Dolutegravir

Dolutegravir is an HIV-1 antiretroviral agent [see Microbiology ( 12.4 )].

• TIVICAY and TIVICAY PD are indicated in combination with other antiretroviral agents for the treatment of HIV‑1 infection in adults (treatment-naïve or -experienced) and in pediatric patients (treatment-naïve or -experienced but integrase strand transfer inhibitor [INSTI]-naïve) aged at least 4 weeks and weighing at least 3 kg [see Microbiology ( 12.4 )]. TIVICAY is indicated in combination with rilpivirine as a complete regimen for the treatment of HIV-1 infection in adults to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA less than 50 copies/ mL) on a stable antiretroviral regimen for at least 6 months with no history of treatment failure or known substitutions associated with resistance to either antiretroviral agent.ICD-10: B20

• TIVICAY and TIVICAY PD are contraindicated in patients: with previous hypersensitivity reaction to dolutegravir [see Warnings and Precautions ( 5.1 )]. receiving dofetilide due to the potential for increased dofetilide plasma concentrations and the risk for serious and/or life-threatening events [see Drug Interactions ( 7 )] .contraindicated

May be taken without regard to food. ( 2.2 , 2.6) UGT = uridine diphosphate glucuronosyltransferase; CYP = cytochrome P450. a Rilpivirine dose is 25 mg once daily for those switching to dolutegravir plus rilpivirine. b Alternative combinations that do not include metabolic inducers should be considered where possible. Adult Population Recommended Dose Treatment-naïve or treatment-experienced INSTI-naïve or virologically suppressed (HIV-1 RNA <50 copies per mL) adults switching to dolutegravir plus rilpivirine a ( 2.1 ) 50 mg once daily Treatment-naïve or treatment-experienced INSTI-naïve when coadministered with certain UGT1A or CYP3A inducers ( 2.1 , 7.2 , 7.3 ) 50 mg twice daily INSTI-experienced with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance b ( 2.1 , 12.4 ) 50 mg twice daily Pediatric Patients: Treatment-naïve or treatment-experienced INSTI-naïve patients aged at least 4 weeks and weighing at least 3 kg. See Tables 2 , 3 , and 4 for complete pediatric dosing recommendations. ( 2.3 , 2.4 , 2.5 ). TIVICAY and TIVICAY PD are not bioequivalent and are not substitutable on a milligram-per-milligram basis. a If certain UGT1A or CYP3A inducers are coadministered, then adjust the weight-based dose of TIVICAY to twice daily.

Hypersensitivity reactions characterized by rash, constitutional findings, and sometimes organ dysfunction, including liver injury, have been reported. Discontinue TIVICAY or TIVICAY PD and other suspect agents immediately if signs or symptoms of hypersensitivity reactions develop, as a delay in stopping treatment may result in a life-threatening reaction. ( 5.1 ) Hepatotoxicity has been reported in patients receiving dolutegravir-containing regimens. Patients with underlying hepatitis B or C may be at increased risk for worsening or development of transaminase elevations. Monitoring for hepatotoxicity is recommended. ( 5.2 ) Immune reconstitution syndrome has been reported in patients treated with combination antiretroviral therapy. ( 5.4 ) TIVICAY tablets and TIVICAY PD tablets for oral suspension are not substitutable. ( 2.2 , 5.5 ) 5.1 Hypersensitivity Reactions Hypersensitivity reactions have been reported and were characterized by rash, constitutional findings, and sometimes organ dysfunction, including liver injury. The events were reported in less than 1% of subjects receiving TIVICAY in Phase III clinical trials. Discontinue TIVICAY or TIVICAY PD and other suspect agents immediately if signs or symptoms of hypersensitivity reactions develop (including, but not limited to, severe rash or rash accompanied by fever, general malaise, fatigue, muscle or joint aches, blisters or peeling of the skin, oral blisters or lesions, conjunctivitis, facial edema, hepatitis, eosinophilia, angioedema, difficulty breathing).

