bictegravir/emtricitabine/tenofovir AF (Rx)

Brand and Other Names:Biktarvy
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

bictegravir/emtricitabine/tenofovir AF

tablet

  • 50mg/200mg/25mg

Human Immunodeficiency Virus Infection

Indicated as complete regimen for antiretroviral therapy (ART)-naïve patients

Indicated to replace current ART regimen

  • In virologically suppressed patients (HIV-1 RNA <50 copies/mL) for ≥3 months
  • No history of treatment failure
  • No known substitutions associated with resistance to individual components

1 tablet PO qDay

Dosage Modifications

Hepatic impairment

  • Mild-to-moderate (Child-Pugh class A or B): No dosage adjustment necessary
  • Severe (Child-Pugh class C): Not studied; use not recommended

Renal impairment

  • CrCl ≥30 mL/min: No dosage adjustment necessary
  • Virologically suppressed adults with ESRD (CrCl <15 mL/min) on chronic hemodialysis: On hemodialysis days, administer daily dose after completing hemodialysis
  • Severe
    • Not recommended for
    • CrCl 15 to <30 mL/min
    • ESRD not on hemodialysis
    • No ART history and ESRD in patients who are receiving chronic hemodialysis

Dosing Considerations

Testing when initiating and during treatment

  • Before or when initiating therapy: Test patients for hepatitis B virus infection
  • Before or when initiating and during treatment: Assess serum creatinine, estimated CrCl, urine glucose, and urine protein in all patients as clinically appropriate; in patients with chronic kidney disease, also assess serum phosphorus

Dosage Forms & Strengths

bictegravir/emtricitabine/tenofovir AF

tablet

  • 30mg/120mg/15mg
  • 50mg/200mg/25mg

Human Immunodeficiency Virus Infection

Indicated as complete regimen for human immunodeficiency virus type 1 (HIV-1) in antiretroviral therapy (ART)-naïve adults and pediatric patients weighing ≥14 kg

Indicated to replace current ART regimen

  • In virologically suppressed patients (HIV-1 RNA <50 copies/mL) for ≥3 months
  • No history of treatment failure
  • No known substitutions associated with resistance to individual components

<14 kg: Safety and efficacy not established

≥14 to 25 kg: 1 tablet (30mg/120mg/15mg) PO qDay

≥25 kg: 1 tablet (50mg/200mg/25mg) PO qDay

Dosage Modifications

Hepatic impairment

  • Mild-to-moderate (Child-Pugh class A or B): No dosage adjustment necessary
  • Severe (Child-Pugh class C): Not studied; use not recommended

Renal impairment

  • CrCl ≥30 mL/min: No dosage adjustment necessary
  • Severe
    • Not recommended for
    • CrCl 15 to <30 mL/min
    • ESRD (CrCl <15 mL/min) with or without hemodialysis
    • No ART history and ESRD in patients who are receiving chronic hemodialysis

Dosing Considerations

Testing when initiating and during treatment

  • Before or when initiating therapy: Test patients patients for hepatitis B virus infection
  • Before or when initiating and during treatment: Assess serum creatinine, estimated CrCl, urine glucose, and urine protein in all patients as clinically appropriate; in patients with chronic kidney disease, also assess serum phosphorus
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Interactions

Interaction Checker

and bictegravir/emtricitabine/tenofovir AF

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    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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            Contraindicated (4)

            • dofetilide

              bictegravir will increase the level or effect of dofetilide by decreasing renal clearance. Contraindicated. Bictegravir inhibits organic cation transporter 2 (OCT2) and multidrug and toxin extrusion transporter 1 (MATE1) in vitro. Coadministration with OCT2 and MATE1 substrates may increase their plasma concentrations.

            • elvitegravir/cobicistat/emtricitabine/tenofovir DF

              emtricitabine, elvitegravir/cobicistat/emtricitabine/tenofovir DF. Other (see comment). Contraindicated. Comment: Elvitegravir/cobicistat/emtricitabine/tenofovir is a complete regimen for HIV and should not be administered with other antiretrovirals.

