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EFAVIRENZ Drug Record

  • Summary
  • Interactions
  • Claims
  • EFAVIRENZ chembl:CHEMBL223228 Approved

    Alternate Names:

    EFAVIRENZ
    SUSTIVA 600
    SUSTIVA
    (-)-6-CHLORO-4-CYCLOPROPYLETHYNYL-4-TRIFLUOROMETHYL-1,4-DIHYDRO-2H-3,1-BENZOXAZIN-2-ONE
    (S)-6-CHLORO-4-CYCLOPROPYLETHYNYL-4-TRIFLUOROMETHYL-1,4-DIHYDRO-BENZO[D][1,3]OXAZIN-2-ONE
    ÉFAVIRENZ
    6-CHLORO-4-(2-CYCLOPROPYL-1-ETHYNYL)-4-TRIFLUOROMETHYL-(4S)-1,4-DIHYDRO-2H-BENZO[D][1,3]OXAZIN-2-ONE
    EFAVIRENZUM
    (S)-6-CHLORO-4-(CYCLOPROPYLETHYNYL)-1,4-DIHYDRO-4-(TRIFLUOROMETHYL)-2H-3,1-BENZOXAZIN-2-ONE
    chembl:CHEMBL223228
    drugbank:00625
    rxcui:195085
    chemidplus:154598-52-4
    pubchem.compound:64139

    Drug Info:

    (2 More Sources)

    Publications:

    Bertrand J et al., 2014, Dependence of efavirenz- and rifampicin-isoniazid-based antituberculosis treatment drug-drug interaction on CYP2B6 and NAT2 genetic polymorphisms: ANRS 12154 study in Cambodia., J Infect Dis
    Sarfo FS et al., 2014, Pharmacogenetic associations with plasma efavirenz concentrations and clinical correlates in a retrospective cohort of Ghanaian HIV-infected patients., J Antimicrob Chemother
    Swart M et al., 2012, PXR and CAR single nucleotide polymorphisms influence plasma efavirenz levels in South African HIV/AIDS patients., BMC Med Genet
    Cortes CP et al., 2013, 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
    Vitezica ZG et al., 2008, HLA-DRB1*01 associated with cutaneous hypersensitivity induced by nevirapine and efavirenz., AIDS
    Haas DW et al., 2014, Secondary metabolism pathway polymorphisms and plasma efavirenz concentrations in HIV-infected adults with CYP2B6 slow metabolizer genotypes., J Antimicrob Chemother
    Zembruski NC et al., 2011, Interaction potential of etravirine with drug transporters assessed in vitro., Antimicrob Agents Chemother
    Sánchez Martín A et al., 2013, Impact of pharmacogenetics on CNS side effects related to efavirenz., Pharmacogenomics
    Rodrigues Rde O et al., 2014, Interleukin-10 gene polymorphism (-1082G/A) and allergy to efavirenz in patients infected with human immunodeficiency virus., Braz J Infect Dis
    Haas DW et al., 2005, Pharmacogenetics of long-term responses to antiretroviral regimens containing Efavirenz and/or Nelfinavir: an Adult Aids Clinical Trials Group Study., J Infect Dis
    Haas DW et al., 2004, Pharmacogenetics of efavirenz and central nervous system side effects: an Adult AIDS Clinical Trials Group study., AIDS
    Le Tiec et al., 2005, Clinical pharmacokinetics and summary of efficacy and tolerability of atazanavir., Clin Pharmacokinet
    Weiss J et al., 2007, Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors., Drug Metab Dispos
    Cusato J et al., 2016, Efavirenz pharmacogenetics in a cohort of Italian patients., Int J Antimicrob Agents
    Elens L et al., 2010, Influence of host genetic factors on efavirenz plasma and intracellular pharmacokinetics in HIV-1-infected patients., Pharmacogenomics
    Kwara A et al., 2009, CYP2B6, CYP2A6 and UGT2B7 genetic polymorphisms are predictors of efavirenz mid-dose concentration in HIV-infected patients., AIDS
    Bélanger AS et al., 2009, Glucuronidation of the antiretroviral drug efavirenz by UGT2B7 and an in vitro investigation of drug-drug interaction with zidovudine., Drug Metab Dispos
    Faucette et al., 2007, Relative activation of human pregnane X receptor versus constitutive androstane receptor defines distinct classes of CYP2B6 and CYP3A4 inducers., J. Pharmacol. Exp. Ther.
    Zubiaur P et al., 2020, Influence of CYP2B6 activity score on the pharmacokinetics and safety of single dose efavirenz in healthy volunteers., Pharmacogenomics J
    Mukonzo JK et al., 2016, CYP2B6 genotype-based efavirenz dose recommendations during rifampicin-based antituberculosis cotreatment for a sub-Saharan Africa population., Pharmacogenomics
    Mukonzo JK et al., 2014, CYP2B6 genotype, but not rifampicin-based anti-TB cotreatments, explains variability in long-term efavirenz plasma exposure., Pharmacogenomics
    Mukonzo JK et al., 2014, Pharmacogenetic-based efavirenz dose modification: suggestions for an African population and the different CYP2B6 genotypes., PLoS One
    Mukonzo JK et al., 2013, Influence of efavirenz pharmacokinetics and pharmacogenetics on neuropsychological disorders in Ugandan HIV-positive patients with or without tuberculosis: a prospective cohort study., BMC Infect Dis
    Cabrera Figueroa S et al., 2010, The convergence of therapeutic drug monitoring and pharmacogenetic testing to optimize efavirenz therapy., Ther Drug Monit
    Ribaudo HJ et al., 2010, Effect of CYP2B6, ABCB1, and CYP3A5 polymorphisms on efavirenz pharmacokinetics and treatment response: an AIDS Clinical Trials Group study., J Infect Dis
    Chen J et al., 2010, CYP2B6 polymorphism and nonnucleoside reverse transcriptase inhibitor plasma concentrations in Chinese HIV-infected patients., Ther Drug Monit
    Ritchie MD et al., 2006, Drug transporter and metabolizing enzyme gene variants and nonnucleoside reverse-transcriptase inhibitor hepatotoxicity., Clin Infect Dis
    Csajka C et al., 2003, Population pharmacokinetics and effects of efavirenz in patients with human immunodeficiency virus infection., Clin Pharmacol Ther
    Fellay J et al., 2002, Response to antiretroviral treatment in HIV-1-infected individuals with allelic variants of the multidrug resistance transporter 1: a pharmacogenetics study., Lancet
    Sukasem C et al., 2014, Pharmacogenetics and clinical biomarkers for subtherapeutic plasma efavirenz concentration in HIV-1 infected Thai adults., Drug Metab Pharmacokinet
  • EFAVIRENZ   UGT2B7

