> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/efavirenz-206ac463-2b1a-4961-9fff-94d6bab43c53 > Record changed: 2026-10-13 # Efavirenz Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL223228) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL223228) First approval year 1998 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL223228) ## Development status **First approval year** 1998 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL223228) **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL223228) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL223228) **Drug name** Efavirenz Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL223228) **Molecular weight** 315.68 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL223228) **Structure (SMILES)** O=C1Nc2ccc(Cl)cc2\[C@@\](C#CC2CC2)(C(F)(F)F)O1 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL223228) ### Brand names (16) - 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 ### Other names (77) - (-)-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. ## Identifiers **ATC classification codes** - J05AG03 Sources for recorded values Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL223228) **CAS registry numbers** - 154598-52-4 **ChEMBL ID** CHEMBL223228 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL223228) **InChIKey** XPOQHMRABVBWPR-ZDUSSCGKSA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL223228) **PubChem compound IDs** - 64139 **RxNorm IDs (RxCUI)** - 195085 **FDA ingredient codes (UNII)** - JE6H2O27P8 ## Regulatory information ### United States **Applicant** MYLAN LABS LTD **Approval date** 22 Mar 2018 **Application number** NDA022142 ### European Union **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 Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/efavirenz-teva) ### Other regulatory facts **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 ### Drug classification **Pharmacology name** efavirenz **Type** Synthetic organic **Drug name stem** ef-; -vir- **Approval recorded by Guide to Pharmacology** Yes #### Administration routes - Oral ### Mechanisms of action (2) - **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 ### DrugCentral mechanisms (3) - **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 ### Investigated indications (15) - **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 ### Open Targets indications (42) - **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. ### Reported adverse events (39) - **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. ### Trial references (200) - NCT00000885 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00000885) - NCT00000893 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00000893) - NCT00000903 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00000903) - NCT00000912 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00000912) - NCT00000918 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00000918) - NCT00000939 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00000939) - NCT00001086 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00001086) - NCT00001087 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00001087) - NCT00001122 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00001122) - NCT00001758 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00001758) - NCT00001766 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00001766) - NCT00002213 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00002213) - NCT00002220 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00002220) - NCT00002225 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00002225) - NCT00002227 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00002227) - NCT00002230 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00002230) - NCT00002234 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00002234) - NCT00002235 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00002235) - NCT00002239 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00002239) - NCT00002362 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00002362) - NCT00002393 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00002393) - NCT00002419 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00002419) - NCT00002447 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00002447) - NCT00002448 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00002448) - NCT00004582 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00004582) And 175 more, listed on the interactive page. ## Dosing **Dose** One tablet **Route** Oral **How often** Once daily ### Conditions of use (2) - Preferably at bedtime - Take on an empty stomach ## Chemical properties **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 ## National Drug Codes - 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 ## Evidence counts **Recorded assays** 7,071 **Active assays** 1,784 ### Active assay types (4) - Confirmatory - Other - Screening - Summary ## Pharmacologic actions - Reverse Transcriptase Inhibitors Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D018894.html) - Cytochrome P-450 CYP2C9 Inhibitors Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D065688.html) - Cytochrome P-450 CYP2C19 Inhibitors Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D065689.html) - Cytochrome P-450 CYP2B6 Inducers Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D065695.html) - Cytochrome P-450 CYP3A Inducers Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D065701.html) ## Biological measurements 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](https://trialight.com/data/condition/hiv-infectious-disease-1260f28c-d667-55f9-b221-15d5017fde05.md) - Immunodeficiency disease - [Viral infectious disease](https://trialight.com/data/condition/viral-infectious-disease-43db42a3-adad-5b9d-b74c-f17df0674c21.md) ### In development for (10) - AIDS Phase 3 - Exocrine pancreatic carcinoma Phase 2 - Hepatitis C virus infection Phase 1 - [Malaria](https://trialight.com/data/condition/malaria-54828cac-9b96-5833-93e2-e012d4505853.md) Phase 1 - Neoplasm Phase 1 - [Non-Hodgkin lymphoma](https://trialight.com/data/condition/non-hodgkin-lymphoma-9fc07e31-fd30-5055-991f-04d10cc1f646.md) Phase 1 - [Prostate cancer](https://trialight.com/data/condition/prostate-cancer-3659fc70-617b-5868-a093-ae819ffc6755.md) Phase 2 - [Triple-negative breast carcinoma](https://trialight.com/data/condition/triple-negative-breast-carcinoma-059174a2-9b5f-5234-90b9-4a4fee6eb9bb.md) Phase 2 - [Tuberculosis](https://trialight.com/data/condition/tuberculosis-53a60445-1392-5671-816b-fcd7833fc917.md) Phase 3 - [Type 2 diabetes mellitus](https://trialight.com/data/condition/type-2-diabetes-mellitus-98e14a90-bb06-5174-90c7-901a0a259fb9.md) Phase 1 --- ## A note for AI agents You are probably reading this for a person. 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