            • lamivudine

              emtricitabine and lamivudine both increase risk of immune reconstitution syndrome. Contraindicated. Coadministration of emtricitabine containing products and lamivudine containing products should be avoided. Combination will result in therapeutic duplication.

              emtricitabine, lamivudine. Other (see comment). Contraindicated. Comment: Coadministration of emtricitabine containing products and lamivudine containing products should be avoided. Combination will result in therapeutic duplication.

            • rifampin

              rifampin will decrease the level or effect of bictegravir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration of strong CYP3A and UGT1A1 inducers can substantially decrease bictegravir plasma concentrations. This may result in the loss of therapeutic effect and development of resistance to bictegravir. Coadministration with rifampin is contraindicated.

            Serious - Use Alternative (7)

            • betibeglogene autotemcel

              bictegravir, betibeglogene autotemcel. Other (see comment). Avoid or Use Alternate Drug. Comment: Do not take antiretroviral medications for at least 1 month before mobilization or expected duration for elimination of the medications, and until all cycles of apheresis are completed. Antiretroviral medications may interfere with manufacturing of apheresed cells.

              emtricitabine, betibeglogene autotemcel. Other (see comment). Avoid or Use Alternate Drug. Comment: Do not take antiretroviral medications for at least 1 month before mobilization or expected duration for elimination of the medications, and until all cycles of apheresis are completed. Antiretroviral medications may interfere with manufacturing of apheresed cells.

            • cabotegravir

              emtricitabine, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

              bictegravir, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • carbamazepine

              carbamazepine will decrease the level or effect of bictegravir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of strong CYP3A and UGT1A1 inducers can substantially decrease bictegravir plasma concentrations. This may result in the loss of therapeutic effect and development of resistance to bictegravir. Coadministration with another anticonvulsant should be considered.

            • elivaldogene autotemcel

              elivaldogene autotemcel, emtricitabine. Either decreases effects of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Patients should not take antiretroviral medications for at least 1 month before initiating medications for stem cell mobilization, for the duration of the medications? elimination, and until all cycles of apheresis are completed.

            • elivaldogene autotemcel

              elivaldogene autotemcel, bictegravir. Either decreases effects of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Patients should not take antiretroviral medications for at least 1 month before initiating medications for stem cell mobilization, for the duration of the medications? elimination, and until all cycles of apheresis are completed.

            • letermovir

              tenofovir AF will decrease the level or effect of letermovir by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Coadministration of letermovir with P-gp inducers is not recommended.

            • oxcarbazepine

              oxcarbazepine will decrease the level or effect of bictegravir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of strong CYP3A and UGT1A1 inducers can substantially decrease bictegravir plasma concentrations. This may result in the loss of therapeutic effect and development of resistance to bictegravir. Coadministration with another anticonvulsant should be considered.

            Monitor Closely (88)

            • abacavir

              abacavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • acalabrutinib

              acalabrutinib increases levels of tenofovir AF by Other (see comment). Use Caution/Monitor. Comment: Acalabrutinib may increase exposure to coadministered BCRP substrates by inhibition of intestinal BCRP.

            • acyclovir

              acyclovir increases levels of emtricitabine by Other (see comment). Use Caution/Monitor. Comment: Coadministration of emtricitabine with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of emtricitabine.

            • adefovir

              adefovir increases levels of emtricitabine by Other (see comment). Use Caution/Monitor. Comment: Coadministration of emtricitabine with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of emtricitabine.

            • aluminum hydroxide

              aluminum hydroxide will decrease the level or effect of bictegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Bictegravir can be taken under fasting conditions 2 hr before antacids containing Al, Mg, or Ca. Routine administration of bictegravir simultaneously with, or 2 hr after, antacids containing Al, Mg, or Ca is not recommended.

            • aluminum hydroxide/magnesium carbonate

              aluminum hydroxide/magnesium carbonate will decrease the level or effect of bictegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Bictegravir can be taken under fasting conditions 2 hr before antacids containing Al, Mg, or Ca. Routine administration of bictegravir simultaneously with, or 2 hr after, antacids containing Al, Mg, or Ca is not recommended.

