What is Bictegravir?

Bictegravir (INN; BIC, formerly known as GS-9883) is a second-generation integrase strand transfer inhibitor (INSTI) developed by Gilead Sciences. It was structurally derived from the earlier compound dolutegravir. Gilead presented in vitro and clinical data for bictegravir in the summer of 2016. By that time, bictegravir had entered Phase 3 clinical trials as part of a single-tablet regimen combined with tenofovir alafenamide (TAF) and emtricitabine (FTC) for the treatment of HIV-1 infection.

The combination drug bictegravir/emtricitabine/tenofovir alafenamide, marketed as Biktarvy, was approved for use in 2018 in Australia, the European Union, and the United States. It received approval in 2019 in New Zealand and the United Kingdom, and a generic version was approved by the Drugs Controller General of India the same year. As of 2024, Biktarvy is recommended as a first-line antiretroviral therapy in several countries, including the European Union, the United Kingdom, and the United States.

Medical Use

Bictegravir is used in a fixed-dose combination with tenofovir alafenamide and emtricitabine for the treatment of HIV-1 infection.


Bictegravir should not be used with dofetilide and rifampin. The use of dofetilide with bictegravir increases the concentration of dofetilide, potentially leading to life-threatening events. Concomitant use of bictegravir and rifampin is contraindicated due to significant drug interactions caused by rifampin’s effect on bictegravir. Bictegravir is primarily metabolized by the liver enzyme CYP3A4, so CYP3A4 inducers should be avoided.

Adverse Effects

The most common side effects of bictegravir include diarrhea, nausea, and headache.