Facts About Tivicay (dolutegravir)

HIV Drug Moved to Preferred First-Line Option in U.S.

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Courtesy ViiV Healthcare Co.

Tivicay (dolutegravir) is an integrase inhibitor-class antiretroviral drug used in the treatment of HIV. It was the second in the class of integrase inhibitors to be approved by the U.S. Food and Drug Administration (FDA).

Tivicay was granted FDA licensing on August 12, 2013 for use in adults, as well as children aged 12 or older who weigh at least 88 lbs (40kg) and have not been previously treated with an integrase inhibitor.

(Tivicay is currently not approved for children under 12 although Phase III clinical trials are underway to assess its safety and efficacy in that age group.)

Tivicay is also a component of the once-daily, fixed dose combination drug, Triumeq, which includes the drugs abacavir and lamivudine. Triumeq was approved by the FDA on August 22, 2014.

Clinical Research Highlights

The VIKING-3 Study demonstrated that Tivicay was effective in 63% of adult patients with resistance to multiple classes of HIV drugs, including the integrase inhibitors Isentress (ratelgravir) and elvitegravir (found in the single pill, fixed dose combination drug, Stribild).

The SINGLE Study revealed that patients on Tivicay had a lower incidence of discontinuation due to adverse drug effects than Atripla (tenofovir + emtricitabine + efavirenz). After 48 weeks, 2% of subjects on the Tivicay-based regimen discontinued treatment versus 10% of those receiving Atripla.

Dosage

  • Adults: 50mg tablet, once daily
  • Adults with certain integrase inhibitor-associated resistance: 50mg tablet, twice daily
  • Children 12 and over (weighing 88 lbs/40kg or more): 50mg tablet, once daily

Additionally, for children who are co-administered Sustiva (efavirenz), Aptivus (tipranavir) + Norvir (ritonavir), Lexiva (fosamprenavir) + Norvir (ritonavir), or rifampin, the Tivicay dose is 50mg, twice daily.

It is not yet known if Tivicay is effective in children with integrase inhibitor-associated resistance.

Drug Administration:

Tivicay may be taken with or without food, and at any time of the day.

Common Side Effects:

The most commonly noted side effects (occurring in 2% or less of cases) are:

  • Insomnia
  • Headache
  • Dizziness
  • Nausea

Drug Interactions or Incompatibility

Tikosyn (dofetilide), used in the treatment of arrhythmia (irregular heartbeat), is contraindicated for use with Tivicay.

To avoid possible drug-drug interaction, advise your doctor is you are taking any of the following medications or supplements:

  • Antiretroviral medication: Sustiva (efavirenz), Intelence (etravirine), Viramun (nevirapine), as well as the combination of Lexiva (fosamprenavir) + Norvir (ritonavir), or Aptivus (tipranavir) + Norvir (ritonavir)
  • Anti-seizure medication: Trileptal (oxcarbazepine), Dilantin (phenytoin), Phenytek (phenytoin), Luminal (phenobarbital), or carbamazepine-based drugs such as Carbatrol, Equetro, Tegretol, Teril, or Epitol
  • Rifampin-based antibiotics: Rifadan, Rifater, Rifamate, Rimactane
  • Metformin-based diabetic medication: Fortamet, Glucophage, Glumetza, Riomet
  • St. John's Wort

Considerations

  • Patients who experience an allergic reaction after starting Tivicay should contact their doctor immediately. Treatment should be stopped and medical treatment sought if a rash is accompanied by fever, muscle or joint pains, blisters or sores, redness or swelling of the eyes, swelling of the face or mouth, or breathing problems. Patients who have previously experienced a hypersensitive reaction to Tivicay should not be re-challenged with the drug after resolution of symptoms.
  • Tivicay should be taken two hours before or six hours after taking aluminum- or magnesium-containing antacids or laxatives, iron supplements, calcium supplements, buffered medications, or Carafate (sucralfate) use in the treatment of duodenal ulcers.
  • Inform your doctor of any liver condition you may have before starting Tivicay. There may be an increased risk for liver problems in some, particularly for people with hepatitis B (HVB), hepatitis C (HCV), or a pre-existing liver dysfunction. Liver enzymes should be regularly monitored as part of a person's routine blood tests taking Tivicay.

Sources:

U.S. National Library of Medicine. "TIVICAY (dolutegravir sodium) tablet, film coated." Bethesda, Maryland; revised August 2013.

ViiV Healthcare. "ViiV Healthcare receives FDA approval for Triumeq." London, England; press release issued 22 August 2014.

Walmsley S.; Antela, A.; Clumeck, N.; et al. "Dolutegravir (DTG; S/GSK1349572) + abacavir/lamivudine once daily statistically superior to tenofovir/emtricitabine/efavirenz: 48-week results - SINGLE (ING114467)." 52nd Interscience Conference on Antimicrobial Agents and Chemotherapy. San Francisco; September 9-12, 2012; Abstract H-556b.

Nichols, G.; Grossberg, R.; Lazzarin, A.; et al. "Antiviral Activity of Dolutegravir in Subjects With Failure on an Integrase Inhibitor-Based Regimen: Week 24 Phase 3 Results From VIKING-3." 11th International Congress on Drug Therapy in HIV Infection (HIV11). Glasgow, Scotland; November 11-15, 2012; Abstract O232.

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