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=CC=C(Cl)C=C12)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
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL378 |
4.0 nM [EC50] | ||
Target ID: CHEMBL612848 |
26.1 µM [IC50] | ||
Target ID: CHEMBL206 |
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 |
|---|---|---|---|---|
1.6 μM |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
EFAVIRENZ plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
9.1 μM |
1600 mg single, oral dose: 1600 mg route of administration: Oral experiment type: SINGLE co-administered: |
EFAVIRENZ plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
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 |
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 |
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 |
|
600 mg 1 times / day multiple, oral Recommended Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: |
unhealthy, 33 years |
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) Health Status: unhealthy Age Group: 33.9 months (range: 29.2–40.2 months) Sex: M+F 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 Health Status: unhealthy Age Group: 37.3 years Sex: M+F 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 Sources: |
unhealthy, 33 years |
| 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 Health Status: unhealthy Age Group: 37.3 years Sex: M+F 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 Health Status: unhealthy Age Group: 37.3 years Sex: M+F 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 Health Status: unhealthy Age Group: 37.3 years Sex: M+F 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 Health Status: unhealthy Age Group: 37.3 years Sex: M+F 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 Health Status: unhealthy Age Group: 37.3 years Sex: M+F 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 Health Status: unhealthy Age Group: 37.3 years Sex: M+F 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 Health Status: unhealthy Age Group: 37.3 years Sex: M+F Sources: |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| likely | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| yes [IC50 1 uM] | ||||
| yes [IC50 10 uM] | ||||
| yes [IC50 10 uM] | ||||
| yes [IC50 13 uM] | ||||
| yes [IC50 160 uM] | ||||
| yes [IC50 17 uM] | ||||
| yes [IC50 2.3 uM] | ||||
| yes [IC50 250 uM] | ||||
| yes [IC50 3.85 uM] | ||||
| yes [IC50 31.5 uM] | ||||
| yes [IC50 33.3 uM] | ||||
| yes [IC50 390 uM] | ||||
| yes [IC50 4.9 uM] | ||||
| yes [IC50 5.66 uM] | ||||
| yes [IC50 6 uM] | ||||
| yes [IC50 8.5 uM] | ||||
| yes [Ki 82 uM] | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | yes (co-administration study) Comment: Efavirenz decreased Raltegravir AUCinf by 14% and Cmax by 9%. |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| major | ||||
| major | ||||
| minor | ||||
| minor | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| yes [Km 22.7 uM] | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes |
PubMed
| Title | Date | PubMed |
|---|---|---|
| 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. | 2001-11-30 |
|
| Other issues: penetration into sanctuary sites, immune reconstitution and NNRTI sequencing. | 2001-11 |
|
| Factors affecting adherence and convenience in antiretroviral therapy. | 2001-11 |
|
| Comparison of NNRTIs in antiretroviral-experienced patients. | 2001-11 |
|
| Comparison of NNRTIs in antiretroviral-naïve patients. | 2001-11 |
|
| The role of NNRTIs in antiretroviral combination therapy: an introduction. | 2001-11 |
|
| New developments in anti-HIV chemotherapy. | 2001-11 |
|
| Protease-sparing regimen in a real-life practice with naïve patients: an equal opportunity approach? | 2001-10-09 |
|
| Efavirenz-induced psychosis. | 2001-09-28 |
|
| Response to first protease inhibitor- and efavirenz-containing antiretroviral combination therapy. The Swiss HIV Cohort Study. | 2001-09-28 |
|
| 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. | 2001-09-28 |
|
| Comparison of initial combination antiretroviral therapy with a single protease inhibitor, ritonavir and saquinavir, or efavirenz. | 2001-09-07 |
|
| Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. | 2001-09-03 |
|
| Thiosugars. VIII. Preparation of new 4'-thio-L-lyxo pyrimidine nucleoside analogues. | 2001-09 |
|
| 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. | 2001-09 |
|
| Solution structures and reactivities of the mixed aggregates derived from n-butyllithium and vicinal amino alkoxides. | 2001-08-22 |
|
| Non-nucleoside reverse transcriptase inhibitor failure impairs HIV-RNA responses to efavirenz-containing salvage antiretroviral therapy. | 2001-08-17 |
|
| 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. | 2001-08-15 |
|
| Antiretroviral therapy for previously treated patients. | 2001-08-09 |
|
| Nelfinavir, efavirenz, or both after the failure of nucleoside treatment of HIV infection. | 2001-08-09 |
|
| [Apropos of atypical melancholia with Sustiva (efavirenz)]. | 2001-08-08 |
|
| Eruptive cheilitis: a new adverse effect in reactive HIV-positive patients subjected to high activity antiretroviral therapy (HAART). Presentation of six clinical cases. | 2001-08-08 |
|
| Metformin in an HIV-infected patient with protease inhibitor-induced diabetic ketoacidosis. | 2001-08-04 |
|
| 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. | 2001-08-02 |
|
| Preliminary data of a prospective study on neuropsychiatric side effects after initiation of efavirenz. | 2001-08-01 |
|
| Antiretroviral rounds. When success is a pain. | 2001-08 |
|
| 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. | 2001-08 |
|
| Antiviral drugs: current state of the art. | 2001-08 |
|
| [Drug interactions with antiretroviral agents]. | 2001-07-31 |
|
| Gynecomastia without lipodystrophy syndrome in HIV-infected men treated with efavirenz. | 2001-07-27 |
|
| Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors. | 2001-07-23 |
|
| Manic syndrome associated with efavirenz overdose. | 2001-07-15 |
|
| Management of sudden psychiatric disorders related to efavirenz. | 2001-07-06 |
|
| The steady-state pharmacokinetics of efavirenz and nevirapine when used in combination in human immunodeficiency virus type 1-infected persons. | 2001-07-01 |
