Pharmacokinetics of rilpivirine and 24-week outcomes after switching from efavirenz in virologically suppressed HIV-1-infected adolescents

• Main Authors: Watsamon Jantarabenjakul, Suvaporn Anugulruengkitt, Naruporn Kasipong, Narukjaporn Thammajaruk, Jiratchaya Sophonphan, Torsak Bunupuradah, Tim R. Cressey, Angela Colbers, David M. Burger, Wanatpreeya Phongsamart, Thanyawee Puthanakit, Chitsanu Pancharoen
• Format: Journal
• Published: 2018
• Subjects: Medicine; Pharmacology, Toxicology and Pharmaceutics
• Online Access: https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85051217524&origin=inward; http://cmuir.cmu.ac.th/jspui/handle/6653943832/59058
• Institution: Chiang Mai University

© 2018 International Medical Press. Background: Rilpivirine (RPV), a non-nucleoside reverse transcriptase inhibitor drug, could be a favourable drug for maintenance therapy in HIV-infected adolescents because it has few long-term side effects. However, data among adolescents switching from efavirenz (EFV) to RPV are limited. This study investigated the pharmacokinetics (PK), safety and efficacy of RPV in virologically suppressed HIV-1-infected adolescents after switching from EFV. Methods: Adolescents aged 12–18 years on EFV-based antiretroviral therapy (ART) were switched from EFV to RPV (25 mg, once daily). Intensive 24-h blood samplings at 0 (pre-dose), 1, 2, 4, 5, 6, 9, 12 and 24 h were performed 4 weeks after switching. PK parameters were calculated using a non-compartmental method and compared with published data from the PAINT and pooled ECHO/THRIVE substudies. HIV RNA level was measured at weeks 12 and 24. Biochemical profiles were measured at baseline and week 24. Results: From January to June 2016, 20 adolescents (12 male) were enrolled. Median (IQR) age was 16 (15–17) years and weight was 49 (42–59) kg. Mean (sd) AUC24 h, C24 hand Cmaxof RPV were 2,041 (745) ng•h/ml, 69 (29) ng/ml and 143 (65) ng/ml, respectively. Median (IQR) Tmaxwas 5 (2–9) h. Four adolescents had C24 h<40 ng/ml. All PK parameters were comparable with published data. All adolescents remained virologically suppressed at week 24. Significant decreases in fasting total cholesterol, triglyceride and low-density lipoprotein were observed (P-value <0.05). Conclusions: Virologically suppressed HIV-infected adolescents had adequate RPV exposure and remained virologically suppressed after switching from EFV. RPV can be used as long-term maintenance ART in HIV-infected adolescents.