197
Views
0
CrossRef citations to date
0
Altmetric
Research Article

Pharmacogenomics and Pharmacokinetics of Efavirenz 400 or 600 mg in 184 Treatment-Naive HIV-Infected Patients in China

, , , , , , , , & ORCID Icon show all
Pages 945-956 | Received 13 Nov 2019, Accepted 05 Jun 2020, Published online: 25 Aug 2020

References

  • OARAC . Guidelines for the use of antiretroviral agents in adults and adolescents living with HIV. (2019). www.aidsinfo.nih.gov/guidelines
  • European AIDS Clinical Society . EACS guidelines (version 9.1). (2018). http://www.eacsociety.org/files/2018_guidelines-9.1-english.pdf
  • Li X , BrownTT , HoKSet al. Recent trends and effectiveness of antiretroviral regimens among men who have sex with men living with HIV in the United States: the Multicenter AIDS Cohort Study (MACS) 2008–2017. Open Forum Infect. Dis.6(9), z333 (2019).
  • Chen R , ChenJ , TangQet al. Use of comedications and potential drug–drug interactions in people living with HIV in China. J. Infect. Chemother.26(7), 722–728 (2020).
  • Amariles P , GalindoJ , Mueses-MarinHFet al. Effectiveness and safety of generic version of lamivudine/tenofovir and efavirenz in treatment naive HIV-infected patients: a nonrandomized, open-label, Phase IV study in Cali-Colombia, 2012–2014. Rev. Chilena Infectol.36(1), 32–40 (2019).
  • Harrington BJ , DiPreteBL , JumbeANet al. Safety and efficacy of Option B+ ART in Malawi: few severe maternal toxicity events or infant HIV infections among pregnant women initiating tenofovir/lamivudine/efavirenz. Trop. Med. Int. Health24(10), 1221–1228 (2019).
  • Cassetti I , MadrugaJV , SuleimanJMet al. The safety and efficacy of tenofovir DF in combination with lamivudine and efavirenz through 6 years in antiretroviral-naive HIV-1-infected patients. HIV Clin. Trials8(3), 164–172 (2007).
  • Kenedi CA , GoforthHW. A systematic review of the psychiatric side-effects of efavirenz. AIDS Behav.15(8), 1803–1818 (2011).
  • Sim J , HillA. Is pricing of dolutegravir equitable? A comparative analysis of price and country income level in 52 countries. J. Virus Erad.4(4), 230–237 (2018).
  • Vitoria M , HillA , FordNet al. The transition to dolutegravir and other new antiretrovirals in low-income and middle-income countries: what are the issues? AIDS 32(12), 1551–1561 (2018).
  • Carey D , PulsR , AminJet al. Efficacy and safety of efavirenz 400 mg daily versus 600 mg daily: 96-week data from the randomised, double-blind, placebo-controlled, non-inferiority ENCORE1 study. Lancet Infect. Dis.15(7), 793–802 (2015).
  • Carey D . Efavirenz 400 mg daily remains non-inferior to 600 mg: 96 week data from the double-blind, placebo-controlled ENCORE1 study. J. Int. AIDS Soc.17(3 Suppl. 4), 19523 (2014).
  • Kouanfack C , Mpoudi-EtameM , OmgbaBPet al. Dolutegravir-based or low-dose efavirenz-based regimen for the treatment of HIV-1. N. Engl. J. Med.381(9), 816–826 (2019).
  • ENCORE1 Study Group . Efficacy of 400mg efavirenz versus standard 600mg dose in HIV-infected, antiretroviral-naive adults (ENCORE1): a randomised, double-blind, placebo-controlled, non-inferiority trial. Lancet383(9927), 1474–1482 (2014).
  • WHO . Policy Brief: Update of Recommendations on First- and Second-Line Antiretroviral Regimens. (WHO/CDS/HIV/19.15). Licence: CC BY-NC-SA 3.0 IGO.2019. (2019). https://apps.who.int/iris/bitstream/handle/10665/325892/WHO-CDS-HIV-19.15-eng.pdf?sequence=1&isAllowed=y
  • Ayuso P , NearyM , ChiongJet al. Meta-analysis of the effect of CYP2B6, CYP2A6, UGT2B7 and CAR polymorphisms on efavirenz plasma concentrations.J. Antimicrob. Chemother.74(11), 3281–3290 (2019).
  • Cusato J , TomaselloC , SimieleMet al. Efavirenz pharmacogenetics in a cohort of Italian patients. Int. J. Antimicrob. Agents47(2), 117–123 (2016).
  • Dickinson L , AminJ , ElseLet al. Pharmacokinetic and pharmacodynamic comparison of once-daily efavirenz (400 mg vs. 600 mg) in treatment-naive HIV-infected patients: results of the ENCORE1 study. Clin. Pharmacol. Ther.98(4), 406–416 (2015).
