Bictegravir – HIV Antiviral Therapy

Bictegravir is an innovative second-generation integrase strand transfer inhibitor (INSTI) with high antiviral potency and a high genetic barrier to resistance. The drug is a cornerstone component of modern HIV treatment regimens.

The mechanism of action of bictegravir involves blocking integrase, an enzyme required by HIV to incorporate its viral DNA into the host cell's (CD4+ T-lymphocyte) genetic material. The drug binds tightly to the active site of the integrase, making the integration process impossible and effectively stopping viral replication at an early stage. Due to its chemical structure, bictegravir remains effective even against virus strains that have developed resistance to first-generation integrase inhibitors.

The drug is characterized by excellent tolerability and a long half-life, allowing for once-daily dosing. It is typically administered as part of "three-in-one" combination tablets.

Wikipedia page
Bictegravir

Indications

Bictegravir is indicated for the treatment of HIV-1 infection in adults and pediatric patients weighing at least 14 kg:

  • Naive Patients: initial therapy for patients who have not previously received antiretroviral therapy (ART).
  • Stable Patients: as a replacement for current regimens in patients with achieved virologic suppression (HIV-1 RNA < 50 copies/mL) and no known resistance to integrase inhibitors.

Dosage and administration

Bictegravir dosing is standardized and generally does not require complex adjustment for most patients.

  • Standard Adult Dose: 50 mg once daily.
  • Administration Rules: the drug is taken orally, with or without food.
  • Missed Dose: if less than 18 hours have passed since the missed dose, it should be taken as soon as possible; if more than 18 hours, skip to the next scheduled dose.
  • Drug Interactions: should be taken at least 2 hours before or 6 hours after antacids or supplements containing magnesium, aluminum, iron, or calcium.

The use of bictegravir is contraindicated in the following cases:

  • Hypersensitivity: severe allergy to bictegravir or any excipients.
  • Drug Interactions: co-administration with rifampin or St. John's Wort (potent enzyme inducers), as this significantly reduces drug concentrations.
  • Co-administration with Dofetilide: risk of serious cardiac arrhythmias due to increased dofetilide levels.
  • Pediatric Use: not for use in children weighing less than 14 kg (due to lack of data).

Bictegravir is considered one of the safest agents, although the following reactions may occur:

  • Gastrointestinal: nausea, diarrhea, and occasionally abdominal pain.
  • Nervous System: headache, abnormal dreams, and in rare cases, dizziness.
  • Psychiatric: depression or anxiety (primarily in patients with a prior history).
  • Laboratory Parameters: small increases in serum creatinine (without affecting renal function) and creatine kinase (CK).
  • Metabolic: potential risk of weight gain associated with effective therapy.

Frequently Asked Questions

Bictegravir is a potent integrase strand transfer inhibitor (INSTI). It works by blocking the integrase enzyme, which the HIV virus uses to insert its genetic material into the DNA of healthy human cells. Without this step, the virus cannot complete its replication cycle, effectively halting the spread of the infection within the body.
Bictegravir has a high genetic barrier to resistance, meaning there is a lower risk of the virus developing resistance to the treatment. Additionally, it is highly effective at reducing viral load and is generally well-tolerated, causing fewer gastrointestinal and nervous system side effects compared to earlier generations of HIV drugs.
Bictegravir is typically taken once daily as part of a fixed-dose combination tablet. It can be taken with or without food. The most important factor for efficacy is maintaining a strict daily schedule, taking the medication at the same time every day to ensure stable levels of the drug in the bloodstream.
Bictegravir can bind with polyvalent cations, which reduces its absorption. Supplements containing magnesium or aluminum (antacids) should be taken at least 2 hours before or 2 hours after bictegravir. Iron or calcium supplements can be taken simultaneously with bictegravir only if taken with food.
Bictegravir can cause a slight increase in serum creatinine levels. This occurs because it inhibits a specific transport protein in the renal tubules rather than causing actual kidney damage. Nevertheless, physicians should monitor kidney function regularly before and during therapy.

List of medicines by active substance Bictegravir

-13%
Taffic 50 mg + 200 mg + 25 mg Hetero
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Hetero

Taffic

Bictegravir + Emtricitabine + Tenofovir Alafenamide
50 mg + 200 mg + 25 mg 30 tablets
3076₴ 3516₴
✅ All products loaded (1)

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