Penetration of enfuvirtide, tenofovir, efavirenz, and protease inhibitors in the genital tract of HIV-1-infected men.
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.
Ghosn
Jade
J
Laboratoire de Virologie, EA MRT 3620 Université René Descartes, France.
Chaix
Marie-Laure
ML
Peytavin
Gilles
G
Rey
Elisabeth
E
Bresson
Jean-Louis
JL
Goujard
Cécile
C
Katlama
Christine
C
Viard
Jean-Paul
JP
Tréluyer
Jean-Marc
JM
Rouzioux
Christine
C
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
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