  • Meng X , YinK , WangJet al. Effect of CYP2B6 gene polymorphisms on efavirenz plasma concentrations in chinese patients with HIV infection. PLoS ONE10(6), e130583 (2015).
  • Sinxadi PZ , LegerPD , McIlleronHMet al. Pharmacogenetics of plasma efavirenz exposure in HIV-infected adults and children in South Africa. Br. J. Clin. Pharmacol.80(1), 146–156 (2015).
  • Boffito M , LamordeM , WatkinsMet al. Antiretroviral dose optimization: the future of efavirenz 400 mg dosing. Curr. Opin. HIV AIDS12(4), 339–342 (2017).
  • Cerrone M , WangX , NearyMet al. Pharmacokinetics of efavirenz 400 mg once daily coadministered with isoniazid and rifampicin in human immunodeficiency virus-infected individuals. Clin. Infect. Dis.68(3), 446–452 (2019).
  • Lamorde M , WangX , NearyMet al. Pharmacokinetics, pharmacodynamics and pharmacogenetics of efavirenz 400 mg once daily during pregnancy and post-partum. Clin. Infect. Dis.67(5), 785–790 (2018).
  • Chen J , ChenR , ShenYet al. Efficacy and safety of lower dose tenofovir disoproxil fumarate and efavirenz versus standard dose in HIV-infected, antiretroviral-naive adults: a multicentre, randomized, noninferiority trial. Emerg. Microbes Infect.9(1), 843–850 (2020).
  • Barrett JC , FryB , MallerJet al. Haploview: analysis and visualization of LD and haplotype maps. Bioinformatics21(2), 263–265 (2005).
  • Manosuthi W , SukasemC , LueangniyomkulAet al. Impact of pharmacogenetic markers of CYP2B6, clinical factors and drug–drug interaction on efavirenz concentrations in HIV/tuberculosis-coinfected patients. Antimicrob. Agents Chemother.57(2), 1019–1024 (2013).
  • Lloret-Linares C , RahmounY , LopesAet al. Effect of body weight and composition on efavirenz, atazanavir or darunavir concentration. Therapie73(3), 185–191 (2018).
  • Gutierrez-Valencia A , VicianaP , PalaciosRet al. Stepped-dose versus full-dose efavirenz for HIV infection and neuropsychiatric adverse events: a randomized trial. Ann. Intern. Med.151(3), 149–156 (2009).
  • Haas DW , RibaudoHJ , KimRBet al. Pharmacogenetics of efavirenz and central nervous system side effects: an Adult AIDS Clinical Trials Group study. AIDS18(18), 2391–2400 (2004).
  • Swart M , EvansJ , SkeltonMet al. An expanded analysis of pharmacogenetics determinants of efavirenz response that includes 3′-UTR single nucleotide polymorphisms among Black South African HIV/AIDS patients. Front Genet.6, 356 (2015).
  • Habtewold A , AmogneW , MakonnenEet al. Long-term effect of efavirenz autoinduction on plasma/peripheral blood mononuclear cell drug exposure and CD4 count is influenced by UGT2B7 and CYP2B6 genotypes among HIV patients. J. Antimicrob. Chemother.66(10), 2350–2361 (2011).
  • Gallien S , JournotV , LoriotMAet al. Cytochrome 2B6 polymorphism and efavirenz-induced central nervous system symptoms: a substudy of the ANRS ALIZE trial. HIV Med.18(8), 537–545 (2017).
  • Soeria-Atmadja S , OsterbergE , GustafssonLLet al. Genetic variants in CYP2B6 and CYP2A6 explain interindividual variation in efavirenz plasma concentrations of HIV-infected children with diverse ethnic origin. PLoS ONE12(9), e181316 (2017).
  • Grilo NM , CorreiaMJ , SequeiraCet al. Efavirenz biotransformation as an up-stream event of mood changes in HIV-infected patients. Toxicol. Lett.260, 28–35 (2016).
  • Svard J , SpiersJP , MulcahyFet al. Nuclear receptor-mediated induction of CYP450 by antiretrovirals: functional consequences of NR1I2 (PXR) polymorphisms and differential prevalence in whites and sub-Saharan Africans. J. Acquir. Immune Defic. Syndr.55(5), 536–549 (2010).
  • Sukasem C , ManosuthiW , KoomdeeNet al. Low level of efavirenz in HIV-1-infected Thai adults is associated with the CYP2B6 polymorphism. Infection42(3), 469–474 (2014).
