Pharmacokinetics and Pharmacodynamics of Darunavir and Etravirine in HIV-1-Infected, Treatment-Experienced Patients in the Gender, Race, and Clinical Experience (GRACE) Trial.
AIDS Res Treat
; 2012: 186987, 2012.
Article
en En
| MEDLINE
| ID: mdl-22536495
Objectives. Evaluation of pharmacokinetics and pharmacodynamics of darunavir and etravirine among HIV-1-infected, treatment-experienced adults from GRACE, by sex and race. Methods. Patients received darunavir/ritonavir 600/100mg twice daily plus other antiretrovirals, which could include etravirine 200mg twice daily. Population pharmacokinetics for darunavir and etravirine were determined over 48 weeks and relationships assessed with virologic response and safety. Rich sampling for darunavir, etravirine, and ritonavir was collected in a substudy at weeks 4, 24, and 48. Results. Pharmacokinetics were estimated in 376 patients for darunavir and 190 patients for etravirine. Median darunavir AUC(12h) and C(0h) were 60,642ng·h/mL and 3624ng/mL, respectively; and for etravirine were 4183ng · h/mL and 280ng/mL, respectively. There were no differences in darunavir or etravirine AUC(12h) or C(0h) by sex or race. Age, body weight, or use of etravirine did not affect darunavir exposure. No relationships were seen between darunavir pharmacokinetics and efficacy or safety. Patients with etravirine exposure in the lowest quartile generally had lower response rates. Rich sampling showed no time-dependent relationship for darunavir, etravirine, or ritonavir exposure over 48 weeks. Conclusions. Population pharmacokinetics showed no relevant differences in darunavir or etravirine exposure by assessed covariates. Lower etravirine exposures were associated with lower response rates.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Aspecto:
Determinantes_sociais_saude
Idioma:
En
Revista:
AIDS Res Treat
Año:
2012
Tipo del documento:
Article
País de afiliación:
Estados Unidos
Pais de publicación:
Estados Unidos