Sustiva(efavirenz)
Atripla, Stocrin, Sustiva, Symfi (efavirenz) is a small molecule pharmaceutical. Efavirenz was first approved as Sustiva on 1998-09-17. It is used to treat acquired immunodeficiency syndrome and HIV infections in the USA. It has been approved in Europe to treat HIV infections. It is known to target cytochrome P450 3A4.
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BMS
Commercial
Therapeutic Areas
Therapeutic Area | MeSH |
|---|---|
| infections | D007239 |
| urogenital diseases | D000091642 |
| immune system diseases | D007154 |
Trade Name
FDA
EMA
Combinations
Atripla, Symfi, Symfi lo (generic drugs available since 2017-12-15)
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Efavirenz
Efavirenz
+
Emtricitabine
+
Tenofovir disoproxil fumarate
Tradename | Company | Number | Date | Products |
|---|---|---|---|---|
| ATRIPLA | Gilead Sciences | N-021937 RX | 2006-07-12 | 1 products, RLD, RS |
Labels
FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| atripla | New Drug Application | 2021-12-14 |
| efavirenz, emtricitabine and tenofovir disoproxil fumarate | ANDA | 2023-01-27 |
| sustiva | New Drug Application | 2020-11-20 |
| symfi | New Drug Application | 2019-10-15 |
Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
|---|---|---|---|
| acquired immunodeficiency syndrome | EFO_0000765 | D000163 | B20 |
| hiv infections | EFO_0000764 | D015658 | B20 |
Agency Specific
FDA
EMA
No data
Patent Expiration
Patent | Expires | Flag | FDA Information |
|---|---|---|---|
| Efavirenz / Emtricitabine / Tenofovir Disoproxil Fumarate, Atripla, Gilead Sciences | |||
| 8598185 | 2029-04-28 | DP | |
| 9018192 | 2026-06-13 | U-750, U-1170 | |
| 9545414 | 2026-06-13 | DP | U-750, U-1170 |
| 8592397 | 2024-01-13 | DP | U-750, U-1170 |
| 8716264 | 2024-01-13 | DP | U-257 |
| 9457036 | 2024-01-13 | DP | U-257 |
| 9744181 | 2024-01-13 | DP | U-257 |
ATC Codes
J: Antiinfectives for systemic use
— J05: Antivirals for systemic use
— J05A: Direct acting antivirals
— J05AG: Non-nucleoside reverse transcriptase inhibitors
— J05AG03: Efavirenz
— J05AR: Antivirals for treatment of hiv infections, combinations
— J05AR06: Emtricitabine, tenofovir disoproxil and efavirenz
— J05AR11: Lamivudine, tenofovir disoproxil and efavirenz
HCPCS
No data
Clinical
Clinical Trials
307 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Hiv infections | D015658 | EFO_0000764 | B20 | 21 | 47 | 62 | 47 | 35 | 205 |
| Hiv | D006678 | O98.7 | 8 | 5 | 4 | 12 | 6 | 34 | |
| Tuberculosis | D014376 | EFO_0000774 | A15-A19 | 4 | 5 | 6 | 4 | 3 | 21 |
| Acquired immunodeficiency syndrome | D000163 | EFO_0000765 | B20 | 1 | 4 | 5 | 5 | 3 | 17 |
| Healthy volunteers/patients | — | 10 | — | — | 4 | — | 14 | ||
| Hiv-1 | D015497 | — | 3 | 3 | 2 | — | 8 | ||
| Infections | D007239 | EFO_0000544 | 1 | 3 | 1 | 1 | — | 6 | |
| Drug interactions | D004347 | 3 | — | — | 1 | 1 | 5 | ||
| Hiv-2 | D015498 | — | — | 2 | 1 | 1 | 4 | ||
| Lipodystrophy | D008060 | E88.1 | 1 | 1 | — | 1 | — | 3 |
Show 9 more
Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Malaria | D008288 | EFO_0001068 | B54 | 3 | — | 2 | — | — | 5 |
| Breast feeding | D001942 | — | — | 1 | — | 1 | 2 | ||
| Pregnancy | D011247 | EFO_0002950 | Z33.1 | — | — | 1 | — | 1 | 2 |
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Hepatitis c | D006526 | B19.2 | 2 | 1 | — | — | 3 | 6 | |
| Contraception | D003267 | 1 | 2 | — | — | — | 3 | ||
| Drug-related side effects and adverse reactions | D064420 | T88.7 | 1 | 1 | — | — | 1 | 2 | |
| Parasitemia | D018512 | 1 | 1 | — | — | — | 1 | ||
| Pancreatic neoplasms | D010190 | EFO_0003860 | C25 | — | 1 | — | — | — | 1 |
| Prostatic neoplasms | D011471 | C61 | — | 1 | — | — | — | 1 | |
| Triple negative breast neoplasms | D064726 | — | 1 | — | — | — | 1 |
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Pharmacokinetics | D010599 | 4 | — | — | — | — | 4 | ||
