U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C14H9ClF3NO2
Molecular Weight 315.675
Optical Activity ( - )
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of EFAVIRENZ

SMILES

FC(F)(F)[C@]1(OC(=O)NC2=C1C=C(Cl)C=C2)C#CC3CC3

InChI

InChIKey=XPOQHMRABVBWPR-ZDUSSCGKSA-N
InChI=1S/C14H9ClF3NO2/c15-9-3-4-11-10(7-9)13(14(16,17)18,21-12(20)19-11)6-5-8-1-2-8/h3-4,7-8H,1-2H2,(H,19,20)/t13-/m0/s1

HIDE SMILES / InChI

Molecular Formula C14H9ClF3NO2
Molecular Weight 315.675
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: Description was created based on several sources, including

Efavirenz (brand names Sustiva® and Stocrin®) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and is used as part of highly active antiretroviral therapy (HAART) for the treatment of a human immunodeficiency virus (HIV) type 1. For HIV infection that has not previously been treated, efavirenz and lamivudine in combination with zidovudine or tenofovir is the preferred NNRTI-based regimen. Efavirenz is also used in combination with other antiretroviral agents as part of an expanded postexposure prophylaxis regimen to prevent HIV transmission for those exposed to materials associated with a high risk for HIV transmission.

Originator

Curator's Comment: # Merck & Co

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
4.0 nM [EC50]
26.1 µM [IC50]
52.0 µM [IC50]
20.0 nM [EC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
SUSTIVA

Approved Use

SUSTIVA is a non-nucleoside reverse transcriptase inhibitor indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus type 1 infection.

Launch Date

9.05904E11
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
12.9 μM
600 mg 1 times / day steady-state, oral
dose: 600 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
EFAVIRENZ plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
7.04 μg/mL
300 mg 1 times / day steady-state, oral
dose: 300 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
EFAVIRENZ plasma
Homo sapiens
population: UNHEALTHY
age: CHILD
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
184 μM × h
600 mg 1 times / day steady-state, oral
dose: 600 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
EFAVIRENZ plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
257.56 μM × h
300 mg 1 times / day steady-state, oral
dose: 300 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
EFAVIRENZ plasma
Homo sapiens
population: UNHEALTHY
age: CHILD
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
40 h
600 mg 1 times / day steady-state, oral
dose: 600 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
EFAVIRENZ plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
0.5%
600 mg 1 times / day steady-state, oral
dose: 600 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
EFAVIRENZ plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
3 g single, oral
Overdose
Dose: 3 g
Route: oral
Route: single
Dose: 3 g
Sources:
unhealthy, 12 years
n = 1
Health Status: unhealthy
Condition: HIV infection
Age Group: 12 years
Sex: M
Population Size: 1
Sources:
600 mg 1 times / day multiple, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Co-administed with::
abacavir(300 mg q12h)
nelfinavir(1250 mg q12h)
Sources:
unhealthy, 33 years
n = 1
Health Status: unhealthy
Condition: HIV infection
Age Group: 33 years
Sex: F
Population Size: 1
Sources:
Disc. AE: Mania...
AEs leading to
discontinuation/dose reduction:
Mania (1 patient)
Sources:
25 mg/kg 1 times / day steady, oral
Highest studied dose
Dose: 25 mg/kg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg/kg, 1 times / day
Sources:
unhealthy, 33.9 months (range: 29.2–40.2 months)
n = 52
Health Status: unhealthy
Condition: HIV infection
Age Group: 33.9 months (range: 29.2–40.2 months)
Sex: M+F
Population Size: 52
Sources:
800 mg 1 times / day steady, oral
Highest studied dose
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources:
unhealthy, 37.3 years
n = 67
Health Status: unhealthy
Condition: tuberculosis
Age Group: 37.3 years
Sex: M+F
Population Size: 67
Sources:
Disc. AE: Hallucination, Dizziness...
AEs leading to
discontinuation/dose reduction:
Hallucination (1 patient)
Dizziness (1 patient)
Insomnia (1 patient)
Hepatotoxicity (1 patient)
Skin rash (1 patient)
Pruritus (1 patient)
Rash (1 patient)
Sources:
AEs