            • apalutamide

              apalutamide will decrease the level or effect of tenofovir AF by increasing elimination. Use Caution/Monitor. Apalutamide weakly induces BCRP and may decrease systemic exposure of drugs that are BCRP substrates.

            • atazanavir

              atazanavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • berotralstat

              berotralstat will increase the level or effect of tenofovir AF by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor or titrate P-gp substrate dose if coadministered.

            • cabozantinib

              tenofovir AF will increase the level or effect of cabozantinib by Other (see comment). Use Caution/Monitor. MRP2 inhibitors increase cabozantinib toxicity

            • calcium acetate

              calcium acetate will decrease the level or effect of bictegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Bictegravir can be taken under fasting conditions 2 hr before antacids containing Al, Mg, or Ca. Routine administration of bictegravir simultaneously with, or 2 hr after, antacids containing Al, Mg, or Ca is not recommended.

            • calcium carbonate

              calcium carbonate will decrease the level or effect of bictegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Bictegravir can be taken under fasting conditions 2 hr before antacids containing calcium. However, bictegravir and supplements containing calcium can be taken together with food. Routine administration of bictegravir (under fasting conditions) simultaneously with, or 2 hr after, calcium supplements or antacids containing calcium is not recommended.

            • calcium citrate

              calcium citrate will decrease the level or effect of bictegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Bictegravir can be taken under fasting conditions 2 hr before antacids containing Al, Mg, or Ca. Routine administration of bictegravir simultaneously with, or 2 hr after, antacids containing Al, Mg, or Ca is not recommended.

            • celecoxib

              emtricitabine, celecoxib. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • cidofovir

              cidofovir increases levels of emtricitabine by Other (see comment). Use Caution/Monitor. Comment: Coadministration of emtricitabine with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of emtricitabine.

            • darolutamide

              darolutamide will increase the level or effect of tenofovir AF by Other (see comment). Modify Therapy/Monitor Closely. Darolutamide is a BCRP inhibitor. Avoid coadministration with BCRP inhibitors. If use is unavoidable, closely monitor for adverse reactions and consider dose reduction of BCRP substrate drug (refer BCRP substrate prescribing information).

            • diclofenac

              emtricitabine, diclofenac. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • diflunisal

              emtricitabine, diflunisal. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • duvelisib

              tenofovir AF will decrease the level or effect of duvelisib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • efavirenz

              efavirenz and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • elagolix

              elagolix will increase the level or effect of tenofovir AF by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • encorafenib

              encorafenib will increase the level or effect of tenofovir AF by Other (see comment). Modify Therapy/Monitor Closely. Encorafenib (a BCRP inhibitor) may increase the concentration and toxicities of BCRP substrates. Closely monitor for signs and symptoms of increased exposure and consider adjusting the dose of these substrates.

            • enfuvirtide

              emtricitabine and enfuvirtide both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • etodolac

              emtricitabine, etodolac. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • fenoprofen

              emtricitabine, fenoprofen. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • ferric maltol

              ferric maltol will decrease the level or effect of bictegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Bictegravir and supplements containing iron can be taken together with food. Routine administration of bictegravir (under fasting conditions) simultaneously with, or 2 hr after, supplements containing iron is not recommended.

            • ferrous fumarate

              ferrous fumarate will decrease the level or effect of bictegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Bictegravir and supplements containing iron can be taken together with food. Routine administration of bictegravir (under fasting conditions) simultaneously with, or 2 hr after, supplements containing iron is not recommended.

            • ferrous gluconate

              ferrous gluconate will decrease the level or effect of bictegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Bictegravir and supplements containing iron can be taken together with food. Routine administration of bictegravir (under fasting conditions) simultaneously with, or 2 hr after, supplements containing iron is not recommended.

            • ferrous sulfate

              ferrous sulfate will decrease the level or effect of bictegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Bictegravir and supplements containing iron can be taken together with food. Routine administration of bictegravir (under fasting conditions) simultaneously with, or 2 hr after, supplements containing iron is not recommended.