  • Sanchez MA , CabreraFS , CruzGRet al. Impact of pharmacogenetics on CNS side effects related to efavirenz. Pharmacogenomics14(10), 1167–1178 (2013).
  • de Almeida TB , de AzevedoM , PintoJet al. Drug metabolism and transport gene polymorphisms and efavirenz adverse effects in Brazilian HIV-positive individuals. J. Antimicrob. Chemother.73(9), 2460–2467 (2018).
  • Cortes CP , SiccardiM , ChaikanAet al. Correlates of efavirenz exposure in Chilean patients affected with human immunodeficiency virus reveals a novel association with a polymorphism in the constitutive androstane receptor. Ther. Drug Monit.35(1), 78–83 (2013).
  • Holzinger ER , GradyB , RitchieMDet al. Genome-wide association study of plasma efavirenz pharmacokinetics in AIDS Clinical Trials Group protocols implicates several CYP2B6 variants. Pharmacogenet. Genomics22(12), 858–867 (2012).
  • Hui KH , LeeSS , LamTN. Dose optimization of efavirenz based on individual CYP2B6 polymorphisms in Chinese patients positive for HIV. CPT Pharmacometrics Syst. Pharmacol.5(4), 182–191 (2016).
  • Zubiaur P , Saiz-RodriguezM , OchoaDet al. Influence of CYP2B6 activity score on the pharmacokinetics and safety of single dose efavirenz in healthy volunteers. Pharmacogenomics J.20(2), 235–245 (2020).
  • Desta Z , GammalRS , GongLet al. Clinical Pharmacogenetics Implementation Consortium (CPIC) guideline for CYP2B6 and efavirenz-containing antiretroviral therapy. Clin. Pharmacol. Ther.106(4), 726–733 (2019).
  • Ward BA , GorskiJC , JonesDRet al. The cytochrome P450 2B6 (CYP2B6) is the main catalyst of efavirenz primary and secondary metabolism: implication for HIV/AIDS therapy and utility of efavirenz as a substrate marker of CYP2B6 catalytic activity. J. Pharmacol. Exp. Ther.306(1), 287–300 (2003).
  • Dickinson L , AminJ , ElseLet al. Comprehensive pharmacokinetic, pharmacodynamic and pharmacogenetic evaluation of once-daily efavirenz 400 and 600 mg in treatment-naive HIV-infected patients at 96 weeks: results of the ENCORE1 study. Clin. Pharmacokinet.55(7), 861–873 (2016).
  • Apostolova N , FunesHA , Blas-GarciaAet al. Efavirenz and the CNS: what we already know and questions that need to be answered. J. Antimicrob. Chemother.70(10), 2693–2708 (2015).
  • Mollan KR , TierneyC , HellwegeJNet al. Race/ethnicity and the pharmacogenetics of reported suicidality with efavirenz among clinical trials participants. J. Infect. Dis.216(5), 554–564 (2017).
  • Vujkovic M , BellamySL , ZuppaAFet al. Polymorphisms in cytochrome P450 are associated with extensive efavirenz pharmacokinetics and CNS toxicities in an HIV cohort in Botswana. Pharmacogenomics J.18(5), 678–688 (2018).
  • Varshney E , SahaN , TandonMet al. Prevalence of poor and rapid metabolizers of drugs metabolized by CYP2B6 in North Indian population residing in Indian national capital territory. Springerplus1, 34 (2012).
  • Ribaudo HJ , LiuH , SchwabMet al. Effect of CYP2B6, ABCB1 and CYP3A5 polymorphisms on efavirenz pharmacokinetics and treatment response: an AIDS Clinical Trials Group study. J. Infect. Dis.202(5), 717–722 (2010).
  • Sukasem C , CresseyTR , PrapaithongPet al. Pharmacogenetic markers of CYP2B6 associated with efavirenz plasma concentrations in HIV-1 infected Thai adults. Br. J. Clin. Pharmacol.74(6), 1005–1012 (2012).
  • Poeta J , LindenR , AntunesMVet al. Plasma concentrations of efavirenz are associated with body weight in HIV-positive individuals. J. Antimicrob. Chemother.6(11), 2601–2604 (2011).
  • Guo F , ChengX , HsiehEet al. Prospective plasma efavirenz concentration assessment in Chinese HIV-infected adults enrolled in a large multicentre study. HIV Med.19(7), 440–451 (2018).
  • Pereira SA , BrancoT , CaixasUet al. Intra-individual variability in efavirenz plasma concentrations supports therapeutic drug monitoring based on quarterly sampling in the first year of therapy. Ther. Drug Monit.30(1), 60–66 (2008).

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.