Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C14H9ClF3NO2 |
Molecular Weight | 315.6754 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C1CC1C#C[C@]2(c3cc(ccc3N=C(O)O2)Cl)C(F)(F)F
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
Molecular Formula | C14H9ClF3NO2 |
Molecular Weight | 315.6754 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: http://www.drugbank.ca/drugs/DB00625Curator's Comment:: Description was created based on several sources, including
Sources: http://www.drugbank.ca/drugs/DB00625
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.
CNS Activity
Originator
Sources: http://adisinsight.springer.com/drugs/800005773
Curator's Comment:: # Merck & Co
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL378 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19469474 |
4.0 nM [EC50] | ||
Target ID: CHEMBL612848 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27249967 |
26.1 µM [IC50] | ||
Target ID: CHEMBL206 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20408889 |
52.0 µM [IC50] | ||
Target ID: CHEMBL247 Sources: http://www.drugbank.ca/drugs/DB00625 |
20.0 nM [EC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | SUSTIVA Approved UseSUSTIVA 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 Date9.05904E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Dose | Population | Adverse events |
---|---|---|
3 g single, oral Overdose |
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) Sources: nelfinavir(1250 mg q12h) |
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) Sources: Dizziness (1 patient) Insomnia (1 patient) Hepatotoxicity (1 patient) Skin rash (1 patient) Pruritus (1 patient) Rash (1 patient) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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) Sources: nelfinavir(1250 mg q12h) |
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
Title | Date | PubMed |
---|---|---|
Four new antiretroviral medications will soon offer more options to HIV patients. | 1998 Jul-Aug |
|
Antiretroviral therapy in pregnancy: a focus on safety. | 2001 |
|
A single amino acid change at Leu-188 in the reverse transcriptase of HIV-2 and SIV renders them sensitive to non-nucleoside reverse transcriptase inhibitors. | 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 |
|
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 |
|
[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 |
|
Antiretroviral rounds. When success is a pain. | 2001 Aug |
|
Antiretrovirals: simultaneous determination of five protease inhibitors and three nonnucleoside transcriptase inhibitors in human plasma by a rapid high-performance liquid chromatography--mass spectrometry assay. | 2001 Aug |
|
Antiviral drugs: current state of the art. | 2001 Aug |
|
Efavirenz as a substitute for protease inhibitors in HIV-1-infected patients with undetectable plasma viral load on HAART: a median follow-up of 64 weeks. | 2001 Aug 15 |
|
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase. | 2001 Aug 2 |
|
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 |
|
Dynamics of seminal plasma HIV-1 decline after antiretroviral treatment. | 2001 Feb 16 |
|
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 |
|
Management of sudden psychiatric disorders related to efavirenz. | 2001 Jul 6 |
|
Metformin in an HIV-infected patient with protease inhibitor-induced diabetic ketoacidosis. | 2001 Jul-Aug |
|
Limits of deep salvage antiretroviral therapy with nelfinavir plus either efavirenz or nevirapine, in highly pre-treated patients with HIV disease. | 2001 Jun |
|
Efavirenz plasma concentrations and efficiency. | 2001 Jun 15 |
|
Phenotypic hypersusceptibility to non-nucleoside reverse transcriptase inhibitors in treatment-experienced HIV-infected patients: impact on virological response to efavirenz-based therapy. | 2001 Jun 15 |
|
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors. | 2001 Jun 4 |
|
Use of MM-PBSA in reproducing the binding free energies to HIV-1 RT of TIBO derivatives and predicting the binding mode to HIV-1 RT of efavirenz by docking and MM-PBSA. | 2001 Jun 6 |
|
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. | 2001 Jun 7 |
|
Identification of a putative binding site for [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)thymine (TSAO) derivatives at the p51-p66 interface of HIV-1 reverse transcriptase. | 2001 Jun 7 |
|
The pharmacokinetics of methadone in HIV-positive patients receiving the non-nucleoside reverse transcriptase inhibitor efavirenz. | 2001 Mar |
|
Anti-AIDS drugs available 'at cost'. | 2001 Mar 15 |
|
Sequencing antiretroviral drugs. | 2001 Mar 30 |
|
Efavirenz-induced acute eosinophilic hepatitis. | 2001 May |
|
Development and validation of a reverse-phase HPLC method for analysis of efavirenz and its related substances in the drug substance and in a capsule formulation. | 2001 May |
|
Pulmonary hypersensitivity reaction induced by efavirenz. | 2001 May 12 |
|
Efavirenz-induced photoallergic dermatitis in HIV. | 2001 May 25 |
|
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 |
|
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-naïve patients. | 2001 Nov |
|
The role of NNRTIs in antiretroviral combination therapy: an introduction. | 2001 Nov |
|
The stereoselective targeting of a specific enzyme-substrate complex is the molecular mechanism for the synergic inhibition of HIV-1 reverse transcriptase by (R)-(-)-PPO464: a novel generation of nonnucleoside inhibitors. | 2001 Nov 30 |
|
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 |
|
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. | 2001 Sep 3 |
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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24068579
10 pM efavirenz completely inhibited 0.5 U HIV RT.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Jun 25 21:38:46 UTC 2021
by
admin
on
Fri Jun 25 21:38:46 UTC 2021
|
Record UNII |
JE6H2O27P8
