Lack of a Clinically Significant Pharmacokinetic Interaction between Etravirine and Raltegravir Using an Original Approach Based on Drug Metabolism, Protein Binding, and Penetration in Seminal Fluid: A Pharmacokinetic Substudy of the ANRS-163 ETRAL Study

Pharmacotherapy
Minh Patrick LêANRS-163 ETRAL study group

Abstract

The ANRS163-ETRAL study showed that etravirine 200 mg/raltegravir 400 mg twice-daily dual therapy was highly effective in the treatment of human immunodeficiency virus (HIV)-infected patients older than 45 years, with virologic and therapeutic success rates at week 48 of 99.4% and 94.5%, respectively. The objective of this study was to determine whether a clinically significant pharmacokinetic interaction between etravirine and raltegravir exists by assessing steady-state total and unbound etravirine, raltegravir, and inactive raltegravir-glucuronide concentrations 12 hours after last intake (C12h ) in blood plasma (BP) and seminal plasma (SP). Pharmacokinetic analysis of data from the ANRS163-ETRAL study. One hundred forty-six HIV-1-infected patients (of the 165 patients included in the ANRS-163 ETRAL study) who were receiving etravirine 200 mg and raltegravir 400 mg twice daily. Blood was collected from all 146 patients at weeks 2-4, 12, 24, and 48, and semen was collected from 21 patients at week 48. The extent of BP and SP protein binding was determined by using ultrafiltration assay. Total and unbound etravirine, raltegravir, and raltegravir-glucuronide C12h were determined by ultra high performance liquid chromatography c...Continue Reading

References

Nov 11, 2009·Antimicrobial Agents and Chemotherapy·Anne-Genevieve MarcelinUNKNOWN ANRS AC11 Resistance Study Group
Sep 9, 2010·Antimicrobial Agents and Chemotherapy·Michael NeelyAlexandra Calmy
Dec 30, 2010·Antimicrobial Agents and Chemotherapy·Nadine Cécile Luise ZembruskiJohanna Weiss
May 11, 2011·Antimicrobial Agents and Chemotherapy·Ivy SongStephen C Piscitelli
Sep 17, 2011·Clinical Infectious Diseases : an Official Publication of the Infectious Diseases Society of America·Jürgen K RockstrohUNKNOWN STARTMRK Investigators
Jan 3, 2012·The Journal of Antimicrobial Chemotherapy·G FätkenheuerUNKNOWN SENSE Study Team
Sep 8, 2012·The Journal of Antimicrobial Chemotherapy·J M TiraboschiD Podzamczer
Sep 12, 2012·Antimicrobial Agents and Chemotherapy·Edward P AcostaChristos J Petropoulos
Jan 22, 2013·The Journal of Antimicrobial Chemotherapy·Anh NguyenUNKNOWN CHARTER Group
Jul 17, 2013·Antimicrobial Agents and Chemotherapy·Caroline BarauAurélie Barrail-Tran
Feb 13, 2014·Antiviral Therapy·Tony AntoniouCharles la Porte
May 13, 2014·Reproductive Toxicology·David M KleinNathan J Cherrington
May 16, 2014·Current Opinion in HIV and AIDS·Dominique Costagliola
Feb 19, 2015·Antimicrobial Agents and Chemotherapy·M Tozammel HoqueReina Bendayan

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Citations

Apr 8, 2020·The Journal of Antimicrobial Chemotherapy·Cathia SoulieUNKNOWN ANRS-163 ETRAL study group

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