|
| Predictors of protease inhibitor-associated adverse events. | 2001-07 |
|
| Efavirenz plasma concentrations and efficiency. | 2001-06-15 |
|
| Phenotypic hypersusceptibility to non-nucleoside reverse transcriptase inhibitors in treatment-experienced HIV-infected patients: impact on virological response to efavirenz-based therapy. | 2001-06-15 |
|
| 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. | 2001-06-06 |
|
| In vitro anti-HIV-1 synergy between non-nucleoside reverse transcriptase inhibitors nevirapine and efavirenz. | 2001-06 |
|
| Limits of deep salvage antiretroviral therapy with nelfinavir plus either efavirenz or nevirapine, in highly pre-treated patients with HIV disease. | 2001-06 |
|
| [Vertical trasmission of human immunodeficiency virus (HIV) and other sexually transmitted infections (STI)]. | 2001-06 |
|
| Efavirenz-induced photoallergic dermatitis in HIV. | 2001-05-25 |
|
| 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. | 2001-05-05 |
|
| Efavirenz-induced acute eosinophilic hepatitis. | 2001-05 |
|
| High prevalence of genotypic and phenotypic HIV-1 drug-resistant strains among patients receiving antiretroviral therapy in Abidjan, Côte d'Ivoire. | 2001-04-15 |
|
| A pilot study of the use of mycophenolate mofetil as a component of therapy for multidrug-resistant HIV-1 infection. | 2001-04-15 |
|
| 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. | 2001-02-01 |
|
| Switching from protease inhibitors to the non-nuke efavirenz. | 2001 |
|
| 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 |
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
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:07:40 GMT 2025
by
admin
on
Mon Mar 31 18:07:40 GMT 2025
|
| Record UNII |
JE6H2O27P8
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Official Name | English | ||
|
Preferred Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
|
NDF-RT |
N0000009948
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
||
|
LIVERTOX |
NBK548521
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
||
|
WHO-ATC |
J05AR11
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
||
|
NDF-RT |
N0000175460
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
||
|
EMA ASSESSMENT REPORTS |
SUSTIVA (AUTHORIZED: HIV INFECTIONS)
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
||
|
EMA ASSESSMENT REPORTS |
ATRIPLA (AUTHORIZED: HIV INFECTIONS)
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
||
|
NDF-RT |
N0000175463
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
||
|
WHO-ESSENTIAL MEDICINES LIST |
6.4.2.3 (EFV/FTC/TEN)
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
||
|
WHO-VATC |
QJ05AR11
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
||
|
WHO-ATC |
J05AR06
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
||
|
WHO-VATC |
QJ05AR06
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
||
|
WHO-ESSENTIAL MEDICINES LIST |
6.4.2.2
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
||
|
NCI_THESAURUS |
C97453
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
||
|
WHO-VATC |
QJ05AG03
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
||
|
WHO-ATC |
J05AG03
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
||
|
EMA ASSESSMENT REPORTS |
STOCRIN (AUTHORIZED: HIV INFECTIONS)
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
||
|
EMA ASSESSMENT REPORTS |
EFAVIRENZ TEVA (AUTHORIZED: HIV INFECTIONS)
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
N0000182140
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | Cytochrome P450 2C19 Inhibitors [MoA] | ||
|
JE6H2O27P8
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
CHEMBL223228
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
DTXSID9046029
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
989
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
EFAVIRENZ
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
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. | ||
|
SUB06463MIG
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
64139
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
C098320
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
1234103
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
195085
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | RxNorm | ||
|
N0000182141
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | Cytochrome P450 3A4 Inhibitors [MoA] | ||
|
Efavirenz
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
m4839
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | Merck Index | ||
|
7163
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
119486
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
7718
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
JE6H2O27P8
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
C29027
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
100000085266
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
EFAVIRENZ
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
II-77
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
N0000185504
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | Cytochrome P450 2C9 Inhibitors [MoA] | ||
|
N0000187064
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | Cytochrome P450 2B6 Inducers [MoA] | ||
|
154598-52-4
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
DB00625
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | |||
|
N0000190118
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY | Cytochrome P450 3A Inducers [MoA] | ||
|
742403
Created by
admin on Mon Mar 31 18:07:40 GMT 2025 , Edited by admin on Mon Mar 31 18:07:40 GMT 2025
|
PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
TRANSPORTER -> INHIBITOR | |||
|
BASIS OF STRENGTH->SUBSTANCE |
calculated on the anhydrous, solvent-free basis
ASSAY (HPLC)
USP
|
||
|
|
TARGET ORGANISM->INHIBITOR |
|
||
|
METABOLIC ENZYME -> SUBSTRATE |
|
||
|
BINDER->LIGAND |
BINDING
|
||
|
METABOLIC ENZYME -> SUBSTRATE | |||
|
|
TARGET -> INHIBITOR |
|
||
|
TRANSPORTER -> 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 | |||
|
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 |
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 |
|
||
|
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 |
|
||