Once-daily dolutegravir–based antiretroviral therapy amongst adults with advanced HIV disease receiving 1-month of daily rifapentine and isoniazid for TB preventive therapy and fluconazole for treatment of cryptococcal meningitis: results of a pharmacokinetic study

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2026
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Abstract
Abstract Background One month of daily isoniazid and rifapentine (1HP) is an efficacious, well-tolerated, and safe TB preventive therapy regimen. 1HP implementation has been slow due to concern about drug-drug interactions with rifapentine. Methods A single arm, pharmacokinetic study including 15 adults with advanced HIV disease receiving once daily 50mg dolutegravir-based ART during 1HP therapy, alongside once daily 800mg fluconazole for treatment of cryptococcal meningitis. Participants underwent intensive pharmacokinetic sampling on days-1, 5 and 14 of 1HP therapy; sampling was conducted pre-dose and 2, 4, 8, 24-hours post-dose. Dolutegravir, rifapentine, and fluconazole plasma concentrations were measured by high-performance liquid chromatography mass spectrometry with bioequivalence assessed with standard 90% confidence intervals. Results Fifteen participants were enrolled, 60% female. Median age was 37 (IQR 27-41) years, median CD4 was 11 (IQR 10-25) cells/μL. Overall, 14 of 15 participants completed day 5 and day 14 sampling. Day 14 dolutegravir trough (C24h) geometric mean concentration was 0.61 (95%CI 0.32-1.16) mg/L, while the median (IQR) was 0.63 (0.34-0.87), with 100% of samples above the dolutegravir protein adjusted 90% inhibitory concentration (PA-IC90) of 0.064 mg/L, with a geometric mean ratio (GMR) of 0.76 (90%CI 0.4-1.46) compared to day 1. Day 14 fluconazole Cmax and AUC0-24h were reduced compared to day 1, with GMR 0.73 (90%CI 0.57-0.94) and 0.77 (90%CI 0.64-0.93) respectively. Of 14 participants alive at 12 weeks after 1HP initiation, 11 (78%) had HIV viral load (VL) <200 copies/ml. No cases of cryptococcal meningitis relapse occurred during the 18-week follow-up. Conclusion Standard once-daily 50mg dolutegravir and 800mg fluconazole dosing may be a safe and effective option for patients receiving 1HP TB preventive therapy. These findings support further evaluation in larger studies.
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Authors Jayne Ellis, Gila Hale, Allan Buzibye, Denis Omali, Sandra Naluyima, Nathan Ntenkaire, Laura Nsangi, Jane Francis Ndyetukira, Alisat Sadiq, Cynthia Ahimbisibwe, Shifah Nabbaale, Asmus Tukundane, Wilber Bakka, Jane Gakuru, Aida N. Kawuma, Fiona V Cresswell, David A J Moore, David B Meya, David R Boulware, Catriona Waitt, Joseph N Jarvis, Melanie R. Nicol
Journal Open forum infectious diseases
Year 2026
DOI
10.1093/ofid/ofag415
URL
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