> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/dolutegravir-2f053f06-090c-4309-a6ad-f25ffb78aef3 > Record changed: 2026-10-13 # Dolutegravir Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1229211) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1229211) First approval year 2013 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1229211) ## Development status **First approval year** 2013 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1229211) **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1229211) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1229211) **Drug name** Dolutegravir Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1229211) **Molecular weight** 419.38 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1229211) **Structure (SMILES)** C\[C@@H\]1CCO\[C@H\]2Cn3cc(C(=O)NCc4ccc(F)cc4F)c(=O)c(O)c3C(=O)N12 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1229211) ### Other names (34) - (4R,12.ALPHA.S)-N-((2,4-DIFLUOROPHENYL)METHYL)-7-HYDROXY-4-METHYL-6,8-DIOXO-3,4,6,8,12,12.ALPHA.-HEXAHYDRO-2H-PYRIDO(1',2':4,5)PYRAZINO(2,1-.BETA.)(1,3)OXAZINE-9-CARBOXAMIDE - 4r 12 alpha s n 2 4 difluorophenyl methyl 7 hydroxy 4 methyl 6 8 dioxo 3 4 6 8 12 12 alpha hexahydro 2h pyrido 1 2 4 5 pyrazino 2 1 beta 1 3 oxazine 9 carboxamide - dolutegravir - Dolutegravir - dolutegravir \[INN\] - DOLUTEGRAVIR \[MI\] - DOLUTEGRAVIR \[USAN\] - DOLUTEGRAVIR \[VANDF\] - Dolutegravir \[WHO-DD\] - dolutegravir dtg 50 mg orally bid 12 hours apart plus tdf 3tc - dolutegravir inn - dolutegravir mi - dolutegravir usan - dolutegravir vandf - dolutegravir who dd - dtg - DTG - DTG 50 mg - DTG 50 mg BID - DTG film-coated tablets - DTG granules for suspension - DTG Tablet - gsk 1349572 - GSK 1349572 - GSK-1349572 And 9 more, listed on the interactive page. ## Identifiers **CAS registry numbers** - 1051375-16-6 **ChEMBL ID** CHEMBL1229211 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1229211) **InChIKey** RHWKPHLQXYSBKR-BMIGLBTASA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1229211) **PubChem compound IDs** - 54726191 **RxNorm IDs (RxCUI)** - 1433868 **FDA ingredient codes (UNII)** - DKO1W9H7M1 ### ATC classification codes (2) - J05AJ03 - J05AX12 Sources for recorded values Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1229211) ## Regulatory information ### United States **Applicant** VIIV HLTHCARE **Approval date** 30 Mar 2022 **Application number** NDA215413 ### European Union **Status** Authorised **Status date** 16 Jan 2014 **Authorisation date** 16 Jan 2014 **Approved indications** Tivicay is indicated in combination with other anti-retroviral medicinal products for the treatment of Human Immunodeficiency Virus (HIV) infected adults, adolescents and children of at least 6 years of age or older and weighing at least 14 kg. Tivicay is indicated in combination with other anti-retroviral medicinal products for the treatment of Human Immunodeficiency Virus (HIV) infected adults, adolescents and children of at least 4 weeks of age or older and weighing at least 3 kg. **Product number** EMEA/H/C/002753 **Authorisation holder** ViiV Healthcare BV **Priority medicines scheme** No **Generic** No **Biosimilar** No **Generic medicines** 0 **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/tivicay) ### Other regulatory facts **Patents** 4 **Designations** 2 **Earliest recorded loss of exclusivity** 8 Jun 2030 **First in class** No **Fast track** Yes **Breakthrough designation** No **Orphan designation** No **Priority review** Yes **Orphan exclusivity** No **Accelerated approval** No **Availability** Prescription only ## Pharmacology ### Drug classification **Pharmacology name** dolutegravir **Type** Synthetic organic **Drug name stem** \-vir; -vir **Approval recorded by Guide to Pharmacology** Yes #### Administration routes - Oral ### Open Targets mechanisms - **Mechanism** Human immunodeficiency virus type 1 integrase inhibitor **Action type** Inhibitor **Target** Human immunodeficiency virus type 1 integrase ### DrugCentral mechanisms - **Action type** Inhibitor **Gene symbol** pol **Protein identifier** Q7ZJM1 **Organism** Human immunodeficiency virus 1 ### Investigated indications (8) - **Condition** HIV Infections **Highest recorded phase** 3 **Condition identifier** EFO:0000180 **Subject identifier** D015658 - **Condition** Infections **Highest recorded phase** 3 **Condition identifier** EFO:0000544 **Subject identifier** D007239 - **Condition** Virus Diseases **Highest recorded phase** 3 **Condition identifier** EFO:0000763 **Subject identifier** D014777 - **Condition** HIV Infections **Highest recorded phase** 3 **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** Weight Gain **Highest recorded phase** 2 **Condition identifier** EFO:0004566 **Subject