Population Pharmacokinetics of Dolutegravir in African Children: Results From the CHAPAS-4 Trial

Author:

Waalewijn Hylke12,Wasmann Roeland E1ORCID,Bamford Alasdair34,Gibb Diana M3,McIlleron Helen M15ORCID,Colbers Angela2ORCID,Burger David M2,Denti Paolo1ORCID, ,Gibb Di,Walker Sarah,Turkova Anna,Shakeshaft Clare,Spyer Moira,Thomason Margaret,Griffiths Anna,Monkiewicz Lara,Massingham Sue,Szubert Alex,Bamford Alasdair,Doerholt Katja,Bigault Amanda,Dudakia Nimisha,South Annabelle,Van Looy Nadine,Au Carly,Sweeney Hannah,Kityo Cissy M,Musiime Victor,Natukunda Eva,Nambi Esether,Rutebarika Antonia Diana,Nazzinda Rashida,Namyalo Imelda,Nangiya Joan,Nabeeta Lilian,Nakalyango Aidah,Kobusingye Lilian,Otike Caroline,Namala Winnie,Ampaire Phionah,Edgar Ayesiga,Nasaazi Claire,Ndigendawani Milly,Ociti Paul,Kyobutungi Priscilla,Mbabazi Ritah,Mwesigwa Rubondo Phyllis,Ankunda Juliet,Naabalamba Mariam,Nannungi Mary,Musiime Alex,Mbasani Faith,Enoch Louis Babu,Namusanje Josephine,Odoch Denis,Bagirigomwa Edward,Rubanga Eddie,Mulima Disan,Oronon Paul,David Williams Eram,Baliruno David,Kobusingye Josephine,Uyungrwoth Agnes,Mukanza Barbara,Okello Jimmy,Ninsiima Emily,Ezra Lutaro,Nambi Christine,Mangadalen Nansaigi,Sharif Musumba,Serunjogi Nobert B,Thomas Otim,Lugemwa Abbas,Makumbi Shafic,Musumba Sharif,Mawejje Edward,Yawe Ibrahim,Jovia Kyomuhendo Linda,Kasozi Mariam,Ankunda Rogers,kariisa Samson,Inyakuwa Christine,Ninsiima Emily,Atwine Lorna,Tumusiime Beatrice,Ahuura John,Tukwasibwe Deogracious,Nagasha Violet,Kukundakwe Judith,Zahara Nakisekka Mariam,Winnie Nambejja Ritah,Tukamushaba Mercy,Baker Rubinga,Keminyeto Edridah,Ainebyoona Barbara,Myalo Sula,Acen Juliet,Jinta Wangwe Nicholas,Natuhurira Ian,Kananura Natukunatsa Gershom,Mulenga Veronica,Chabala Chishala,Chipili Lungu Joyce,Kapasa Monica,Zyambo Khonzya,Zimba Kevin,Zangata Dorothy,shingalili Ellen,Mumba Naomi,kaonga Nayunda,Kabesha Mukumbi,Mwenechanya Oliver,Chipoya Terrence,Manakalanga Friday,Malama Stephen,Chola Daniel,Nduna Bwendo,Mwamabazi Mwate,Banda Kabwe,Kabamba Beatrice,Inambao Muleya,Mahy Mukandila Pauline,Nachamba Mwizukanji,Himabala Stella,Ngosa Shadrick,Sondashi Davies,Banda Collins,Munyangabe Mark,Mbewe Ngoma Grace,Chimfwembe Sarah,Lukonde Malasha Mercy,Kajimalwendo Mumba,Musukwa Henry,Mumba Shadrick,Hakim James,Bwakura-Dangarembizi Mutsa,Nathoo Kusum,Kamuzungu Taneal,Chidziva Ennie,Bhiri Joyline,Choga Joshua,Angela Mujuru Hilda,Musoro Godfrey,Mumbiro Vivian,Chitsamatanga Moses,Mutata Constantine,Zimunhu Rudo,Mudzingwa Shepherd,Gondo Secrecy,Moyo Columbus,Nhema Ruth,Boyd Kathryn,Matimba Farai,Kouamou Vinie,Matarise Richard,Tangwena Zorodzai,Mudzviti Taona,Matubu Allen,Kateta Alfred,Chinembiri Victor,Mukura Dorinda,Chimanzi Joy,Murungu Dorothy,Mapfumo Wendy,Ngwaru Pia,Chivere Lynette,Dube Prosper,Mukanganiki Trust,Weza Sibusisiwe,Gwenzi Tsitsi,Mutsai Shirley,Phiri Misheck,Ndlovu Makhosonke,Gwaze Tapiwa,Chitongo Stuart,Njaravani Winisayi,Musarurwa Sandra,Langa Cleopatra,Tafeni Sue,Ishemunyoro Wilbert,Mudzimirema Nathalie,Ndebele Wedu,Nyathi Mary,Siziba Grace,Tawodzera Getrude,Makuchete Tracey,Chidarura Takudzwa,Murangandi Shingaidzo,Mafaro Lawrence,Chivima Owen,Dumani Sifiso,Mampondo Beaullar,Maphosa Constance,Mwale Debra,Dhlamini Rangarirai,Sibanda Thabani,Madubeko Nobukhosi,Nyathi Silibaziso,Matiwaza Zibusiso,Nabukenya Sylvia,Tibakabikoba Harriet,Nakalanzi Sarah,Williams Cynthia,Chandiwana Precious,Gozhora Winnie,Dube Benedictor,Mulambo Sylvia,Mwanyungwi Hope,Burger David,Colbers Angela,Waalewijn Hylke,Bevers Lisanne,Mohsenian-Naghani Shaghayegh,McIlleron Helen,Norman Jennifer,Wiesner Lubbe,Wasmann Roeland,Denti Paolo,Tsirizani Galileya Lufina,Natukunda Eva,Musiime Victor,Musoke Phillipa,Revill Paul,Walker Simon,Kekitiinwa Adeodata,Mushavi Angela,Banda Kawamya Febby,Tindyebwa Denis,Lyall Hermione,Weller Ian,Peto Tim,Musoke Philippa,Siwale Margaret,Kambarami Rose,Roth Johanna,Beattie Pauline

