High concentration of raltegravir in semen of HIV-infected men: results from a substudy of the EASIER-ANRS 138 trial

Abstract

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.

FIG. 1.

(A) Raltegravir concentrations in plasma and semen samples obtained from 10 HIV-infected patients enrolled in the EASIER-ANRS 138 trial at week 24, 5 hours following drug intake. Semen (grey bars) and plasma (black bars) samples were drawn at 5 h postdosing. A plasma sample from patient 8 was drawn at 9 h postdosing (hatched bars). (B) Individual semen-to-plasma ratios of raltegravir concentrations. The ratio is not calculated for patient 8.