Journal article

Effects of enzyme inducers efavirenz and tipranavir/ritonavir on the pharmacokinetics of the HIV integrase inhibitor dolutegravir

Ivy Song, Julie Borland, Shuguang Chen, Phyllis Guta, Yu Lou, David Wilfret, Toshihiro Wajima, Paul Savina, Amanda Peppercorn, Stephen Castellino, David Wagner, Louise Hosking, Michael Mosteller, Justin P Rubio, Stephen C Piscitelli



PURPOSE: Dolutegravir (DTG) is an unboosted, integrase inhibitor for the treatment of HIV infection. Two studies evaluated the effects of efavirenz (EFV) and tipranavir/ritonavir (TPV/r) on DTG pharmacokinetics (PK) in healthy subjects. METHODS: The first study was an open-label crossover where 12 subjects received DTG 50 mg every 24 hours (q24h) for 5 days, followed by DTG 50 mg and EFV 600 mg q24h for 14 days. The second study was an open-label crossover where 18 subjects received DTG 50 mg q24h for 5 days followed by TPV/r 500/200 mg every 12 hours (q12h) for 7 days and then DTG 50 mg q24h and TPV/r 500/200 mg q12h for a further 5 days. Safety assessments and serial PK samples were collec..

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Funding Acknowledgements

Funding for this work was provided by ViiV Healthcare. All listed authors meet the criteria for authorship set forth by the International Committee for Medical Journal Editors. The authors attest that the funding source did not have an influence on the analysis and reporting of results. We would like to acknowledge Astrid Yeo for genetics support and the editorial assistance of Rashida Rana and Gina Uhlenbrauck.