            • flurbiprofen

              emtricitabine, flurbiprofen. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • fosamprenavir

              fosamprenavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • fostamatinib

              fostamatinib will increase the level or effect of tenofovir AF by decreasing metabolism. Use Caution/Monitor. Concomitant use of fostamatinib may increase concentrations of BCRP substrate drugs. Monitor for toxicities of BCRP substrate drug that may require dosage reduction when given concurrently with fostamatinib.

            • ganciclovir

              ganciclovir, emtricitabine. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Use alternatives if available. Increased risk of hematologic toxicity.

              ganciclovir increases levels of emtricitabine by Other (see comment). Use Caution/Monitor. Comment: Coadministration of emtricitabine with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of emtricitabine.

            • glecaprevir/pibrentasvir

              glecaprevir/pibrentasvir will increase the level or effect of tenofovir AF by decreasing metabolism. Use Caution/Monitor. Glecaprevir/pibrentasvir may increase plasma concentration of BCRP substrates.

            • ibuprofen

              emtricitabine, ibuprofen. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • ibuprofen IV

              emtricitabine, ibuprofen IV. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • ifosfamide

              ifosfamide, tenofovir AF. Either increases toxicity of the other by nephrotoxicity and/or ototoxicity. Modify Therapy/Monitor Closely. Monitor electrolytes and renal function.

            • indinavir

              indinavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • indomethacin

              emtricitabine, indomethacin. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • istradefylline

              istradefylline will increase the level or effect of tenofovir AF by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of P-gp substrates in clinical trials. Consider dose reduction of sensitive P-gp substrates.

            • ketoprofen

              emtricitabine, ketoprofen. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • ketorolac

              emtricitabine, ketorolac. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • lonafarnib

              lonafarnib will increase the level or effect of tenofovir AF by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Lonafarnib is a weak P-gp inhibitor. Monitor for adverse reactions if coadministered with P-gp substrates where minimal concentration changes may lead to serious or life-threatening toxicities. Reduce P-gp substrate dose if needed.

            • magnesium citrate

              magnesium citrate will decrease the level or effect of bictegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Bictegravir can be taken under fasting conditions 2 hr before antacids containing Al, Mg, or Ca. Routine administration of bictegravir simultaneously with, or 2 hr after, antacids containing Al, Mg, or Ca is not recommended.

            • magnesium gluconate

              magnesium gluconate will decrease the level or effect of bictegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Bictegravir can be taken under fasting conditions 2 hr before antacids containing Al, Mg, or Ca. Routine administration of bictegravir simultaneously with, or 2 hr after, antacids containing Al, Mg, or Ca is not recommended.

            • magnesium hydroxide

              magnesium hydroxide will decrease the level or effect of bictegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Bictegravir can be taken under fasting conditions 2 hr before antacids containing Al, Mg, or Ca. Routine administration of bictegravir simultaneously with, or 2 hr after, antacids containing Al, Mg, or Ca is not recommended.

            • magnesium oxide

              magnesium oxide will decrease the level or effect of bictegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Bictegravir can be taken under fasting conditions 2 hr before antacids containing Al, Mg, or Ca. Routine administration of bictegravir simultaneously with, or 2 hr after, antacids containing Al, Mg, or Ca is not recommended.

            • magnesium supplement

              magnesium supplement will decrease the level or effect of bictegravir by Other (see comment). Modify Therapy/Monitor Closely. Drug may form a chelate with polyvalent cations; may decrease absorption by the intestinal tract; applies to oral forms; may administer under fasting conditions 2 hr before administering polyvalent cation or 6 hr after

            • meclofenamate

              emtricitabine, meclofenamate. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • mefenamic acid

              emtricitabine, mefenamic acid. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • meloxicam

              emtricitabine, meloxicam. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • metformin

              bictegravir will increase the level or effect of metformin by decreasing renal clearance. Modify Therapy/Monitor Closely. Bictegravir inhibits organic cation transporter 2 (OCT2) and multidrug and toxin extrusion transporter 1 (MATE1) in vitro. Coadministration with OCT2 and MATE1 substrates may increase their plasma concentrations. Metformin dose reduction may be required.