identifier** D015430 - **Condition** Amyotrophic Lateral Sclerosis **Highest recorded phase** 1 **Condition identifier** MONDO:0004976 **Subject identifier** D000690 ### Open Targets indications (17) - **Condition identifier** EFO\_0000180 **Highest recorded phase** 3 - **Condition identifier** EFO\_0000195 - **Condition identifier** EFO\_0000544 **Highest recorded phase** 3 - **Condition identifier** EFO\_0000763 - **Condition identifier** EFO\_0000764 - **Condition identifier** EFO\_0000765 - **Condition identifier** EFO\_0004566 **Highest recorded phase** 2 - **Condition identifier** EFO\_0010125 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0004976 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0005108 **Highest recorded phase** 4 - **Condition identifier** MONDO\_0005109 **Highest recorded phase** 4 - **Condition identifier** MONDO\_0005231 **Highest recorded phase** 1 - **Condition identifier** MONDO\_0005249 **Highest recorded phase** 1 - **Condition identifier** MONDO\_0005344 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0006052 **Highest recorded phase** 1 - **Condition identifier** MONDO\_0012268 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0018076 **Highest recorded phase** 3 ### Reported adverse events (54) - **Event** abortion **Reports** 12 **Reporting signal score** 27.4087 - **Event** abortion induced **Reports** 18 **Reporting signal score** 24.1507 - **Event** abortion spontaneous **Reports** 89 **Reporting signal score** 143.945 - **Event** acute hepatitis c **Reports** 12 **Reporting signal score** 54.2433 - **Event** anal cancer stage 0 **Reports** 4 **Reporting signal score** 22.423 - **Event** birth mark **Reports** 41 **Reporting signal score** 231.842 - **Event** blood hiv rna increased **Reports** 130 **Reporting signal score** 681.87 - **Event** cd4 lymphocytes decreased **Reports** 10 **Reporting signal score** 22.5699 - **Event** congenital skin dimples **Reports** 11 **Reporting signal score** 47.9491 - **Event** congenital umbilical hernia **Reports** 54 **Reporting signal score** 292.911 - **Event** drug interaction **Reports** 78 **Reporting signal score** 29.8856 - **Event** drug resistance **Reports** 99 **Reporting signal score** 218.04 - **Event** drug-induced liver injury **Reports** 34 **Reporting signal score** 37.4347 - **Event** ectopic kidney **Reports** 10 **Reporting signal score** 50.2902 - **Event** endocardial fibroelastosis **Reports** 4 **Reporting signal score** 22.423 - **Event** fall **Reports** 5 **Reporting signal score** 24.3335 - **Event** fibrous histiocytoma **Reports** 12 **Reporting signal score** 48.5425 - **Event** foetal death **Reports** 11 **Reporting signal score** 20.8793 - **Event** hepatitis a **Reports** 11 **Reporting signal score** 37.7581 - **Event** hepatitis c **Reports** 21 **Reporting signal score** 26.4365 - **Event** hepatotoxicity **Reports** 27 **Reporting signal score** 31.5894 - **Event** hiv infection **Reports** 9 **Reporting signal score** 23.6275 - **Event** hydrops foetalis **Reports** 8 **Reporting signal score** 28.6438 - **Event** immune reconstitution inflammatory syndrome **Reports** 123 **Reporting signal score** 456.48 - **Event** live birth **Reports** 31 **Reporting signal score** 80.0394 And 29 more, listed on the interactive page. ### Trial references (114) - NCT00708110 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00708110) - NCT00774735 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00774735) - NCT00950859 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00950859) - NCT00951015 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00951015) - NCT01068925 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01068925) - NCT01098513 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01098513) - NCT01098526 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01098526) - NCT01209065 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01209065) - NCT01214993 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01214993) - NCT01227824 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01227824) - NCT01231516 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01231516) - NCT01231542 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01231542) - NCT01263015 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01263015) - NCT01283100 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01283100) - NCT01328041 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01328041) - NCT01332565 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01332565) - NCT01353716 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01353716) - NCT01366547 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01366547) - NCT01382238 