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
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
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 |
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 Date1998 |
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 |
---|---|---|
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 |
|
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 |
|
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 |
|
Preliminary data of a prospective study on neuropsychiatric side effects after initiation of efavirenz. | 2001 Aug 1 |
|
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 |
|
Non-nucleoside reverse transcriptase inhibitor failure impairs HIV-RNA responses to efavirenz-containing salvage antiretroviral therapy. | 2001 Aug 17 |
|
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 |
|
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 |
|
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 |
|
Predictors of protease inhibitor-associated adverse events. | 2001 Jul |
|
The steady-state pharmacokinetics of efavirenz and nevirapine when used in combination in human immunodeficiency virus type 1-infected persons. | 2001 Jul 1 |
|
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 |
|
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 |
|
In vitro anti-HIV-1 synergy between non-nucleoside reverse transcriptase inhibitors nevirapine and efavirenz. | 2001 Jun |
|
Limits of deep salvage antiretroviral therapy with nelfinavir plus either efavirenz or nevirapine, in highly pre-treated patients with HIV disease. | 2001 Jun |
|
[Vertical trasmission of human immunodeficiency virus (HIV) and other sexually transmitted infections (STI)]. | 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 |
|
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 |
|
Efavirenz-induced acute eosinophilic hepatitis. | 2001 May |
|
Efavirenz-induced photoallergic dermatitis in HIV. | 2001 May 25 |
|
High-performance liquid chromatographic method for the determination of HIV-1 non-nucleoside reverse transcriptase inhibitor efavirenz in plasma of patients during highly active antiretroviral therapy. | 2001 May 5 |
|
[Apropos of atypical melancholia with Sustiva (efavirenz)]. | 2001 May-Jun |
|
[Drug interactions with antiretroviral agents]. | 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 |
|
The role of NNRTIs in antiretroviral combination therapy: an introduction. | 2001 Nov |
|
New developments in anti-HIV chemotherapy. | 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 |
|
Thiosugars. VIII. Preparation of new 4'-thio-L-lyxo pyrimidine nucleoside analogues. | 2001 Sep |
|
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 |
|
Efavirenz-induced psychosis. | 2001 Sep 28 |
|
Response to first protease inhibitor- and efavirenz-containing antiretroviral combination therapy. The Swiss HIV Cohort Study. | 2001 Sep 28 |
|
Structural mechanisms of drug resistance for mutations at codons 181 and 188 in HIV-1 reverse transcriptase and the improved resilience of second generation non-nucleoside inhibitors. | 2001 Sep 28 |
|
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. | 2001 Sep 3 |
|
Comparison of initial combination antiretroviral therapy with a single protease inhibitor, ritonavir and saquinavir, or efavirenz. | 2001 Sep 7 |
|
Switching from protease inhibitors to the non-nuke efavirenz. | 2001 Spring |
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 Dec 15 15:45:38 GMT 2023
by
admin
on
Fri Dec 15 15:45:38 GMT 2023
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Record UNII |
JE6H2O27P8
|
Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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NDF-RT |
N0000009948
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LIVERTOX |
NBK548521
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WHO-ATC |
J05AR11
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NDF-RT |
N0000175460
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EMA ASSESSMENT REPORTS |
SUSTIVA (AUTHORIZED: HIV INFECTIONS)
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EMA ASSESSMENT REPORTS |
ATRIPLA (AUTHORIZED: HIV INFECTIONS)
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NDF-RT |
N0000175463
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WHO-ESSENTIAL MEDICINES LIST |
6.4.2.3 (EFV/FTC/TEN)
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WHO-VATC |
QJ05AR11
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WHO-ATC |
J05AR06
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WHO-VATC |
QJ05AR06
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WHO-ESSENTIAL MEDICINES LIST |
6.4.2.2
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NCI_THESAURUS |
C97453
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WHO-VATC |
QJ05AG03
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WHO-ATC |
J05AG03
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EMA ASSESSMENT REPORTS |
STOCRIN (AUTHORIZED: HIV INFECTIONS)
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EMA ASSESSMENT REPORTS |
EFAVIRENZ TEVA (AUTHORIZED: HIV INFECTIONS)
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Code System | Code | Type | Description | ||
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N0000182140
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PRIMARY | Cytochrome P450 2C19 Inhibitors [MoA] | ||
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JE6H2O27P8
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PRIMARY | |||
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CHEMBL223228
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PRIMARY | |||
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DTXSID9046029
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PRIMARY | |||
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989
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PRIMARY | |||
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EFAVIRENZ
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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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1234103
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PRIMARY | |||
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195085
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PRIMARY | RxNorm | ||
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N0000182141
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PRIMARY | Cytochrome P450 3A4 Inhibitors [MoA] | ||
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Efavirenz
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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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119486
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PRIMARY | |||
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7718
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JE6H2O27P8
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PRIMARY | |||
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C29027
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PRIMARY | |||
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100000085266
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PRIMARY | |||
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EFAVIRENZ
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PRIMARY | |||
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II-77
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PRIMARY | |||
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N0000185504
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PRIMARY | Cytochrome P450 2C9 Inhibitors [MoA] | ||
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N0000187064
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PRIMARY | Cytochrome P450 2B6 Inducers [MoA] | ||
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154598-52-4
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PRIMARY | |||
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DB00625
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PRIMARY | |||
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N0000190118
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PRIMARY | Cytochrome P450 3A Inducers [MoA] | ||
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742403
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PRIMARY |
Related Record | Type | Details | ||
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METABOLIC ENZYME -> SUBSTRATE | |||
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TRANSPORTER -> INHIBITOR | |||
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BASIS OF STRENGTH->SUBSTANCE |
calculated on the anhydrous, solvent-free basis
ASSAY (HPLC)
USP
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TRANSPORTER -> INHIBITOR | |||
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TARGET ORGANISM->INHIBITOR |
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METABOLIC ENZYME -> SUBSTRATE |
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BINDER->LIGAND |
BINDING
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TARGET -> INHIBITOR |
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TRANSPORTER -> INHIBITOR |
Related Record | Type | Details | ||
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METABOLITE ACTIVE -> PARENT |
THE MAJOR OXIDATIVE METABOLITE OF EFAVIRENZ IN VIVO AND IN VITRO HUMAN LIVER MICROSOMAL PREPARATIONS IS 8-HYDROXYEFAVIRENZ
MAJOR
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METABOLITE -> PARENT |
7-HYDROXYEFAVIRENZ REPRESENTS A MINOR PATHWAY
MINOR
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Related Record | Type | Details | ||
---|---|---|---|---|
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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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 |
|
||
Biological Half-life | PHARMACOKINETIC |
|
SINGLE DOSE |
|
||
Biological Half-life | PHARMACOKINETIC |
|
MULTIPLE DOSES |
|
||
Tmax | PHARMACOKINETIC |
|
SINGLE DOSE |
|
||