Efavirenz
Highest phase reached
Approved
Drug type
Small molecule
First approval year
1998
- First approval year
- 1998
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Efavirenz
- Molecular weight
- 315.68
- Structure (SMILES)
- O=C1Nc2ccc(Cl)cc2[C@@](C#CC2CC2)(C(F)(F)F)O1
- efavirenz
- Efavirenz
- efavirenz component of atripla
- Efavirenz component of atripla
- efavirenz component of symfi
- Efavirenz component of symfi
- efavirenz component of telura
- Efavirenz component of telura
- efavirenz teva
- Efavirenz teva
- stocrin
- Stocrin
- sustiva
- Sustiva
- sustiva 600
- Sustiva 600
- (-)-efavirenz
- 400mg sustiva
- 400mg Sustiva
- 600mg Sustiva
- atripla component efavirenz
- ATRIPLA COMPONENT EFAVIRENZ
- dmp 266
- DMP-266
- efavirenz
- Efavirenz
- efavirenz (drug)
- efavirenz (EFV)
- Efavirenz (EFV)
- EFAVIRENZ [EMA EPAR]
- EFAVIRENZ [HSDB]
- efavirenz [INN]
- EFAVIRENZ [JAN]
- EFAVIRENZ [MART.]
- EFAVIRENZ [MI]
- EFAVIRENZ [ORANGE BOOK]
- EFAVIRENZ [USAN]
- EFAVIRENZ [USP MONOGRAPH]
- EFAVIRENZ [USP-RS]
- EFAVIRENZ [VANDF]
- Efavirenz [WHO-DD]
And 52 more, listed on the interactive page.
- ATC classification codes
- J05AG03
Sources for recorded values
- CAS registry numbers
- 154598-52-4
- ChEMBL ID
- CHEMBL223228
- InChIKey
- XPOQHMRABVBWPR-ZDUSSCGKSA-N
- PubChem compound IDs
- 64139
- RxNorm IDs (RxCUI)
- 195085
- FDA ingredient codes (UNII)
- JE6H2O27P8
- Applicant
- MYLAN LABS LTD
- Approval date
- 22 Mar 2018
- Application number
- NDA022142
- Status
- Authorised
- Status date
- 9 Jan 2012
- Authorisation date
- 9 Jan 2012
- Approved indications
- Efavirenz is indicated in antiviral combination treatment of human-immunodeficiency-virus-1 (HIV-1)-infected adults, adolescents and children 3 years of age and older. Efavirenz has not been adequately studied in patients with advanced HIV disease, namely in patients with CD4 counts < 50 cells/mm3, or after failure of protease inhibitor (PI)-containing regimens. Although cross-resistance of efavirenz with protease inhibitors (PIs) has not been documented, there are at present insufficient data on the efficacy of subsequent use of PI-based combination therapy after failure of regimens containing efavirenz.
- Product number
- EMEA/H/C/002352
- Authorisation holder
- Teva B.V.
- Priority medicines scheme
- No
- Generic
- Yes
- Biosimilar
- No
- Generic medicines
- 1
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- HIV Infections
European medicines record
- Patents
- 0
- Designations
- 3
- First in class
- No
- Fast track
- Yes
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- Yes
- Availability
- Prescription only
- Pharmacology name
- efavirenz
- Type
- Synthetic organic
- Drug name stem
- ef-; -vir-
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- CYP3A4
- Gene symbol
- CYP3A4
- Protein identifier
- P08684
- Median affinity
- 4.76
- Affinity units
- pIC50
- Mechanism
- Human immunodeficiency virus type 1 reverse transcriptase inhibitor
- Action type
- Inhibitor
- Target
- Human immunodeficiency virus type 1 reverse transcriptase
- Protein identifier
- Q72547
Open Targets mechanisms
- Mechanism
- Human immunodeficiency virus type 1 reverse transcriptase inhibitor
- Action type
- Inhibitor
- Target
- Human immunodeficiency virus type 1 reverse transcriptase
- Action type
- Inhibitor
- Gene symbol
- gag-pol
- Protein identifier
- P03369
- Organism
- Human immunodeficiency virus type 1 group M subtype B (isolate ARV2/SF2)
- Action type
- Inhibitor
- Gene symbol
- CYP3A4
- Protein identifier
- P08684
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- pol
- Protein identifier
- Q72547
- Organism
- Human immunodeficiency virus 1
- Condition
- HIV Infections
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000180
- Subject identifier
- D015658
- Condition
- Infections
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000544
- Subject identifier
- D007239
- Condition
- Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Virus Diseases
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000763
- Subject identifier
- D014777
- Condition
- HIV Infections
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000764
- Subject identifier
- D015658
- Condition
- Acquired Immunodeficiency Syndrome
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000765
- Subject identifier
- D000163
- Condition
- Malaria
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001068
- Subject identifier
- D008288
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002618
- Subject identifier
- D010190
- Condition
- Hepatitis C
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003047
- Subject identifier
- D006526
- Condition
- Triple Negative Breast Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005537
