Bictegravir

Bictegravir is an antiretroviral drug used in the treatment of HIV/AIDS. It is classified as an integrase strand transfer inhibitor (INSTI), which works by blocking the action of the HIV enzyme integrase. This enzyme is crucial for the viral replication process, as it integrates the viral DNA into the host cell's DNA. By inhibiting this enzyme, bictegravir prevents the virus from multiplying and reduces the amount of HIV in the body.

Mechanism of Action

Bictegravir inhibits the integrase enzyme by binding to the active site of the enzyme and blocking the strand transfer step of the integration process. This prevents the viral DNA from integrating into the host cell genome, which is a critical step in the HIV replication cycle. As a result, the virus is unable to replicate and produce new virions.

Pharmacokinetics

Bictegravir is known for its favorable pharmacokinetic profile. It has a long half-life, which allows for once-daily dosing. The drug is metabolized primarily by the liver enzyme CYP3A4 and by UGT1A1, a uridine diphosphate-glucuronosyltransferase enzyme. Bictegravir is also a substrate of the drug transporters P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP).

Clinical Use

Bictegravir is commonly used in combination with other antiretroviral agents. One of the most well-known fixed-dose combinations is Biktarvy, which includes bictegravir, emtricitabine, and tenofovir alafenamide. This combination is used as a complete regimen for the treatment of HIV-1 infection in adults and pediatric patients weighing at least 25 kg.

Side Effects

Common side effects of bictegravir include headache, nausea, and diarrhea. More serious side effects can include lactic acidosis, hepatomegaly with steatosis, and severe skin reactions. Patients are advised to report any unusual symptoms to their healthcare provider.

Drug Interactions

Bictegravir can interact with other medications that are metabolized by CYP3A4 and UGT1A1. It is important to review all medications with a healthcare provider to avoid potential drug interactions. Bictegravir should not be co-administered with rifampin, a potent CYP3A4 inducer, as it can significantly reduce the plasma concentrations of bictegravir.

History

Bictegravir was developed by Gilead Sciences and was approved by the U.S. Food and Drug Administration (FDA) in 2018 as part of the fixed-dose combination Biktarvy. It has since become a widely used option in the treatment of HIV due to its efficacy and favorable safety profile.

See Also

• HIV/AIDS
• Antiretroviral drug
• Integrase strand transfer inhibitor
• Biktarvy
• Gilead Sciences

References

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