| Neoplasms | D009369 | C80 | 2 | — | — | — | — | 2 | |
| Type 2 diabetes mellitus | D003924 | EFO_0001360 | E11 | 1 | — | — | — | — | 1 |
| Substance-related disorders | D019966 | EFO_0003890 | F13 | 1 | — | — | — | — | 1 |
| Alzheimer disease | D000544 | EFO_0000249 | F03 | 1 | — | — | — | — | 1 |
| Non-hodgkin lymphoma | D008228 | C85.9 | 1 | — | — | — | — | 1 | |
| Hyperlipidemias | D006949 | EFO_0003774 | E78.5 | 1 | — | — | — | — | 1 |
| Hepacivirus | D016174 | 1 | — | — | — | — | 1 | ||
| Hepatic insufficiency | D048550 | 1 | — | — | — | — | 1 | ||
| Hiv seronegativity | D018023 | 1 | — | — | — | — | 1 |
Show 1 more
Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Sleep wake disorders | D012893 | G47 | — | — | — | — | 2 | 2 | |
| Biological availability | D001682 | — | — | — | — | 1 | 1 | ||
| Contraception behavior | D003268 | — | — | — | — | 1 | 1 | ||
| Dyslipidemias | D050171 | HP_0003119 | — | — | — | — | 1 | 1 | |
| Sustained virologic response | D000072230 | — | — | — | — | 1 | 1 | ||
| Neurobehavioral manifestations | D019954 | EFO_0004364 | — | — | — | — | 1 | 1 | |
| Medication adherence | D055118 | EFO_0006344 | — | — | — | — | 1 | 1 | |
| Child behavior | D002652 | — | — | — | — | 1 | 1 | ||
| Cd4 lymphocyte count | D018791 | — | — | — | — | 1 | 1 | ||
| Meningeal tuberculosis | D014390 | A17.0 | — | — | — | — | 1 | 1 |
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | EFAVIRENZ |
| INN | efavirenz |
| Description | Efavirenz is 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection. It has a role as a HIV-1 reverse transcriptase inhibitor and an antiviral drug. It is a benzoxazine, an acetylenic compound, an organochlorine compound, an organofluorine compound and a member of cyclopropanes. |
| Classification | Small molecule |
| Drug class | Fc fusion protein; antivirals: non-nucleoside reverse transcriptase inhibitors; benzoxazinone derivatives |
| Image (chem structure or protein) | |
| Structure (InChI/SMILES or Protein Sequence) | O=C1Nc2ccc(Cl)cc2[C@@](C#CC2CC2)(C(F)(F)F)O1 |
Identifiers
| PDB | — |
| CAS-ID | 154598-52-4 |
| RxCUI | 195085 |
| ChEMBL ID | CHEMBL223228 |
| ChEBI ID | 119486 |
| PubChem CID | 64139 |
| DrugBank | DB00625 |
| UNII ID | JE6H2O27P8 (ChemIDplus, GSRS) |
Target
Agency Approved
No data
Alternate
CYP3A4
CYP3A4
Organism
Homo sapiens
Gene name
CYP3A4
Gene synonyms
CYP3A3
NCBI Gene ID
Protein name
cytochrome P450 3A4
Protein synonyms
1,4-cineole 2-exo-monooxygenase, 1,8-cineole 2-exo-monooxygenase, Albendazole monooxygenase (sulfoxide-forming), Albendazole sulfoxidase, Cholesterol 25-hydroxylase, CYPIIIA3, CYPIIIA4, Cytochrome P450 3A3, Cytochrome P450 HLp, Cytochrome P450 NF-25, cytochrome P450, family 3, subfamily A, polypeptide 4, cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 3, cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 4, Cytochrome P450-PCN1, glucocorticoid-inducible P450, Nifedipine oxidase, P450-III, steroid inducible, Quinine 3-monooxygenase, taurochenodeoxycholate 6-alpha-hydroxylase
Uniprot ID
Mouse ortholog
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Variants
Clinical Variant
Identifier | Target mutation | Effect | Evaluation | Status |
|---|---|---|---|---|
| VCV000029671 | CYP2B6, 516G>T, Gln172His | drug response | 2021-03-24 | 1A |
Financial
Atripla - Gilead Sciences
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Trends
PubMed Central
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Additional graphs summarizing 18,088 documents
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Safety
Black-box Warning
Black-box warning for: Atripla, Efavirenz, emtricitabine and tenofovir disoproxil fumarate, Symfi
Adverse Events
Top Adverse Reactions
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12,251 adverse events reported
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