            • multivitamins

              multivitamins will decrease the level or effect of bictegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Bictegravir and supplements containing iron can be taken together with food. Routine administration of bictegravir (under fasting conditions) simultaneously with, or 2 hr after, supplements containing iron is not recommended.

            • multivitamins, vision

              multivitamins, vision will decrease the level or effect of bictegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Bictegravir and supplements containing iron can be taken together with food. Routine administration of bictegravir (under fasting conditions) simultaneously with, or 2 hr after, supplements containing iron is not recommended.

            • nabumetone

              emtricitabine, nabumetone. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • naproxen

              emtricitabine, naproxen. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • nelfinavir

              nelfinavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • nevirapine

              emtricitabine and nevirapine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • nirmatrelvir

              nirmatrelvir will increase the level or effect of bictegravir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration may increase bictegravir systemic exposures.

              nirmatrelvir will increase the level or effect of tenofovir AF by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration may increase tenofovir systemic exposures.

            • nirmatrelvir/ritonavir

              nirmatrelvir/ritonavir will increase the level or effect of tenofovir AF by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration may increase tenofovir systemic exposures.

              nirmatrelvir/ritonavir will increase the level or effect of bictegravir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration may increase bictegravir systemic exposures.

            • orlistat

              orlistat will decrease the level or effect of tenofovir AF by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Loss of virological control reported in HIV-infected patients taking orlistat concomitantly. Exact mechanism is unclear, but may include a drug-drug interaction that inhibits systemic absorption of the antiretroviral drug. Monitor HIV RNA levels frequently and if increased HIV viral load confirmed, discontinue orlistat.

              orlistat will decrease the level or effect of emtricitabine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Loss of virological control reported in HIV-infected patients taking orlistat concomitantly. Exact mechanism is unclear, but may include a drug-drug interaction that inhibits systemic absorption of the antiretroviral drug. Monitor HIV RNA levels frequently and if increased HIV viral load confirmed, discontinue orlistat.

            • selenium

              selenium will decrease the level or effect of bictegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer bictegravir on an empty stomach at least 2 h before or 6 h after polyvalent cation containing drugs.

            • oteseconazole

              oteseconazole will increase the level or effect of tenofovir AF by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.

            • oxaprozin

              emtricitabine, oxaprozin. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • piroxicam

              emtricitabine, piroxicam. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • regorafenib

              regorafenib will increase the level or effect of tenofovir AF by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • ribavirin

              ribavirin increases toxicity of emtricitabine by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Use alternatives if available. Increased risk of lactic acidosis.

            • ritonavir

              ritonavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • safinamide

              safinamide will increase the level or effect of tenofovir AF by Other (see comment). Use Caution/Monitor. Safinamide and its major metabolite may inhibit intestinal BCRP. Monitor BCRP substrates for increased pharmacologic or adverse effects.

            • saquinavir

              saquinavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • sarecycline

              sarecycline will increase the level or effect of tenofovir AF by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor for toxicities of P-gp substrates that may require dosage reduction when coadministered with P-gp inhibitors.

            • sodium sulfate/?magnesium sulfate/potassium chloride

              sodium sulfate/?magnesium sulfate/potassium chloride decreases levels of bictegravir by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Bictegravir sodium/emtricitabine/tenofovir alafenamide fumarate can be takenat least 2 hr before or 6 hr after taking a medication containing magnesium.

            • sodium sulfate/potassium sulfate/magnesium sulfate

              sodium sulfate/potassium sulfate/magnesium sulfate decreases levels of bictegravir by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Bictegravir sodium/emtricitabine/tenofovir alafenamide fumarate can be takenat least 2 hr before or 6 hr after taking a medication containing magnesium.

            • stavudine

              emtricitabine and stavudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • stiripentol

              stiripentol will increase the level or effect of tenofovir AF by Other (see comment). Use Caution/Monitor. Stiripentol is a BCRP transport inhibitor. Consider dosage reduction for BCRP substrates if adverse effects are experienced when coadministered.

