Products
Bictegravir was approved in the United States and EU in 2018 and in many countries in 2019 in fixed combination with emtricitabine and tenofoviralafenamide in the form of film-coated tablets (Biktarvy).
Structure and properties
Bictegravir (C21H18F3N3O5, Mr = 449.4 g/mol) exists as a white to yellowish substance.
Effects
Bictegravir (ATC J05AR20) has antiviral properties. The effects are due to inhibition of HIV integrase. This enzyme is responsible for inserting viral DNA into the genome of human host cells. Inhibition results in inhibition of viral replication. Bictegravir has a long half-life of about 17 hours. Unlike other integrase inhibitors, bictegravir does not require a pharmacokinetic booster (cobicistat) and can be administered once daily.
Indications
For the treatment of patients with HIV-1 infection.
Dosage
According to the SmPC. Tablets are taken once daily, regardless of meals.
Contraindications
- Hypersensitivity
- Concurrent use with strong inducers of CYP3A as well as of UGT1A1, such as rifampicin or St. John’s wort
- Concurrent use with dofetilide.
For complete precautions, see the drug label.
Interactions
Bictegravir is a substrate of CYP3A and UGT1A1.
Adverse effects
The most common potential adverse effects include headache, diarrhea, and nausea. This information refers to the fixed combination with the two other active ingredients.
