Bictegravir/emtricitabine/tenofovir alafenamide

What is Bictegravir/emtricitabine/tenofovir alafenamide?

Bictegravir/emtricitabine/tenofovir alafenamide (BIKTARVY) is a three-drug combination of bictegravir (BIC), a human immunodeficiency virus type 1 (HIV-1) integrase strand transfer inhibitor (INSTI), and emtricitabine (FTC) and tenofovir alafenamide (TAF), both HIV-1 nucleoside analog reverse transcriptase inhibitors (NRTIs) used without other HIV-1 medicines to treat human immunodeficiency virus-1 (HIV-1) infection.

Bictegravir

Emtricitabine

Tenofovir alafenamide

What are the uses of this medicine?

• This medicine is used without other HIV-1 medicines to treat human immunodeficiency virus-1 (HIV-1) infection in adults and children who weigh at least 55 pounds (25 kg).

How does this medicine work?

• BIKTARVY is a fixed dose combination of antiretroviral drugs bictegravir (BIC), emtricitabine (FTC), and tenofovir alafenamide (TAF).

Bictegravir

• BIC inhibits the strand transfer activity of HIV-1 integrase (integrase strand transfer inhibitor; INSTI), an HIV-1 encoded enzyme that is required for viral replication.
• Inhibition of integrase prevents the integration of linear HIV-1 DNA into host genomic DNA, blocking the formation of the HIV-1 provirus and propagation of the virus.

Emtricitabine

• FTC, a synthetic nucleoside analog of cytidine, is phosphorylated by cellular enzymes to form emtricitabine 5'-triphosphate.
• Emtricitabine 5'-triphosphate inhibits the activity of the HIV-1 reverse transcriptase by competing with the natural substrate deoxycytidine 5'-triphosphate and by being incorporated into nascent viral DNA which results in chain termination.
• Emtricitabine 5′-triphosphate is a weak inhibitor of mammalian DNA polymerases α, β, Ɛ, and mitochondrial DNA polymerase γ.

Tenofovir Alafenamide

• TAF is a phosphonamidate prodrug of tenofovir (2′-deoxyadenosine monophosphate analog).
• Plasma exposure to TAF allows for permeation into cells and then TAF is intracellularly converted to tenofovir through hydrolysis by cathepsin A. Tenofovir is subsequently phosphorylated by cellular kinases to the active metabolite tenofovir diphosphate.
• Tenofovir diphosphate inhibits HIV-1 replication through incorporation into viral DNA by the HIV reverse transcriptase, which results in DNA chain-termination.
• Tenofovir diphosphate is a weak inhibitor of mammalian DNA polymerases that include mitochondrial DNA polymerase γ and there is no evidence of toxicity to mitochondria in cell culture.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who take a medicine that contains:

• dofetilide
• rifampin

What drug interactions can this medicine cause?

• Because BIKTARVY is a complete regimen, coadministration with other antiretroviral medications for the treatment of HIV-1 infection is not recommended.
• Coadministration of BIKTARVY with drugs that are substrates of OCT2 and MATE1 (e.g., dofetilide) may increase their plasma concentrations.
• Coadministration with St. John's wort is not recommended.
• The use of BIKTARVY with a drug that is a strong inhibitor of CYP3A and also an inhibitor of UGT1A1 may significantly increase the plasma concentrations of BIC.
• Coadministration of BIKTARVY with drugs that reduce renal function(eg: acyclovir, cidofovir, ganciclovir, valacyclovir, valganciclovir, aminoglycosides (e.g., gentamicin), and high-dose or multiple NSAIDs) or compete for active tubular secretion may increase concentrations of FTC, tenofovir, and other renally eliminated drugs and this may increase the risk of adverse reactions.

Is this medicine FDA approved?

• It was approved for use in the United States in 2018.

How should this medicine be used?

• Prior to or when initiating BIKTARVY, test patients for hepatitis B virus infection.
• Prior to or when initiating BIKTARVY, and during treatment with BIKTARVY, assess serum creatinine, estimated creatinine clearance, urine glucose and urine protein in all patients as clinically appropriate. In patients with chronic kidney disease, also assess serum phosphorus.

Recommended Dosage

• BIKTARVY is a three-drug fixed dose combination product containing 50 mg of bictegravir (BIC), 200 mg of emtricitabine (FTC), and 25 mg of tenofovir alafenamide (TAF).
• The recommended dosage of BIKTARVY is one tablet taken orally once daily with or without food.

Renal impairment:

BIKTARVY is not recommended in patients with:

• severe renal impairment (estimated creatinine clearance of 15 to below 30 mL per minute); or
• end stage renal disease (ESRD; estimated creatine clearance below 15 mL per minute) who are not receiving chronic hemodialysis; or
• no antiretroviral treatment history and ESRD who are receiving chronic hemodialysis

Hepatic impairment:

• BIKTARVY is not recommended in patients with severe hepatic impairment.