AEs

AESignificanceDosePopulation
Mania 1 patient
Disc. AE
600 mg 1 times / day multiple, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Co-administed with::
abacavir(300 mg q12h)
nelfinavir(1250 mg q12h)
Sources:
unhealthy, 33 years
n = 1
Health Status: unhealthy
Condition: HIV infection
Age Group: 33 years
Sex: F
Population Size: 1
Sources:
Dizziness 1 patient
Disc. AE
800 mg 1 times / day steady, oral
Highest studied dose
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources:
unhealthy, 37.3 years
n = 67
Health Status: unhealthy
Condition: tuberculosis
Age Group: 37.3 years
Sex: M+F
Population Size: 67
Sources:
Hallucination 1 patient
Disc. AE
800 mg 1 times / day steady, oral
Highest studied dose
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources:
unhealthy, 37.3 years
n = 67
Health Status: unhealthy
Condition: tuberculosis
Age Group: 37.3 years
Sex: M+F
Population Size: 67
Sources:
Hepatotoxicity 1 patient
Disc. AE
800 mg 1 times / day steady, oral
Highest studied dose
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources:
unhealthy, 37.3 years
n = 67
Health Status: unhealthy
Condition: tuberculosis
Age Group: 37.3 years
Sex: M+F
Population Size: 67
Sources:
Insomnia 1 patient
Disc. AE
800 mg 1 times / day steady, oral
Highest studied dose
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources:
unhealthy, 37.3 years
n = 67
Health Status: unhealthy
Condition: tuberculosis
Age Group: 37.3 years
Sex: M+F
Population Size: 67
Sources:
Pruritus 1 patient
Disc. AE
800 mg 1 times / day steady, oral
Highest studied dose
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources:
unhealthy, 37.3 years
n = 67
Health Status: unhealthy
Condition: tuberculosis
Age Group: 37.3 years
Sex: M+F
Population Size: 67
Sources:
Rash 1 patient
Disc. AE
800 mg 1 times / day steady, oral
Highest studied dose
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources:
unhealthy, 37.3 years
n = 67
Health Status: unhealthy
Condition: tuberculosis
Age Group: 37.3 years
Sex: M+F
Population Size: 67
Sources:
Skin rash 1 patient
Disc. AE
800 mg 1 times / day steady, oral
Highest studied dose
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources:
unhealthy, 37.3 years
n = 67
Health Status: unhealthy
Condition: tuberculosis
Age Group: 37.3 years
Sex: M+F
Population Size: 67
Sources:
PubMed