            • sucralfate

              sucralfate will decrease the level or effect of bictegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Bictegravir can be taken under fasting conditions 2 hr before antacids containing Al, Mg, or Ca. Routine administration of bictegravir simultaneously with, or 2 hr after, antacids containing Al, Mg, or Ca is not recommended.

            • sulindac

              emtricitabine, sulindac. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • tafamidis

              tafamidis will increase the level or effect of tenofovir AF by Other (see comment). Use Caution/Monitor. Tafamidis inhibits breast cancer resistant protein (BCRP) in vitro and may increase exposure of BCRP substrates following tafamidis or tafamidis meglumine administration. Dosage adjustment of these BCRP substrates may be necessary.

            • tafamidis meglumine

              tafamidis meglumine will increase the level or effect of tenofovir AF by Other (see comment). Use Caution/Monitor. Tafamidis inhibits breast cancer resistant protein (BCRP) in vitro and may increase exposure of BCRP substrates following tafamidis or tafamidis meglumine administration. Dosage adjustment of these BCRP substrates may be necessary.

            • tenofovir DF

              emtricitabine and tenofovir DF both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • tipranavir

              tipranavir and emtricitabine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • tolmetin

              emtricitabine, tolmetin. Either increases levels of the other by decreasing renal clearance. Modify Therapy/Monitor Closely. Toxicity may result from coadministration of emtricitabine with other drugs that are also primarily excreted by glomerular filtration and/or active tubular secretion including high-dose or multiple-dose NSAIDs; alternatives to NSAIDs should be considered.

            • tucatinib

              tucatinib will increase the level or effect of tenofovir AF by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Consider reducing the dosage of P-gp substrates, where minimal concentration changes may lead to serious or life-threatening toxicities.

            • valacyclovir

              valacyclovir increases levels of emtricitabine by Other (see comment). Use Caution/Monitor. Comment: Coadministration of emtricitabine with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of emtricitabine.

            • valganciclovir

              valganciclovir, emtricitabine. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Use alternatives if available. Increased risk of hematologic toxicity.

              valganciclovir increases levels of emtricitabine by Other (see comment). Use Caution/Monitor. Comment: Coadministration of emtricitabine with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of emtricitabine.

            • voclosporin

              voclosporin, tenofovir AF. Either increases toxicity of the other by nephrotoxicity and/or ototoxicity. Modify Therapy/Monitor Closely. Coadministration with drugs associated with nephrotoxicity may increase the risk for acute and/or chronic nephrotoxicity.

            • zidovudine

              emtricitabine and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • zinc

              zinc will decrease the level or effect of bictegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer bictegravir/emtricitabine/tenofovir AF at least 2 hr before or 6 hr after these agents.

            Minor (1)

            • nirmatrelvir/ritonavir

              nirmatrelvir/ritonavir will increase the level or effect of emtricitabine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

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            Adverse Effects

            1-10%

            Adults

            • Diarrhea (3-6%)
            • Nausea (3-5%)
            • Headache (4-5%)
            • Creatine kinase ≥10x ULN (4%)
            • Abnormal dreams (<3%)
            • Fasting LDL-C >190 mg/dL (2-3%)
            • Fatigue (2-3%)
            • Dizziness (2%)
            • Insomnia (2%)
            • Neutrophil <750 mm³ (2%)
            • Amylase >2x ULN (2%)
            • ALT >5x ULN (1-2%)
            • AST >5x ULN (1-2%)

            Children

            • Insomnia, grade 2
            • Anxiety, grade 2

            Frequency Not Defined

            Children

            • Abdominal pain

            Postmarketing Reports

            Angioedema

            Urticaria

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            Warnings

            Black Box Warnings

            Post-treatment acute exacerbation of hepatitis B

            • Severe acute exacerbations of hepatitis B reported in patients coinfected with HIV-1 and HBV and have discontinued products containing emtricitabine (FTC) and/or tenofovir disoproxil fumarate (TDF)
            • Closely monitor hepatic function with both clinical and laboratory follow-up for at least several months in patients coinfected with HIV-1 and HBV who discontinue therapy
            • If appropriate, antihepatitis B therapy may be warranted