Administration

• Take BIKTARVY exactly as your healthcare provider tells you to take it. BIKTARVY is taken by itself (not with other HIV-1 medicines) to treat HIV-1 infection.
• Take BIKTARVY 1 time each day with or without food.
• If you are on dialysis, take your daily dose of BIKTARVY following dialysis.
• Do not change your dose or stop taking BIKTARVY without first talking with your healthcare provider. Stay under a healthcare provider's care during treatment with BIKTARVY.
• If you take antacids that contain aluminum or magnesium, take BIKTARVY at least 2 hours before or 6 hours after you take these antacids.
• If you take supplements or antacids that contain iron or calcium, take BIKTARVY with food at the same time that you take these supplements or antacids.
• Do not miss a dose of BIKTARVY.
• If you take too much BIKTARVY, call your healthcare provider or go to the nearest hospital emergency room right away.
• When your BIKTARVY supply starts to run low, get more from your healthcare provider or pharmacy. This is very important because the amount of virus in your blood may increase if the medicine is stopped for even a short time. The virus may develop resistance to BIKTARVY and become harder to treat.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 50 mg of bictegravir (equivalent to 52.5 mg of bictegravir sodium), 200 mg of emtricitabine, and 25 mg of tenofovir alafenamide (equivalent to 28 mg of tenofovir alafenamide fumarate).

This medicine is available in fallowing brand namesː

• BIKTARVY

What side effects can this medication cause?

The most common side effects of this medicine include:

• diarrhea
• nausea
• headache

BIKTARVY may cause serious side effects, including:

• Changes in your immune system (Immune Reconstitution Syndrome)
• New or worse kidney problems, including kidney failure
• Too much lactic acid in your blood (lactic acidosis)
• Severe liver problems

What special precautions should I follow?

• Patients with HIV-1 should be tested for the presence of chronic hepatitis B virus (HBV) infection before or when initiating antiretroviral therapy.
• Immune reconstitution syndrome has been reported in patients treated with combination antiretroviral therapy. May necessitate further evaluation and treatment.
• Assess serum creatinine, estimated creatinine clearance, urine glucose and urine protein when initiating BIKTARVY and during therapy as clinically appropriate in all patients. Also assess serum phosphorus in patients with chronic kidney disease.
• Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogs, including emtricitabine, a component of BIKTARVY, and tenofovir DF, another prodrug of tenofovir, alone or in combination with other antiretrovirals. Discontinue treatment in patients who develop symptoms or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity.

What to do in case of emergency/overdose?

• No data are available on overdose of BIKTARVY in patients.

Management for overdosage:

• If overdose occurs, monitor the patient for evidence of toxicity.
• Treatment of overdose with BIKTARVY consists of general supportive measures including monitoring of vital signs as well as observation of the clinical status of the patient.
• Hemodialysis treatment removes approximately 30% of the FTC dose over a 3-hour dialysis period starting within 1.5 hours of FTC dosing (blood flow rate of 400 mL per minute and a dialysate flow rate of 600 mL per minute).
• It is not known whether FTC can be removed by peritoneal dialysis.
• Tenofovir is efficiently removed by hemodialysis with an extraction coefficient of approximately 54%.

Can this medicine be used in pregnancy?

• There are insufficient human data on the use of BIKTARVY during pregnancy to inform a drug-associated risk of birth defects and miscarriage.
• There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to BIKTARVY during pregnancy.
• Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263.

Can this medicine be used in children?

• The safety and effectiveness of BIKTARVY for the treatment of HIV-1 infection was established in pediatric patients with body weight greater than or equal to 25 kg.
• Safety and effectiveness of BIKTARVY in pediatric patients weighing less than 25 kg have not been established.

What are the active and inactive ingredients in this medicine?

• Active ingredients: bictegravir, emtricitabine, and tenofovir alafenamide.
• Inactive ingredients: croscarmellose sodium, magnesium stearate, and microcrystalline cellulose.

Who manufactures and distributes this medicine?

Manufactured and distributed by: Gilead Sciences, Inc. Foster City, CA 94404

• BIKTARVY is a trademark of Gilead Sciences, Inc., or its related companies. All other trademarks referenced herein are the property of their respective owners.

What should I know about storage and disposal of this medication?

• Store BIKTARVY bottle below 86 °F (30 °C).
• Keep the bottle tightly closed.
• Store BIKTARY blister pack at room temperature between 68 °F to 77 °F (20 °C to 25 °C).
• Keep BIKTARVY in its original bottle or blister pack.

• Dailymed label info on Bictegravir/emtricitabine/tenofovir alafenamide
• FDA Bictegravir/emtricitabine/tenofovir alafenamide

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