- Subject identifier
- D064726
- Condition
- Lymphoma, Non-Hodgkin
- Highest recorded phase
- 1
- Condition identifier
- EFO:0005952
- Subject identifier
- D008228
- Condition
- Diabetes Mellitus, Type 2
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0005148
- Subject identifier
- D003924
- Condition
- Prostatic Neoplasms, Castration-Resistant
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0008315
- Subject identifier
- D064129
- Condition
- Tuberculosis
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0018076
- Subject identifier
- D014376
- Condition
- Autoimmune Diseases
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0021094
- Subject identifier
- D001327
- Condition identifier
- EFO_0000180
- Condition identifier
- EFO_0000180
- Highest recorded phase
- 4
- Condition identifier
- EFO_0000544
- Condition identifier
- EFO_0000544
- Highest recorded phase
- 4
- Condition identifier
- EFO_0000616
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000763
- Condition identifier
- EFO_0000764
- Condition identifier
- EFO_0000765
- Highest recorded phase
- 3
- Condition identifier
- EFO_0002618
- Highest recorded phase
- 2
- Condition identifier
- EFO_0005952
- Highest recorded phase
- 1
- Condition identifier
- EFO_0010125
- Highest recorded phase
- 3
- Condition identifier
- HP_0001939
- Highest recorded phase
- 2
- Condition identifier
- HP_0003124
- Highest recorded phase
- 2
- Condition identifier
- HP_0100806
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0002525
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0004975
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005055
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005070
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005108
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005109
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005136
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005148
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005186
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005231
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005249
- Highest recorded phase
- 3
And 17 more, listed on the interactive page.
- Event
- abortion induced
- Reports
- 110
- Reporting signal score
- 203.517
- Event
- abortion spontaneous
- Reports
- 250
- Reporting signal score
- 351.758
- Event
- birth mark
- Reports
- 29
- Reporting signal score
- 117.348
- Event
- blood hiv rna increased
- Reports
- 55
- Reporting signal score
- 171.197
- Event
- congenital umbilical hernia
- Reports
- 42
- Reporting signal score
- 164.196
- Event
- depression
- Reports
- 279
- Reporting signal score
- 151.681
- Event
- drug interaction
- Reports
- 315
- Reporting signal score
- 149.87
- Event
- drug resistance
- Reports
- 532
- Reporting signal score
- 1,395.16
- Event
- drug-induced liver injury
- Reports
- 115
- Reporting signal score
- 122.576
- Event
- eyelid ptosis
- Reports
- 64
- Reporting signal score
- 98.2611
- Event
- fatigue
- Reports
- 64
- Reporting signal score
- 122.492
- Event
- hiv infection
- Reports
- 44
- Reporting signal score
- 129.629
- Event
- hiv-associated neurocognitive disorder
- Reports
- 19
- Reporting signal score
- 85.5442
- Event
- human immunodeficiency virus transmission
- Reports
- 32
- Reporting signal score
- 136.591
- Event
- hyperlipidaemia
- Reports
- 83
- Reporting signal score
- 122.091
- Event
- immune reconstitution inflammatory syndrome
- Reports
- 207
- Reporting signal score
- 614.178
- Event
- immune reconstitution inflammatory syndrome associated tuberculosis
- Reports
- 24
- Reporting signal score
- 90.6357
- Event
- immune reconstitution syndrome
- Reports
- 137
- Reporting signal score
- 555.963
- Event
- injection site pain
- Reports
- 2
- Reporting signal score
- 88.9381
- Event
- kaposi's sarcoma
- Reports
- 55
- Reporting signal score
- 124.252
- Event
- lipoatrophy
- Reports
- 33
- Reporting signal score
- 104.086
- Event
- lipodystrophy acquired
- Reports
- 173
- Reporting signal score
- 650.981
- Event
- live birth
- Reports
- 55
- Reporting signal score
- 105.64
- Event
- mitochondrial toxicity
- Reports
- 68
- Reporting signal score
- 264.002
- Event
- nervous system disorder
- Reports
- 111
- Reporting signal score
- 170.356
And 14 more, listed on the interactive page.
- NCT00000885
- NCT00000893
- NCT00000903
- NCT00000912
- NCT00000918
- NCT00000939
- NCT00001086
- NCT00001087
- NCT00001122
- NCT00001758
- NCT00001766
- NCT00002213
- NCT00002220
- NCT00002225
- NCT00002227
- NCT00002230
- NCT00002234
- NCT00002235
- NCT00002239
- NCT00002362
- NCT00002393
- NCT00002419
- NCT00002447
- NCT00002448
- NCT00004582
And 175 more, listed on the interactive page.
