Open AccessEtravirine concentrations in seminal plasma in HIV‐infected patients
Author(s) -
Tiraboschi J,
Niubo J,
Ferrer E,
BarreraCastillo G,
Rozas N,
MasoSerra M,
Podzamczer D
Publication year - 2012
Publication title -
journal of the international aids society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.724
H-Index - 62
ISSN - 1758-2652
DOI - 10.7448/ias.15.6.18341
Subject(s) - etravirine , medicine , viral load , regimen , virology , human immunodeficiency virus (hiv) , pharmacology , antiretroviral therapy
Purpose of the study Good penetration of antiretroviral drugs to the seminal plasma may be associated with a decrease in viral replication and play an important role in the prevention of sexual transmission of HIV. We present data from a series of HIV‐infected ARV‐experienced patients receiving etravirine‐containing regimens, in whom etravirine concentrations and viral loads were determined in blood plasma and seminal plasma. The objective was to determine etravirine concentrations and HIV‐1 viral load (VL) in blood plasma (BP) and seminal plasma (SP) of HIV‐infected patients. Methods Ten HIV‐1 adult antiretroviral‐experienced patients receiving an etravirine‐containing regimen for at least 1 month were enrolled. Semen and blood samples were both collected around 12–24 h after the last etravirine dose, depending on once‐daily or twice‐daily dosing, respectively. HPLC/MS/MS was used to determine etravirine concentrations, and HIV‐1 VL was determined by real‐time PCR (limit of detection, VL 40 copies/mL). Results Ten blood and twenty semen samples were collected. Median (range) CD4 count was 502 cells/mm 3 (252–817) and median (range) BP VL was<40 copies/mL (40–362). Median (range) time on etravirine was 52 weeks (12–124). Median (range) BP etravirine concentration was 452.5 ng/mL (258–751). Median (range) SP etravirine concentration was 62.9 ng/mL (31.2–166), and values were above the protein‐free IC 50 range (0.39–2.4 ng/mL) in all cases. Median (range) etravirine SP:BP ratio was 0.16 (0.07–0.26). SP VL was<40 copies/mL in all patients, whereas BP VL was detectable in one patient with poor adherence to treatment.Patient SP (ng/ml) BP (ng/ml) SP VL (copies/ml) BP VL (copies/ml) SP:BP Concomitant ARV1 31.2 375 <40 <40 0.08 DRVr/TDF 2* 57.1 307 <40 <40 0.18 3TC/ABC 3* 36.9 506 <40 <40 0.07 TDF/FTC 4* 60.6 399 <40 <40 0.15 3TC/ABC 5 68.1 258 <40 <40 0.26 LPVr/TDF 6* 104 414 <40 <40 0.25 3TC/ABC 7 107 491 <40 362 0.21 DRVr/TDF/FTC 8* 65.3 592 <40 <40 0.11 TDF/FTC 9 52.2 518 <40 <40 0.1 DRVr 10 166 751 <40 <40 0.22 TDF/FTC Median 62.9 452.5 <40 <40 0.16* Patients taking ETR once a day.Conclusions Total etravirine concentrations in male genital secretion are modest, reaching only 16% of the BP concentration, but nevertheless, more than 10 times above the wild type IC 50 range.