PubMed

TitleDatePubMed
A novel genotype encoding a single amino acid insertion and five other substitutions between residues 64 and 74 of the HIV-1 reverse transcriptase confers high-level cross-resistance to nucleoside reverse transcriptase inhibitors. Abacavir CNA2007 International Study Group.
1999 Oct 1
Prevalence and characteristics of multinucleoside-resistant human immunodeficiency virus type 1 among European patients receiving combinations of nucleoside analogues.
2000 Aug
Efavirenz: a pharmacoeconomic review of its use in HIV infection.
2001
Retinal toxicity due to Efavirenz.
2001 Apr
Smaller amounts of antiretroviral drugs are needed when combined with an active ribozyme against HIV-1.
2001 Apr
An open-label randomized trial to evaluate different therapeutic strategies of combination therapy in HIV-1 infection: design, rationale, and methods of the initio trial.
2001 Apr
Amino acid deletion at codon 67 and Thr-to-Gly change at codon 69 of human immunodeficiency virus type 1 reverse transcriptase confer novel drug resistance profiles.
2001 Apr
Performance of a quadruple combination including nelfinavir plus efavirenz in naive subjects with high baseline viral load and in patients failing protease inhibitor-containing regimens.
2001 Apr 1
Persistent dyslipidemia in HIV-infected individuals switched from a protease inhibitor-containing to an efavirenz-containing regimen.
2001 Apr 1
Determination of serum levels of thirteen human immunodeficiency virus-suppressing drugs by high-performance liquid chromatography.
2001 Apr 13
High prevalence of genotypic and phenotypic HIV-1 drug-resistant strains among patients receiving antiretroviral therapy in Abidjan, Côte d'Ivoire.
2001 Apr 15
A pilot study of the use of mycophenolate mofetil as a component of therapy for multidrug-resistant HIV-1 infection.
2001 Apr 15
[Results of the AIDS-In-Europe Study. Non-nucleoside reverse transcriptase inhibitor does not equal non-nucleoside reverse transcriptase inhibitor].
2001 Apr 2
[Positive change from protease inhibitor to non-nucleoside reverse transcriptase inhibitor efavirenz. Improved virus control thanks to protease inhibitor switch].
2001 Apr 2
Antiviral drugs: current state of the art.
2001 Aug
Preliminary data of a prospective study on neuropsychiatric side effects after initiation of efavirenz.
2001 Aug 1
Non-nucleoside reverse transcriptase inhibitor failure impairs HIV-RNA responses to efavirenz-containing salvage antiretroviral therapy.
2001 Aug 17
Solution structures and reactivities of the mixed aggregates derived from n-butyllithium and vicinal amino alkoxides.
2001 Aug 22
Antiretroviral therapy for previously treated patients.
2001 Aug 9
Nelfinavir, efavirenz, or both after the failure of nucleoside treatment of HIV infection.
2001 Aug 9
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
2001 Feb 1
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
2001 Feb 12
Dynamics of seminal plasma HIV-1 decline after antiretroviral treatment.
2001 Feb 16
Tolerance of efavirenz in children.
2001 Jan 26
Efavirenz plasma levels can predict treatment failure and central nervous system side effects in HIV-1-infected patients.
2001 Jan 5
Efavirenz-associated breast hypertrophy in HIV-infection patients.
2001 Jan 5
Protease-sparing regimen in a real-life practice with naïve patients: an equal opportunity approach?
2001 Jan-Feb
Eruptive cheilitis: a new adverse effect in reactive HIV-positive patients subjected to high activity antiretroviral therapy (HAART). Presentation of six clinical cases.
2001 Jan-Feb
New developments in anti-HIV chemotherapy.
2001 Jan-Feb
Predictors of protease inhibitor-associated adverse events.
2001 Jul
Manic syndrome associated with efavirenz overdose.
2001 Jul 15
Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors.
2001 Jul 23
Gynecomastia without lipodystrophy syndrome in HIV-infected men treated with efavirenz.
2001 Jul 27
Metformin in an HIV-infected patient with protease inhibitor-induced diabetic ketoacidosis.
2001 Jul-Aug
In vitro anti-HIV-1 synergy between non-nucleoside reverse transcriptase inhibitors nevirapine and efavirenz.
2001 Jun
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.
2001 Jun 4
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
2001 Jun 7
Competition prompts drug companies to cut antiretroviral drug prices.
2001 Mar 17
Sequencing antiretroviral drugs.
2001 Mar 30
Efavirenz-induced acute eosinophilic hepatitis.
2001 May
Pulmonary hypersensitivity reaction induced by efavirenz.
2001 May 12
Synthesis and evaluation of efavirenz (Sustiva) analogues as HIV-1 reverse transcriptase inhibitors: replacement of the cyclopropylacetylene side chain.
2001 May 7
[Apropos of atypical melancholia with Sustiva (efavirenz)].
2001 May-Jun
Evidence of hypertriglyceridemia in managing HIV patients on efavirenz.
2001 May-Jun
Other issues: penetration into sanctuary sites, immune reconstitution and NNRTI sequencing.
2001 Nov
Factors affecting adherence and convenience in antiretroviral therapy.
2001 Nov
Comparison of NNRTIs in antiretroviral-experienced patients.
2001 Nov
Comparison of NNRTIs in antiretroviral-naïve patients.
2001 Nov
Mismatched double-stranded RNA (polyI-polyC(12)U) is synergistic with multiple anti-HIV drugs and is active against drug-sensitive and drug-resistant HIV-1 in vitro.
2001 Sep
Comparison of initial combination antiretroviral therapy with a single protease inhibitor, ritonavir and saquinavir, or efavirenz.
2001 Sep 7
Patents

