Rifampicin effect on intracellular and plasma pharmacokinetics of tenofovir alafenamide.

The Journal of Antimicrobial Chemotherapy
Maddalena CerroneMarta Boffito

Abstract

Tenofovir alafenamide produces lower plasma tenofovir and higher intracellular tenofovir diphosphate (DP) concentrations than tenofovir disoproxil fumarate but it is likely a victim of interactions with rifampicin. We aimed to investigate the pharmacokinetics of tenofovir alafenamide/emtricitabine with rifampicin. Healthy volunteers received tenofovir alafenamide/emtricitabine at 25/200 mg once daily, followed by tenofovir alafenamide/emtricitabine + rifampicin daily followed by tenofovir disoproxil fumarate. Plasma tenofovir alafenamide, tenofovir, emtricitabine and intracellular tenofovir-DP and emtricitabine triphosphate pharmacokinetics and genetic polymorphisms were assessed. Tenofovir alafenamide exposure decreased when tenofovir alafenamide/emtricitabine + rifampicin was used compared with tenofovir alafenamide/emtricitabine [geometric mean ratio (GMR) (90% CI): 0.45 (0.33-0.60)]. Plasma tenofovir and intracellular tenofovir-DP concentrations decreased with rifampicin [GMR (90% CI): 0.46 (0.40-0.52) and 0.64 (0.54-0.75), respectively]. GMR (90% CI) of intracellular tenofovir-DP AUC0-24 for tenofovir alafenamide/emtricitabine + rifampicin versus tenofovir disoproxil fumarate was 4.21 (2.98-5.95). Rifampicin did not affect...Continue Reading

References

Jul 20, 1999·The Journal of Clinical Investigation·B GreinerH K Kroemer
Jul 29, 2003·Clinical Pharmacokinetics·Mikko NiemiKari T Kivistö
Jul 11, 2006·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Tracy KingCourtney V Fletcher
Jan 8, 2009·American Journal of Epidemiology·Santiago RodriguezIan N M Day
Jun 29, 2013·Journal of Acquired Immune Deficiency Syndromes : JAIDS·Peter J RuaneKitty Yale
May 30, 2014·Journal of Acquired Immune Deficiency Syndromes : JAIDS·Paul E SaxScott McCallister
Oct 28, 2015·Antimicrobial Agents and Chemotherapy·Gabriel BirkusTomas Cihlar
May 25, 2016·Antimicrobial Agents and Chemotherapy·Joseph M CustodioSrinivasan Ramanathan
Feb 13, 2018·Journal of Pharmaceutical and Biomedical Analysis·Pamela HummertMark A Marzinke

❮ Previous
Next ❯

Citations

Jul 19, 2019·Journal of the International AIDS Society·Neesha RockwoodAnton L Pozniak
Jul 25, 2019·Expert Opinion on Drug Metabolism & Toxicology·Christine Sekaggya-Wiltshire, Kelly E Dooley
Dec 7, 2019·Expert Opinion on Drug Safety·Maddalena CerroneRobert J Wilkinson
Jan 9, 2020·Journal of the International AIDS Society·Lucia González FernándezSusan Swindells
Aug 14, 2020·The Journal of Antimicrobial Chemotherapy·Tom G JacobsUNKNOWN WHO Paediatric Antiretroviral Working Group
Sep 13, 2020·Current HIV/AIDS Reports·Elisa H Ignatius, Susan Swindells
Jun 9, 2020·Expert Opinion on Drug Metabolism & Toxicology·Piyanuch WongananKiat Ruxrungtham
Oct 12, 2019·BMC Infectious Diseases·Bernard SurialUNKNOWN Swiss HIV Cohort Study
Jul 6, 2019·The Lancet. HIV·Graeme MeintjesGary Maartens
Sep 27, 2020·International Journal of Infectious Diseases : IJID : Official Publication of the International Society for Infectious Diseases·Thomas C S MartinShannon M Balcombe
Oct 15, 2020·JAMA : the Journal of the American Medical Association·Michael S SaagPaul A Volberding
May 24, 2021·The Lancet Infectious Diseases·Umang AroraNaveet Wig
Feb 25, 2021·Journal of Acquired Immune Deficiency Syndromes : JAIDS·Zinhle CindiPhumla Sinxadi
Jul 27, 2021·Frontiers in Genetics·Tessa A M MulderRon H N van Schaik
Aug 13, 2021·The American Journal of Gastroenterology·Amit S ChitnisRobert J Wong
Dec 2, 2021·AIDS·Phumla Z SinxadiMarta Boffito
Dec 6, 2021·Clinical Infectious Diseases : an Official Publication of the Infectious Diseases Society of America·Vera E BukkemsUNKNOWN PANNA network
Jan 21, 2022·European Journal of Gastroenterology & Hepatology·Ashley HubbardRobert Wong

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antivirals

Antivirals are medications that are used specifically for treating viral infections. Discover the latest research on antivirals here.

Antivirals (ASM)

Antivirals are medications that are used specifically for treating viral infections. Discover the latest research on antivirals here.

Antimicrobial Resistance (ASM)

Antimicrobial resistance poses a significant threat to the continued successful use of antimicrobial agents for the treatment of bacterial infections.

Antimicrobial Resistance

Antimicrobial resistance poses a significant threat to the continued successful use of antimicrobial agents for the treatment of bacterial infections.