The following serious adverse drug reactions are discussed in other sections of the labeling: Hypersensitivity reactions [see Warnings and Precautions ( 5.1 )] . Hepatotoxicity [see Warnings and Precautions ( 5.2 )]. Immune Reconstitution Syndrome [see Warnings and Precautions ( 5.4 )] . The most common adverse reactions of moderate to severe intensity and incidence at least 2% (in those receiving TIVICAY in any one adult trial) are insomnia, fatigue, and headache. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact ViiV Healthcare at 1-877-844-8872 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice. Clinical Trials Experience in Adult Subjects Treatment-Naïve Subjects: The safety assessment of TIVICAY in HIV‑1–infected treatment-naïve subjects is based on the analyses of data from 2 international, multicenter, double-blind trials, SPRING-2 (ING113086) and SINGLE (ING114467) and data from the international, multicenter, open-label FLAMINGO (ING114915) trial.

8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in individuals exposed to TIVICAY or TIVICAY PD during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263. Risk Summary Data from two, ongoing birth outcome surveillance studies in Botswana and Eswatini which together include over 14,000 individuals evaluated during pregnancy show similar prevalence of neural tube defects among infants born to individuals taking dolutegravir at the time of conception compared to those born to individuals taking non-dolutegravir-containing regimens at conception or infants born to HIV-negative individuals. (see Data) . There are insufficient human data on the use of dolutegravir during pregnancy to definitively assess a drug-associated risk for birth defects and miscarriage. However, available human data from the APR do not indicate an increased risk of birth defects (see Data) . The background risk for major birth defects for the indicated population is unknown. In the U.S. general population, the estimated background rate for major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

Metabolism

The pharmacokinetic properties of dolutegravir have been evaluated in healthy adult subjects and HIV‑1–infected adult subjects. Exposure to dolutegravir was generally similar between healthy subjects and HIV‑1–infected subjects.

There is no known specific treatment for overdose with TIVICAY or TIVICAY PD. If overdose occurs, the patient should be monitored, and standard supportive treatment applied as required. As dolutegravir is highly bound to plasma proteins, it is unlikely that it will be significantly removed by dialysis.

• Aug 12, 2013NDANDA204790Viiv Hlthcare
• Aug 22, 2014NDANDA205551Viiv Hlthcare
• Nov 21, 2017NDANDA210192Viiv Hlthcare
• Apr 8, 2019NDANDA211994Viiv Hlthcare
• Jun 12, 2020NDANDA213983Viiv Hlthcare
• Mar 30, 2022NDANDA215413Viiv Hlthcare

1. 1Product Dose Omission Issue2,49613%
2. 2Pain2,27612%
3. 3Anxiety1,8889.8%
4. 4Emotional Distress1,7479.1%
5. 5Anhedonia1,5788.2%
6. 6Chronic Kidney Disease1,1606.0%
7. 7Fatigue1,0435.4%
8. 8Headache8894.6%
9. 9Renal Failure8364.3%
10. 10Rash7954.1%
11. 11Depression7864.1%
12. 12Exposure During Pregnancy7774.0%
13. 13Off Label Use7463.9%
14. 14Osteoporosis7363.8%
15. 15Product Use Issue7303.8%

Recent PubMed references pinned to Dolutegravir as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Brain Structure of South African Children Born to Mothers on Dolutegravir Versus Efavirenz-Based Antiretroviral Therapy.
  Journal of the Pediatric Infectious Diseases Society · 2026 · Bradford LE, Wedderburn CJ, Malaba TR, et al.
  PMID 41892690DOI 10.1093/jpids/piag022
• Weight Gain Among Children and Adolescents on Dolutegravir in Spain.
  Journal of the Pediatric Infectious Diseases Society · 2025 · Bravo-Queipo-de-Llano B, Prieto Tato LM, Noguera-Julian A, et al.
  PMID 41313249DOI 10.1093/jpids/piaf110
• Reduced Metformin Concentrations in Obese Women With Human Immunodeficiency Virus Treated With Dolutegravir.
  The Journal of infectious diseases · 2025 · van Rensburg R, Kellermann T, Pillay-Fuentes Lorente V, et al.
  PMID 40468972DOI 10.1093/infdis/jiaf305

