BETHESDA, MD 13 August 2013—FDA and Viiv Healthcare on Monday announced the approval of dolutegravir, an integrase strand-transfer inhibitor, for use in combination antiretroviral regimens to treat HIV-1 infection in adults and children age 12 years or older who weigh at least 40 kg.
The FDA-approved labeling (PDF) for dolutegravir, or Tivicay, recommends a dosage of 50 mg once daily for patients in general.
For patients new to therapy with an integrase strand-transfer inhibitor and also taking efavirenz, fosamprenavir–ritonavir, tipranavir–ritonavir, or rifampin, the dosage of dolutegravir should be 50 mg twice daily.
This twice-daily dose is also recommended for adults—but not children—who previously used an integrase strand-transfer inhibitor and have an HIV integrase that is now resistant or may be resistant to this class of antiretroviral agent. There is no recommended dosage for children in this situation.
Therapy with dofetilide is a contraindication to the use of dolutegravir, the latter's labeling states. Dolutegravir can interfere with the organic-cation transporter responsible for the active secretion of dofetilide into the renal tubule, which may ultimately increase patients' risk for serious and life-threatening events.
The labeling states that dolutegravir can be taken without regard to meals but should be taken two hours before or six hours after consumption of cation-containing medications, such as sucralfate and oral calcium supplements.
A table in the labeling lists the known drug interactions with dolutegravir and other potentially important interactions and provides suggestions for management.
During the clinical studies of dolutegravir in adults, the most common moderate-to-severe adverse reactions were insomnia and headache.
Viiv Healthcare said Tivicay will be available in pharmacies in two weeks.
The product will be supplied in 30-count bottles of 50-mg tablets.
Viiv Healthcare was established in 2009 by GlaxoSmithKline plc and Pfizer Inc.