Dolutegravir
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| Trade names | Tivicay |
| AHFS/Drugs.com | Multum Consumer Information |
| MedlinePlus | a613043 |
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Oral |
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| Bioavailability | n/a |
| Protein binding | ≥98.9% |
| Metabolism | UGT1A1 and CYP3A |
| Biological half-life | ~14 hours |
| Excretion | Feces (53%) and urine (18.9%) |
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| Formula | C20H19F2N3O5 |
| Molar mass | 419.38 g/mol |
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Dolutegravir (DTG) is an FDA-approved drug for the treatment of HIV infection. Dolutegravir is an integrase inhibitor. Known as S/GSK1349572 or just "572" the drug is marketed as Tivicay by GlaxoSmithKline (GSK). In February, 2013 the Food and Drug Administration announced that it would fast track dolutegravir's approval process. On August 13, 2013, dolutegravir was approved by the FDA. On November 4, 2013, dolutegravir was approved by Health Canada. On January 16, 2014, Tivicay was approved by the European Commission for use throughout the European Union.
Dolutegravir is approved for use in a broad population of HIV-infected patients. It can be used to treat HIV-infected adults who have never taken HIV therapy (treatment-naïve) and HIV-infected adults who have previously taken HIV therapy (treatment-experienced), including those who have been treated with other integrase strand transfer inhibitors. Tivicay is also approved for children ages 12 years and older weighing at least 40 kilograms (kg) who are treatment-naïve or treatment-experienced but have not previously taken other integrase strand transfer inhibitors.
Common side effects of dolutegravir in clinical trials included insomnia and headache. Serious side effects included allergic reactions and abnormal liver function in patients who were also infected with hepatitis B or C. The package insert warns against a mean rise in serum creatinine of 0.11 mg/dL due to inhibition of tubular secretion of creatinine and does not affect GFR.
Dolutegravir has been compared against both other integrase nuclear strand inhibitors as well as other classes of HIV anti-retrovirals.
SPRING-2 compared dolutegravir to another integrase inhibitor, raltegravir. Both were coformulated with a choice of TDF/FTC or ABC/3TC as a backbone. After 48 weeks of treatment 88% of those on dolutegravir had less than 50 copies of HIV per mL compared to 85% in the raltegravir group, thus demonstrating non-inferiority.
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