DGIdb - EFAVIRENZ Drug Record

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: 1.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26774523 24729586 24080498 23172109 20860463 19779319 19487252

Sources:
PharmGKB
EFAVIRENZ NR1I3

Interaction Score: 0.4

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24080498 23173844 23172109

Sources:
PharmGKB
EFAVIRENZ ABCC3

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21189339 17172311

Sources:
DTC
EFAVIRENZ HNF4A

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26774523

Sources:
PharmGKB
EFAVIRENZ IL10

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24819158

Sources:
PharmGKB
EFAVIRENZ NAT2

Interaction Score: 0.3

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23990572

Sources:
PharmGKB
EFAVIRENZ ABCC2

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21189339 17172311 26774523

Sources:
DTC PharmGKB
EFAVIRENZ ABCB1

Interaction Score: 0.18

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 HLA-DRB1

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18301070

Sources:
PharmGKB
EFAVIRENZ ABCG2

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21189339 23859571

Sources:
DTC PharmGKB
EFAVIRENZ CYP2B6

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17041008

Sources:
NCI FDA
EFAVIRENZ CYP3A5

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24477223 20860463 20625352 16267764 15622315

Sources:
PharmGKB
EFAVIRENZ ABCC1

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21189339 17172311

Sources:
DTC
EFAVIRENZ UGT1A1

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24729586

Sources:
PharmGKB
EFAVIRENZ NPSR1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
EFAVIRENZ HTR2A

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23859571

Sources:
PharmGKB
EFAVIRENZ NR1I2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
EFAVIRENZ CYP3A4

Interaction Score: 0.01

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:

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

Zembruski NC et al., 2011, Interaction potential of etravirine with drug transporters assessed in vitro., Antimicrob Agents Chemother

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

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

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:

EFAVIRENZ Drug Record

EFAVIRENZ chembl:CHEMBL223228 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26774523 24729586 24080498 23172109 20860463 19779319 19487252

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24080498 23173844 23172109

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21189339 17172311

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26774523

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24819158

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23990572

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21189339 17172311 26774523

Sources: DTC PharmGKB

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18301070

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21189339 23859571

Sources: DTC PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17041008

Sources: NCI FDA

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24477223 20860463 20625352 16267764 15622315

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21189339 17172311

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24729586

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23859571

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16267764 15622315 16176117

Sources: NCI PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Interaction Types & Directionality:

n/a

PMIDs:
26774523 24729586 24080498 23172109 20860463 19779319 19487252

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
24080498 23173844 23172109

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
21189339 17172311

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
26774523

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
24819158

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
23990572

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
21189339 17172311 26774523

Sources:
DTC PharmGKB

Interaction Types & Directionality:

n/a

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

Sources:
DTC PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
18301070

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
21189339 23859571

Sources:
DTC PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
17041008

Sources:
NCI FDA

Interaction Types & Directionality:

n/a

PMIDs:
24477223 20860463 20625352 16267764 15622315

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
21189339 17172311

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
24729586

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
23859571

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
16267764 15622315 16176117

Sources:
NCI PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

C29027 NCI drug code

Alternate Names:

CHEMBL223228 ChEMBL Drug ID

Alternate Names:

D07HVY TTD Drug ID