The 10 most recently updated of 361 ClinicalTrials.gov registrations naming Dolutegravir as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study of Daily Rifapentine Combined With Isoniazid (1HP) for Tuberculosis Prevention in Children Less Than 13 Years of Age With and Without HIV
  Not yet recruiting · Phase 1 · Phase 2 · Interventional · 144 enrolled · National Institute of Allergy and Infectious Diseases (NIAID)
  NCT07124559updated 2026-06-12
• Early Metabolic Effects of Antiretroviral Drugs in Healthy volUnteers: a Phase 2 Randomized Study
  Recruiting · Phase 2 · Interventional · 120 enrolled · National Institute of Allergy and Infectious Diseases (NIAID)
  NCT05652478updated 2026-06-12
• A Study to Provide Continued Access to Study Drug to Children and Adolescents Who Have Completed Clinical Studies Involving Gilead HIV Treatments
  Recruiting · Phase 4 · Interventional · 350 enrolled · Gilead Sciences
  NCT06337032updated 2026-06-10
• Resistance Profile to Antiretroviral Medications in Individuals Living With HIV Who Failed a First-Line Regimen With Tenofovir / Lamivudina and Dolutegravir in Brasil
  Completed · Interventional · 777 enrolled · Federal University of São Paulo
  NCT07618507updated 2026-06-10
• Post-Injectable Cabotegravir Antiretroviral Salvage Strategy Options Trial
  Recruiting · Phase 4 · Interventional · 100 enrolled · University of Witwatersrand, South Africa
  NCT06485154updated 2026-06-09
• Reducing Antiretroviral Treatments
  Terminated · Phase 3 · Interventional · 360 enrolled · ANRS, Emerging Infectious Diseases
  NCT04051970updated 2026-06-08
• Dolutegravir Versus Dolutegravir in Combination With Tenofovir for the Treatment of HTLV-1 Infection
  Recruiting · Phase 2 · Interventional · 146 enrolled · Carlos Brites
  NCT07555431updated 2026-06-02
• HIV Drug Resistance Among Individuals Failing Tenofovir/Lamivudine and Dolutegravir First Line Regimen in Brazil
  Active not recruiting · Observational · 2,500 enrolled · Federal University of São Paulo
  NCT04453436updated 2026-06-01
• Multi Interventional Approaches to Mitigate HIV Reservoirs Aiming the Sustained HIV Remission Without Antiretrovirals
  Not yet recruiting · Phase 2 · Interventional · 70 enrolled · Federal University of São Paulo
  NCT06805656updated 2026-06-01
• Shortened Regimen for Drug-susceptible TB in Children
  Recruiting · Phase 3 · Interventional · 860 enrolled · Johns Hopkins University
  NCT06253715updated 2026-06-01

CPIC-curated drug–gene pairs for Dolutegravir. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

• UGT1A1CPIC B/C (provisional)FDA label: Informative PGx

Frequently asked questions

How does Dolutegravir work?

Dolutegravir is an HIV-1 antiretroviral agent [see Microbiology ( 12.4 )].

What is Dolutegravir used for?

According to FDA labeling, Dolutegravir carries indications including: TIVICAY and TIVICAY PD are indicated in combination with other antiretroviral agents for the treatment of HIV‑1 infection in adults (treatment-naïve or -experienced) and in pediatric patients (treatment-naïve or -experienced but integrase strand transfer inhibitor [INSTI]-naïve) aged at least 4 weeks and weighing at least 3 kg [see Microbiology ( 12.4 )]. TIVICAY is indicated in combination with rilpivirine as a complete regimen for the treatment of HIV-1 infection in adults to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA less than 50 copies/ mL) on a stable antiretroviral regimen for at least 6 months with no history of treatment failure or known substitutions associated with resistance to either antiretroviral agent.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Dolutegravir?

Dolutegravir is classified as Integrase inhibitors, Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor, HIV Integrase Inhibitors, Multidrug and Toxin Extrusion Transporter 1 Inhibitors, Organic Cation Transporter 2 Inhibitors, Decreased DNA Integrity.

What are the brand names for Dolutegravir?

Dolutegravir is marketed under brand names including Dovato, Juluca, Tivicay, Triumeq.

What are the contraindications for Dolutegravir?

Dolutegravir labeling lists contraindications including: TIVICAY and TIVICAY PD are contraindicated in patients: with previous hypersensitivity reaction to dolutegravir [see Warnings and Precautions ( 5.1 )]. receiving dofetilide due to the potential for increased dofetilide plasma concentrations and the risk for serious and/or life-threatening events [see Drug Interactions ( 7 )] .. Always consult the full prescribing information and a clinician.