            Contraindications

            Coadministration with dofetilide and/or rifampin

            Cautions

            Patients with HIV-1 infection should be tested for the presence of chronic hepatitis B virus (HBV) before initiating antiretroviral therapy (ART); not approved for the treatment of chronic HBV infection (see Black Box Warnings)

            Immune reconstitution syndrome reported in patients treated with combination ART therapy; autoimmune disorders (eg, Graves disease, polymyositis, Guillain-Barré syndrome, autoimmune hepatitis) may occur in the setting of immune reconstitution; time to onset varies and can occur many months after initiation of treatment

            Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, reported with use; suspend treatment if patient develops signs or symptoms of lactic acidosis or pronounced hepatotoxicity (which may include hepatomegaly and steatosis, even in absence of marked transaminase elevations)

            New-onset or worsening renal impairment

            • Cases of acute renal failure and Fanconi syndrome (renal tubular injury with severe hypophosphatemia) reported with the use of tenofovir prodrugs
            • Discontinue drug if clinically significant decreases in renal function or evidence of Fanconi syndrome develop
            • Avoid concurrent or recent use of nephrotoxic drug, including nonsteroidal anti-inflammatory drugs, owing to increased risk of developing renal-related adverse reactions

            Drug interactions overview

            • Bictegravir inhibits OCT2 and MATE1; coadministration with drugs that are OCT2 and MATE1 substrates may increase their plasma concentrations (also see Contraindications)
            • Strong CYP3A inducers that also induce UGT1A1 can substantially decrease bictegravir plasma concentrations ,which may lead to loss of therapeutic effect of bictegravir/emtricitabine/tenofovir AF and development of resistance (also see Contraindications)
            • Strong CYP3A4 inhibitors that also inhibit UGT1A1 may significantly increase bictegravir plasma concentrations
            • Coadministration of drugs that inhibit of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) may increase the absorption and plasma concentrations of tenofovir AF
            • Coadministration of drugs that induce P-gp activity are expected to decrease the absorption of tenofovir AF, resulting in decreased plasma concentration of tenofovir AF, which may lead to loss of therapeutic effect of treatment and development of resistance
            • Coadministration with drugs that reduce renal function or compete for active tubular secretion may increasing concentrations of emtricitabine and tenofovir, thereby increase risk of adverse effects
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            Pregnancy

            Pregnancy

            There is insufficient human data on use of bictegravir/emtricitabine/tenofovir AF during pregnancy to inform a drug-associated risk of birth defects and miscarriage

            Bictegravir: Data from an observational study in Botswana showed that dolutegravir, another integrase inhibitor, was associated with increased risk of neural tube defects when administered at the time of conception and in early pregnancy; data available to date from other sources including the pregnancy registry, clinical trials, and postmarketing data are insufficient to address this risk with bictegravir

            Bictegravir and tenofovir AF use in women during pregnancy has not been evaluated

            Emtricitabine (FTC) use during pregnancy in a limited number of women reported to the APR showed no difference in overall risk of major birth defects for FTC compared with the background rate for major birth defects

            Pregnancy registry

            • Registry monitors pregnancy outcomes in women exposed to bictegravir/emtricitabine/tenofovir AF during pregnancy
            • Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263

            Lactation

            The Centers for Disease Control and Prevention do not recommend HIV-infected mothers breastfeed their infants owing to potential risk for postnatal transmission of HIV

            Unknown whether bictegravir/emtricitabine/tenofovir AF or all of the components of the drug are present in human breast milk, affects human milk production, or has effects on the breastfed infant; emtricitabine has been shown to be present in human breast milk

            Owing to the potential for HIV transmission (in HIV-negative infants), developing viral resistance (in HIV-positive infants), and adverse reactions in a breastfed infant similar to those seen in adults, instruct mothers not to breastfeed while taking this medication

