Etravirine concentrations in seminal plasma in HIV‐infected patients

In: Journal of the International AIDS Society, Band 15, Heft S4, S. 1-1

Abstract

Purpose of the studyGood 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.MethodsTen 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).ResultsTen blood and twenty semen samples were collected. Median (range) CD4 count was 502 cells/mm3 (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 IC50 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 ARV




1
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.

ConclusionsTotal 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 IC50 range.