Sample Use Guides

SUSTIVA should be taken orally once daily on an empty stomach, preferably at bedtime. • Recommended adult dose: 600 mg. • With voriconazole, increase voriconazole maintenance dose to 400 mg every 12 hours and decrease SUSTIVA dose to 300 mg once daily using the capsule formulation.
Route of Administration: Oral
10 pM efavirenz completely inhibited 0.5 U HIV RT.
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:45:38 UTC 2023
Edited
by admin
on Fri Dec 15 15:45:38 UTC 2023
Record UNII
JE6H2O27P8
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
EFAVIRENZ
EMA EPAR   HSDB   INN   JAN   MART.   MI   ORANGE BOOK   USP-RS   VANDF   WHO-DD   WHO-IP  
USAN   INN  
Official Name English
L-743726
Code English
EFAVIRENZ [USP MONOGRAPH]
Common Name English
SUSTIVA
Brand Name English
(S)-6-Chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one
Systematic Name English
EFAVIRENZ [EMA EPAR]
Common Name English
NSC-742403
Code English
DMP-266
Code English
EFAVIRENZ [MI]
Common Name English
EFAVIRENZ [VANDF]
Common Name English
EFAVIRENZ [ORANGE BOOK]
Common Name English
EFAVIRENZ [WHO-IP]
Common Name English
EFAVIRENZ [USAN]
Common Name English
EFAVIRENZUM [WHO-IP LATIN]
Common Name English
EFAVIRENZ [HSDB]
Common Name English
EFAVIRENZ [JAN]
Common Name English
VIRADAY
Brand Name English
efavirenz [INN]
Common Name English
(4S)-6-Chloro-4-(2-cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one
Systematic Name English
TELURA COMPONENT EFAVIRENZ
Brand Name English
Efavirenz [WHO-DD]
Common Name English
2H-3,1-Benzoxazin-2-one, 6-chloro-4-(2-cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-, (4S)-
Systematic Name English
STOCRIN
Brand Name English
EFAVIRENZ [USP-RS]
Common Name English
EFAVIRENZ TEVA
Brand Name English
EFV
Common Name English
EFAVIRENZ [MART.]
Common Name English
EFAVIRENZ COMPONENT OF ATRIPLA
Common Name English
ATRIPLA COMPONENT EFAVIRENZ
Common Name English
(-)-Efavirenz
Common Name English
Classification Tree Code System Code
NDF-RT N0000009948
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
LIVERTOX NBK548521
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
WHO-ATC J05AR11
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
NDF-RT N0000175460
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
EMA ASSESSMENT REPORTS SUSTIVA (AUTHORIZED: HIV INFECTIONS)
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
EMA ASSESSMENT REPORTS ATRIPLA (AUTHORIZED: HIV INFECTIONS)
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
NDF-RT N0000175463
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
WHO-ESSENTIAL MEDICINES LIST 6.4.2.3 (EFV/FTC/TEN)
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
WHO-VATC QJ05AR11
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
WHO-ATC J05AR06
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
WHO-VATC QJ05AR06
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
WHO-ESSENTIAL MEDICINES LIST 6.4.2.2
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
NCI_THESAURUS C97453
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
WHO-VATC QJ05AG03
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
WHO-ATC J05AG03
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
EMA ASSESSMENT REPORTS STOCRIN (AUTHORIZED: HIV INFECTIONS)
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
EMA ASSESSMENT REPORTS EFAVIRENZ TEVA (AUTHORIZED: HIV INFECTIONS)
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
Code System Code Type Description
NDF-RT
N0000182140
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY Cytochrome P450 2C19 Inhibitors [MoA]
DAILYMED
JE6H2O27P8
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
ChEMBL