    Interaction Score: 1.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26774523 24729586 24080498 23172109 20860463 19779319 19487252


    Sources:
    PharmGKB

  • EFAVIRENZ   NR1I3

    Interaction Score: 0.84

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24080498 23173844 23172109


    Sources:
    PharmGKB

  • EFAVIRENZ   HNF4A

    Interaction Score: 0.39

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26774523


    Sources:
    PharmGKB

  • EFAVIRENZ   ABCC3

    Interaction Score: 0.35

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21189339 17172311


    Sources:
    DTC

  • EFAVIRENZ   IL10

    Interaction Score: 0.35

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24819158


    Sources:
    PharmGKB

  • EFAVIRENZ   NAT2

    Interaction Score: 0.33

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23990572


    Sources:
    PharmGKB

  • EFAVIRENZ   ABCC2

    Interaction Score: 0.28

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21189339 17172311 26774523


    Sources:
    DTC PharmGKB

  • EFAVIRENZ   ABCB1

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    31628422 27045425 26774523 25303294 24497997 23734829 20860463 20720517 20662624 20625352 16912956 16267764 12545140 11809184 21189339


    Sources:
    DTC PharmGKB

  • EFAVIRENZ   ABCG2

    Interaction Score: 0.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21189339 23859571


    Sources:
    DTC PharmGKB

  • EFAVIRENZ   HLA-DRB1

    Interaction Score: 0.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18301070


    Sources:
    PharmGKB

  • EFAVIRENZ   CYP2B6

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17041008


    Sources:
    NCI FDA

  • EFAVIRENZ   ABCC1

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21189339 17172311


    Sources:
    DTC

  • EFAVIRENZ   CYP3A5

    Interaction Score: 0.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24477223 20860463 20625352 16267764 15622315


    Sources:
    PharmGKB

  • EFAVIRENZ   UGT1A1

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24729586


    Sources:
    PharmGKB

  • EFAVIRENZ   HTR2A

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23859571


    Sources:
    PharmGKB

  • EFAVIRENZ   NPSR1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • EFAVIRENZ   NR1I2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • EFAVIRENZ   CYP3A4

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16267764 15622315 16176117


    Sources:
    NCI PharmGKB

  • EFAVIRENZ   CYP2C19

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • EFAVIRENZ   NFE2L2

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • EFAVIRENZ   AR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • NCI: EFAVIRENZ

    • Version: 14-September-2017

    Alternate Names:
    C29027 NCI drug code

    Drug Info:

    Publications:
    Le Tiec et al., 2005, Clinical pharmacokinetics and summary of efficacy and tolerability of atazanavir., Clin Pharmacokinet
    Faucette et al., 2007, Relative activation of human pregnane X receptor versus constitutive androstane receptor defines distinct classes of CYP2B6 and CYP3A4 inducers., J. Pharmacol. Exp. Ther.

  • DTC: EFAVIRENZ

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL223228 ChEMBL Drug ID

    Drug Info:

    Publications:
    Zembruski NC et al., 2011, Interaction potential of etravirine with drug transporters assessed in vitro., Antimicrob Agents Chemother
    Weiss J et al., 2007, Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors., Drug Metab Dispos

  • PharmGKB: efavirenz

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Bertrand J et al., 2014, Dependence of efavirenz- and rifampicin-isoniazid-based antituberculosis treatment drug-drug interaction on CYP2B6 and NAT2 genetic polymorphisms: ANRS 12154 study in Cambodia., J Infect Dis
    Sarfo FS et al., 2014, Pharmacogenetic associations with plasma efavirenz concentrations and clinical correlates in a retrospective cohort of Ghanaian HIV-infected patients., J Antimicrob Chemother
    Swart M et al., 2012, PXR and CAR single nucleotide polymorphisms influence plasma efavirenz levels in South African HIV/AIDS patients., BMC Med Genet

  • TTD: Efavirenz

    • Version: 2020.06.01

    Alternate Names:
    D07HVY TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL223228

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Efavirenz

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21