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
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Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
NDF-RT |
N0000009948
Created by
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LIVERTOX |
341
Created by
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WHO-ATC |
J05AR11
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NDF-RT |
N0000175460
Created by
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EMA ASSESSMENT REPORTS |
SUSTIVA (AUTHORIZED: HIV INFECTIONS)
Created by
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|
EMA ASSESSMENT REPORTS |
ATRIPLA (AUTHORIZED: HIV INFECTIONS)
Created by
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NDF-RT |
N0000175463
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WHO-ESSENTIAL MEDICINES LIST |
6.4.2.3 (EFV/FTC/TEN)
Created by
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WHO-VATC |
QJ05AR11
Created by
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WHO-ATC |
J05AR06
Created by
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WHO-VATC |
QJ05AR06
Created by
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WHO-ESSENTIAL MEDICINES LIST |
6.4.2.2
Created by
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NCI_THESAURUS |
C97453
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WHO-VATC |
QJ05AG03
Created by
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WHO-ATC |
J05AG03
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EMA ASSESSMENT REPORTS |
STOCRIN (AUTHORIZED: HIV INFECTIONS)
Created by
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EMA ASSESSMENT REPORTS |
EFAVIRENZ TEVA (AUTHORIZED: HIV INFECTIONS)
Created by
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Code System | Code | Type | Description | ||
---|---|---|---|---|---|
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N0000182140
Created by
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PRIMARY | Cytochrome P450 2C19 Inhibitors [MoA] | ||
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CHEMBL223228
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PRIMARY | |||
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1234103
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PRIMARY | USP-RS | ||
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154598-52-4
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PRIMARY | |||
|
989
Created by
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PRIMARY | |||
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EFAVIRENZ
Created by
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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. | ||
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SUB06463MIG
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PRIMARY | |||
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64139
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PRIMARY | |||
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C098320
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PRIMARY | |||
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195085
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PRIMARY | RxNorm | ||
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N0000182141
Created by
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PRIMARY | Cytochrome P450 3A4 Inhibitors [MoA] | ||
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Efavirenz
Created by
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PRIMARY | |||
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M4839
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PRIMARY | Merck Index | ||
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7163
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PRIMARY | |||
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7718
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PRIMARY | |||
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JE6H2O27P8
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PRIMARY | |||
|
C29027
Created by
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PRIMARY | |||
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EFAVIRENZ
Created by
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PRIMARY | |||
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N0000185504
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PRIMARY | Cytochrome P450 2C9 Inhibitors [MoA] | ||
|
N0000187064
Created by
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PRIMARY | Cytochrome P450 2B6 Inducers [MoA] | ||
|
154598-52-4
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PRIMARY | |||
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DB00625
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PRIMARY | |||
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N0000190118
Created by
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PRIMARY | Cytochrome P450 3A Inducers [MoA] |
Related Record | Type | Details | ||
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INHIBITOR->TARGET ORGANISM | |||
|
TRANSPORTER -> INHIBITOR | |||
|
BASIS OF STRENGTH->SUBSTANCE |
calculated on the anhydrous, solvent-free basis
ASSAY (HPLC)
USP
|
||
|
TRANSPORTER -> INHIBITOR | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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BINDER->LIGAND |
BINDING
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|
TRANSPORTER -> INHIBITOR | |||
|
METABOLIC ENZYME -> SUBSTRATE |
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 | |||
|
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 |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT | |||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Tmax | PHARMACOKINETIC |
|
IN HIV-INFECTED PATIENTS |
|
||
Biological Half-life | PHARMACOKINETIC |
|
SINGLE DOSE |
|
||
Biological Half-life | PHARMACOKINETIC |
|
MULTIPLE DOSES |
|
||
Tmax | PHARMACOKINETIC |
|
SINGLE DOSE |
|
||