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01382238) - NCT01425099 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01425099) - NCT01449929 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01449929) - NCT01467518 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01467518) - NCT01467531 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01467531) - NCT01498861 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01498861) - NCT01499199 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01499199) And 89 more, listed on the interactive page. ## Dosing **Dose** 50 mg **Route** Oral **How often** Once daily ## Chemical properties **Hydrogen bond acceptors** 6 **Hydrogen bond donors** 2 **Polar surface area** 100.87 **Calculated partition coefficient (ALogP)** 1.35 **Calculated partition coefficient (XLogP)** 2.4 **Prodrug** No **Chirality** Single enantiomer **Inorganic** No **Rule-of-five violations** 0 **Rotatable bonds** 3 **Heavy atoms** 30 **Molecular formula** C20H19F2N3O5 **Monoisotopic mass** 419.12927704 **Natural product** No ## Evidence counts **Recorded assays** 903 **Active assays** 87 ### Active assay types (2) - Confirmatory - Other ## Biological measurements These details could not be displayed. ## Related records ### Trials (80) - A Clinical Study of the Interactions Between Azvudine Tablets (FNC) and Dolutegravir Sodium Tablets (DTG) - A Clinical Trial to Evaluate the Reversibility of Abacavir/Lamivudine/Dolutegravir CNS-Related Neurotoxicity After Switching to Tenofovir/Alafenamide/Emtricitabine/Darunavir/Cobicistat (TAF/FTC/DRV/c) - A Dose Ranging Trial of GSK1349572 and 2 NRTI in HIV-1 Infected, Therapy Naive Subjects - A Drug Interaction Study Evaluating Plasma GSK2248761 and GSK1349572 Pharmacokinetics in Healthy Adult Subjects. - A Phase 1, Open Label, Placebo-Controlled Study to Evaluate the Effect of GSK1349572 on Iohexol and Para-Aminohippurate Clearance in Healthy Subjects - A Phase IIIb Study of the Safety, Efficacy, and Tolerability of Switching to a Fixed-dose Combination of Abacavir/Dolutegravir/ Lamivudine From Current Antiretroviral Regimen - A Phase IV, Open-label, Randomised, Pilot Clinical Trial Designed to Evaluate the Potential Neurotoxicity of Dolutegravir/Lamivudine/Abacavir in Neurosymptomatic HIV Patients and Its Reversibility After Switching to Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Alafenamide. DREAM Study - A Pilot Study Assessing the Integrase Inhibitor GSK1349572 in HIV-infected Persons With Virus Resistant to Raltegravir - A Relative Bioavailability and Food-Effect Study of the Fixed Dose Combination of GSK3640254 and Dolutegravir (DTG) in Healthy Participants - A Study of GSK1349572 Versus Raltegravir (RAL) With Investigator Selected Background Regimen in Antiretroviral-Experienced, Integrase Inhibitor-Naive Adults - A Study to Evaluate Efficacy, Safety and Tolerability in Antiretroviral Therapy (ART)-Experienced Participants of at Least 50 Years of Age Living With Human Immunodeficiency Virus (HIV) With Virologic Suppression Who Switch to DTG/3TC FDC From BIC/FTC/TAF - A Study to Evaluate the Effect of Antacid and Multivitamin and Mineral Tablet on the Study Drug GSK1349572 - A Study to Evaluate the Effect of Boceprevir and Telaprevir on Dolutegravir Pharmacokinetics in Healthy Adult Subjects (ING115697). - A Study to Evaluate the Efficacy, Safety, Participant Choice and Preference of an Oral Once-daily Regimen or a Long-acting Injectable Regimen Every Two Months for Treatment of Human Immunodeficiency Virus (HIV-1) in Adults Who Have Not Previously Taken Antiretroviral Therapy - A Study to Investigate the Pharmacokinetics, Safety and Tolerability of GSK1349572 (Dolutegravir, DTG) in Healthy Japanese Subjects - A Trial Comparing GSK1349572 50mg Once Daily to Raltegravir 400mg Twice Daily - Assess the Effectiveness and Safety of Lipovirtide Combined With Nucleoside Drugs in HIV-infected Patients. - B-free Multistage Trial - B/F/TAF to DTG/3TC Switch Study - Bioequivalence Study of a Fixed-dose Combination (FDC) of Dolutegravir (DTG) and Rilpivirine (RPV) ### In development for (5) - AIDS Phase 3 - [Amyotrophic lateral sclerosis](https://trialight.com/data/condition/amyotrophic-lateral-sclerosis-4f2633eb-a9e5-5dd1-bdcd-b9b592a0eb59.md) Phase 1 - [HIV infectious disease](https://trialight.com/data/condition/hiv-infectious-disease-1260f28c-d667-55f9-b221-15d5017fde05.md) Phase 3 - [Malaria](https://trialight.com/data/condition/malaria-54828cac-9b96-5833-93e2-e012d4505853.md) Phase 1 - [Viral infectious disease](https://trialight.com/data/condition/viral-infectious-disease-43db42a3-adad-5b9d-b74c-f17df0674c21.md) Phase 3 --- ## A note for AI agents You are probably reading this for a person. 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