Drug information of Bictegravir

Bictegravir

Drug group:

Bictegravir is a recently approved investigational drug that has been used in trials studying the treatment of HIV-1 and HIV-2 infection. It has been approved for HIV-1 monotherapy combined with 2 other antiretrovirals in a single tablet.

Mechanism of effect

Bictegravir, an integrase inhibitor, inhibits HIV integrase by binding to the integrase-active site and blocking the strand transfer step of DNA integration.

Pharmacodynamic

 Bictegravir is an HIV-1 integrase strand transfer inhibitor (INSTI). Bictegravir (BIC) inhibits HIV-1 virus replication into the human genome. It can be taken once daily without additional dosing. Bictegravir (BIC) inhibits strand transfer of viral DNA into the host genome and thereby prevents HIV-1 replication

Pharmacokinetics

absorption:
Bictegravir is rapidly absorbed within the body. Tmax= 2.0-4.0h
volume of distribution: 0.2 L/Kg in humans
protein binding:  > 99 % bound to human plasma Blood to plasma ratio: 0.64
metabolism:
  In a 10-day dose-ranging study, monotherapy (5 mg to 100 mg) once daily in adults who were not previously treated with bictegravir, the median half-life of BIC ranged from 15.9 h - 20.9 h
route of elimination:
BIC is mainly eliminated through UGT1A1 glucuronidation and CYP3A4 oxidation, equally 2. About 1% of the bictegravir dose is excreted in the urine, unchanged [1218,1219].

Drug indications

in combination with emtricitabine and tenofovir alafenamide

Dosage

HIV-1 infection, treatment: One tablet (bictegravir 50 mg/emtricitabine 200 mg/tenofovir alafenamide 25 mg) once daily.

Drug contraindications

Coadministration with dofetilide, rifampin

Pregnancy level

Not assigned

It is not known if bictegravir crosses the placenta.

Breast feeding warning

excretion of bictegravir in milk is unknown.

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