- Dose
- One tablet
- Route
- Oral
- How often
- Once daily
- Preferably at bedtime
- Take on an empty stomach
- Hydrogen bond acceptors
- 2
- Hydrogen bond donors
- 1
- Polar surface area
- 38.33
- Calculated partition coefficient (ALogP)
- 4.07
- Calculated partition coefficient (XLogP)
- 4
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 0
- Heavy atoms
- 21
- Molecular formula
- C14H9ClF3NO2
- Monoisotopic mass
- 315.0273907
- Natural product
- No
- 0093-5234
- 31722-504
- 31722-736
- 33342-013
- 33342-138
- 42385-915
- 42385-928
- 42385-929
- 49502-475
- 65862-049
- 65862-104
- 65862-105
- 65862-106
- 65862-497
- 69097-210
- 69097-301
- 72865-172
- 72162-2565
- Recorded assays
- 7,071
- Active assays
- 1,784
- Confirmatory
- Other
- Screening
- Summary
- Reverse Transcriptase Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2B6 Inducers
- Cytochrome P-450 CYP3A Inducers
These details could not be displayed.
Related records
Trials (321)
- 2NN & CHARM Long-Term Follow-up Study
- A Clinical Trial Comparing the Efficacy of Tenofovir Disoproxil Fumarate/Emtricitabine/Rilpivirine (TDF/FTC/RPV) Versus TDF/FTC/Efavirenz (TDF/FTC/EFV) in Patients With Undetectable Plasma HIV-1 RNA on Current First-line Treatment
- A Clinical Trial Comparing the Tolerability of Etravirine to Efavirenz in Combination With 2 Nucleoside/Nucleotide Reverse Transcriptase Inhibitors in Treatment-naive HIV-1 Infected Patients
- A Comparison of BMS-232632 With Efavirenz, Each in Combination With Zidovudine-Lamivudine
- A Comparison of Emtricitabine and Abacavir Used in a Three-Drug Combination in HIV-Infected Patients Who Have Never Taken Anti-HIV Drugs
- A Comparison of Emtricitabine and Stavudine Used With Didanosine Plus Efavirenz in HIV-Infected Patients Who Have Not Taken Anti-HIV Drugs
- A Dose Ranging Trial of GSK1349572 and 2 NRTI in HIV-1 Infected, Therapy Naive Subjects
- A Dose-Ranging Study to Compare Doravirine (MK-1439) Plus TRUVADA® Versus Efavirenz Plus TRUVADA® in Human Immunodeficiency Virus (HIV)-1 Infected Participants (MK-1439-007)
- A Drug-Drug Interaction Study Between Fenofibric Acid and Efavirenz
- A Drug-drug Interaction Study of SHR6390 on Healthy Chinese Volunteers
- A Long Term Safety Study Of Lersivirine For The Treatment Of HIV-1 Infection In Subjects Who Have Completed Treatment With Lersivirine In Studies A5271015 And A5271022
- A New Tablet Containing Two FDA-Approved Drugs In HIV-Infected Patients Who Have Not Received Prior Therapy
- A Pharmacokinetic Evaluation of Levonorgestrel Implant and Antiretroviral Therapy
- A Pharmacokinetic Study of Once Daily Efavirenz 400 mg Versus 600 mg in Thai HIV-1 Infected Subjects
- A Phase I, Open-label Trial to Explore the Pharmacokinetics, Safety and Tolerability of TMC278 (Rilpivirine) 25 mg Once Daily Following a 2-week Period Receiving Efavirenz, in Healthy Male and Female Volunteers
- A Pilot Project of Virologic, Pharmacologic and Immunologic Correlates of Gastrointestinal-Associated Lymphoid Tissue Immune Reconstitution Following Maraviroc Therapy
- A Pilot Study of Atazanavir/Ritonavir/Efavirenz as a Nucleoside Sparing Regimen
- A Prospective Cohort of Children With HIV Infection
- A Randomized, Placebo-Controlled Study of the Safety and Efficacy of Efavirenz, Didanosine, and Stavudine in Combination With or Without Hydroxyurea in Antiretroviral Naive or Experienced HIV-Infected Patients
- A Simplified Kaletra® (Lopinavir/Ritonavir)-Based Therapy Versus a Sustiva® (Efavirenz)-Based Standard of Care in Previously Non-Treated HIV-Infected Subjects
Approved for (3)
- HIV infectious disease
- Immunodeficiency disease
- Viral infectious disease
In development for (10)
- AIDS Phase 3
- Exocrine pancreatic carcinoma Phase 2
- Hepatitis C virus infection Phase 1
- Malaria Phase 1
- Neoplasm Phase 1
- Non-Hodgkin lymphoma Phase 1
- Prostate cancer Phase 2
- Triple-negative breast carcinoma Phase 2
- Tuberculosis Phase 3
- Type 2 diabetes mellitus Phase 1