CHEMBL223228
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
EPA CompTox
DTXSID9046029
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
DRUG CENTRAL
989
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
WHO INTERNATIONAL PHARMACOPEIA
EFAVIRENZ
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY Description: White to slightly pink powder.Solubility: Practically insoluble in water, freely soluble in methanol.Category. Antiretroviral (Non-nucleoside Reverse Transcriptase Inhibitor).Storage. Efavirenz should be kept in a well-closed container, protected from light.Additional information: Efavirenz may exhibit polymorphism.Requirements: Definition: Efavirenz contains not less than 97.0% and not more than 103.0% of C14H9ClF3NO2, calculated with reference to thedried substance.Manufacture: The production method is validated to ensure that the substance is the (4S)-enantiomer.
EVMPD
SUB06463MIG
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
PUBCHEM
64139
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
MESH
C098320
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
RS_ITEM_NUM
1234103
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
RXCUI
195085
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY RxNorm
NDF-RT
N0000182141
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY Cytochrome P450 3A4 Inhibitors [MoA]
LACTMED
Efavirenz
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
MERCK INDEX
m4839
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY Merck Index
HSDB
7163
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
CHEBI
119486
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
INN
7718
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
FDA UNII
JE6H2O27P8
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
NCI_THESAURUS
C29027
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
SMS_ID
100000085266
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
WIKIPEDIA
EFAVIRENZ
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
USAN
II-77
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
NDF-RT
N0000185504
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY Cytochrome P450 2C9 Inhibitors [MoA]
NDF-RT
N0000187064
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY Cytochrome P450 2B6 Inducers [MoA]
CAS
154598-52-4
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
DRUG BANK
DB00625
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
NDF-RT
N0000190118
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY Cytochrome P450 3A Inducers [MoA]
NSC
742403
Created by admin on Fri Dec 15 15:45:38 UTC 2023 , Edited by admin on Fri Dec 15 15:45:38 UTC 2023
PRIMARY
Related Record Type Details
METABOLIC ENZYME -> SUBSTRATE
TRANSPORTER -> INHIBITOR
BASIS OF STRENGTH->SUBSTANCE
calculated on the anhydrous, solvent-free basis
ASSAY (HPLC)
USP
TRANSPORTER -> INHIBITOR
TARGET ORGANISM->INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
BINDER->LIGAND
BINDING
TARGET -> INHIBITOR
TRANSPORTER -> INHIBITOR
Related Record Type Details
METABOLITE ACTIVE -> PARENT
THE MAJOR OXIDATIVE METABOLITE OF EFAVIRENZ IN VIVO AND IN VITRO HUMAN LIVER MICROSOMAL PREPARATIONS IS 8-HYDROXYEFAVIRENZ
MAJOR
METABOLITE -> PARENT
7-HYDROXYEFAVIRENZ REPRESENTS A MINOR PATHWAY
MINOR
Related Record Type Details
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
IMPURITY -> PARENT
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC IN HIV-INFECTED PATIENTS

ORAL ADMINISTRATION

AT STEADY-STATE

SINGLE DOSE

Biological Half-life PHARMACOKINETIC SINGLE DOSE

Biological Half-life PHARMACOKINETIC MULTIPLE DOSES

Tmax PHARMACOKINETIC SINGLE DOSE

ORAL ADMINISTRATION

IN UNINFECTED VOLUNTEERS