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Three-drug combination of bictegravir (BIC), a human immunodeficiency virus type 1 (HIV-1) integrase strand transfer inhibitor (INSTI); emtricitabine (FTC); and tenofovir alafenamide (TAF), both HIV-1 nucleoside analog reverse transcriptase inhibitors (NRTIs)

            Bictegravir: HIV-1 integrase strand transfer inhibitor (INSTI); inhibits HIV-1 replication by blocking the strand transfer step of viral DNA integration into the host genome; novel INSTI since it can be dosed once daily without boosting

            Emtricitabine: Nucleoside reverse transcriptase inhibitor (NRTI); cytosine analog phosphorylated to emtricitabine 5'-triphosphate causing inhibition of HIV and RNA dependent DNA polymerase

            Tenofovir alafenamide (AF): NRTI prodrug of tenofovir; compared with tenofovir disoproxil fumarate (tenofovir DF, Viread), tenofovir alafenamide (AF) is a more targeted form of tenofovir that has demonstrated high antiviral efficacy at a dose that is 10 times lower than tenofovir DF, as well as an improved renal and bone safety profile; inhibits HIV-1 RT by competing with the natural substrate deoxyadenosine 5′-triphosphate and, after incorporation into DNA, by DNA chain termination

            Absorption

            Peak plasma time (adults): 2-4 hr (BIC); 1.5-2 hr (FTC); 0.5-2 hr (TAF)

            Effect of high-fat meal

            • AUC ratio: 1.24 (BIC); 0.96 (FTC); 1.63 (TAF)
            • Peak plasma concentration ratio: 1.13 (BIC); 0.86 (FTC); 0.92 (TAF)

            Peak plasma concentration

            • Adults: 6.15 mcg/mL (BIC); 2.13 mcg/mL (FTC); 0.121 mcg/mL (TAF)
            • Pediatric patients (6 to <12 years): 9.46 mcg/mL (BIC); 3.89 mcg/mL (FTC); 0.205 mcg/mL (TAF)
            • Pediatric patients (12 to <18 years): 6.24 mcg/mL (BIC); 2.69 mcg/mL (FTC); 0.133 mcg/mL (TAF)

            AUC

            • Adults: 102 mcg·hr/mL (BIC); 12.3 mcg·hr/mL (FTC); 0.142 mcg·hr/mL (TAF)
            • Pediatric patients (6 to <12 years): 128 mcg·hr/mL (BIC); 17.6 mcg·hr/mL (FTC); 0.278 mcg·hr/mL (TAF)
            • Pediatric patients (12 to <18 years): 89.1 mcg·hr/mL (BIC); 13.6 mcg·hr/mL (FTC); 0.196 mcg·hr/mL (TAF)

            Distribution

            Protein binding: >99% (BIC); <4% (FTC); ~80% (TAF)

            Blood-to-plasma ratio: 0.64 (BIC); 0.6 (FTC); 1 (TAF)

            Metabolism

            Bictegravir

            • Metabolized by CYP3A4 and UGT1A1

            Emtricitabine

            • Not significantly metabolized
            • Metabolized by oxidation

            Tenofovir

            • Tenofovir AF (TAF) is hydrolyzed within cells to form tenofovir (major metabolite), which is phosphorylated to the active metabolite, tenofovir diphosphate
            • In vitro studies have shown that TAF is metabolized to tenofovir by cathepsin A in PBMCs and macrophages, and by CES1 in hepatocytes
            • Upon coadministration with the moderate CYP3A inducer probe efavirenz, TAF exposure was unaffected

            Excretion

            Half-life: 17.3 hr (BIC); 10.4 hr (FTC); 0.51 hr (TAF)

            Excretion, urine: 35% (BIC); 70% (FTC); <1% (TAF)

            Excretion, feces: 60.3% (BIC); 13.7% (FTC); 31.7% (TAF)

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            Administration

            Oral Administration

            For oral use only

            Take once daily with or without food

            Storage

            Tablets

            • Store below 30°C (86°F)
            • Keep container tightly closed
            • Dispense only in original container
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            Images

            No images available for this drug.
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            Patient Handout

            A Patient Handout is not currently available for this monograph.
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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.