Affiliation:

1. Division of Clinical Pharmacology, Department of Medicine, University of Cape Town , Cape Town ,  South Africa

2. Department of Pharmacy, Research Institute for Medical Innovation, Radboud University Medical Center , Nijmegen , The Netherlands

3. Medical Research Council Clinical Trials Unit, University College London , London ,  UK

4. Infection, Immunity & Inflammation Department, UCL Great Ormond Street Hospital Institute of Child Health , London , UK

5. Wellcome Centre for Infectious Diseases Research in Africa, Institute of Infectious Disease and Molecular Medicine, University of Cape Town , Cape Town ,  South Africa

Abstract

Abstract We characterized population pharmacokinetics in 42 African children receiving once-daily 25 mg (14 to <20 kg) or 50 mg (>20 kg) dolutegravir. Coadministration with emtricitabine and tenofovir alafenamide reduced dolutegravir bioavailability by 19.6% (95% confidence interval: 8.13%–30.8%) compared with zidovudine or abacavir with lamivudine. Nevertheless, concentrations remained above efficacy targets, confirming current dosing recommendations.

Funder

European and Developing Countries Clinical Trials Partnership

Janssen Pharmaceuticals and Gilead Sciences Inc

South African National Institute of Allergy and Infectious Diseases (NIAID) of the South African National Institutes of Health

Publisher

Oxford University Press (OUP)

Reference13 articles.

1. Pharmacokinetic data of dolutegravir in second-line treatment of children with human immunodeficiency virus: results from the CHAPAS4 trial;Bevers;Clin Infect Dis,2023

2. Adult dolutegravir 50 mg tablets in children living with HIV weighing 20 to 25kg;Bollen,2019

3. Exposure to dolutegravir from two formulations in children in the ODYSSEY trial;Vogelzang,2021

4. Effect of food on the pharmacokinetics of the integrase inhibitor dolutegravir;Song;Antimicrob Agents Chemother,2012

5. Consolidated guidelines on HIV prevention, testing, treatment, service delivery and monitoring: recommendations for a public health approach,2021

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