High concentration of raltegravir in semen of HIV-infected men: results from a substudy of the EASIER-ANRS 138 trial.
Raltegravir concentrations and human immunodeficiency virus type 1 (HIV-1) RNA levels in semen samples from 10 treatment-experienced HIV-1-infected patients were measured after 24 weeks of raltegravir-based highly active antiretroviral therapy (HAART). Semen and plasma HIV-1 RNA levels were below 100 copies/ml and 50 copies/ml, respectively, in all samples. The median raltegravir concentrations in semen samples (n=10) and in plasma samples (n=9) drawn simultaneously were 345 (range, 83 to 707) ng/ml and 206 (range, 106 to 986) ng/ml, respectively. The median semen-to-plasma ratio of raltegravir concentration was 1.42 (range, 0.52 to 6.66), indicating good although variable levels of drug penetration of raltegravir in the seminal compartment.
Barau
Caroline
C
Department of Clinical Pharmacy, Bicêtre Hospital, Assistance Publique Hôpitaux de Paris, 78 Rue du Général Leclerc, 94275 Le Kremlin Bicêtre, France.
Delaugerre
Constance
C
Braun
Joséphine
J
de Castro
Nathalie
N
Furlan
Valérie
V
Charreau
Isabelle
I
Gérard
Laurence
L
Lascoux-Combe
Caroline
C
Molina
Jean-Michel
JM
Taburet
Anne-Marie
AM
D000328:Adult; D019380:Anti-HIV Agents / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D023241:Antiretroviral Therapy, Highly Active / Q000379:methods; D015658:HIV Infections / Q000188:drug therapy* / Q000378:metabolism; D006801:Humans; D008297:Male; D008875:Middle Aged; D011760:Pyrrolidinones / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D000068898:Raltegravir Potassium; D012661:Semen / Q000378:metabolism*
D019380:Anti-HIV Agents; D011760:Pyrrolidinones; D000068898:Raltegravir Potassium