588:Benzoxazines; D001814:Blood-Testis Barrier; D003521:Cyclopropanes; D000077560:Enfuvirtide; D005837:Genitalia, Male / Q000378:metabolism*; D015700:HIV Envelope Protein gp41; D023581:HIV Fusion Inhibitors / Q000493:pharmacokinetics; D015658:HIV Infections / Q000188:drug therapy*; D017320:HIV Protease Inhibitors / Q000493:pharmacokinetics*; D015497:HIV-1; D006801:Humans; D008297:Male; D008875:Middle Aged; D063065:Organophosphonates / Q000493:pharmacokinetics; D010078:Oxazines / Q000493:pharmacokinetics; D010446:Peptide Fragments / Q000493:pharmacokinetics; D000068698:Tenofovir
chemical_list: D000480:Alkynes; D019380:Anti-HIV Agents; D048588:Benzoxazines; D003521:Cyclopropanes; D015700:HIV Envelope Protein gp41; D023581:HIV Fusion Inhibitors; D017320:HIV Protease Inhibitors; D063065:Organophosphonates; D010078:Oxazines; D010446:Peptide Fragments; D000077560:Enfuvirtide; D000068698:Tenofovir; D000225:Adenine; C098320:efavirenz