emtricitabine/tenofovir AF (Rx)

Brand and Other Names:Descovy
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

emtricitabine/tenofovir alafenamide (AF)

tablet

  • 200mg/25mg

HIV Infection

Indicated in combination with other antiretroviral agents (ARTs) for HIV-1 infection in adults

1 tablet PO qDay

HIV-1 Pre-exposure Prophylaxis

Indicated for at-risk patients to reduce risk of HIV-1 infection from sex, excluding those with receptive vaginal sex

1 tablet PO qDay

Dosage Modifications

Renal impairment

  • Mild-to-moderate (CrCl ≥30 mL/min): No dosage adjustment required
  • Severe (CrCl 15 to <30 mL/min): Not recommended
  • CrCl ≤15 mL/min
    • Receiving chronic hemodialysis: On days of hemodialysis, administer daily dose after hemodialysis completion
    • Not receiving chronic hemodialysis: Not recommended
    • Coadministration of HIV-1 protease inhibitor (ie, ritonavir, cobicistat) with or without hemodialysis: Safety and efficacy not established

Hepatic impairment

  • Mild-to-moderate (Child Pugh class A or B): No dosage adjustment required
  • Severe (Child Pugh class C): Not studied

Dosing Considerations

For specific dosing recommendations for coadministered third agents for HIV treatment, refer to their respective prescribing information or AIDSinfo guidelines

HIV-1 screening for for HIV-1 PrEP

  • Screen for HIV-1 infection immediately before initiating for HIV-1 PrEP and at least once q3Months during treatment, and upon diagnosis of any other sexually transmitted infections (STIs)
  • If recent (<1 month) exposure to HIV-1 are suspected or clinical symptoms consistent with acute HIV-1 infection are present, use a test approved or cleared by the FDA to aid in the diagnosis of acute or primary HIV-1 infection

Laboratory testing

  • Must have negative HIV-1 test immediately before initiating drug for HIV-1 PrEP
  • Test for hepatitis B virus infection before initiating for HIV treatment or PrEP
  • Assess estimated CrCl, urine glucose and urine protein before initiating therapy and monitor during therapy in all patients

Limitation of use

  • Indication for PrEP does not include use in individuals at risk of HIV-1 from receptive vaginal sex
  • Effectiveness in this population has not been evaluated

Dosage Forms & Strengths

emtricitabine/tenofovir alafenamide (AF)

tablet

  • 200mg/25mg

HIV Infection

In combination with other antiretroviral agents (ARTs) for pediatric patients aged ≥12 yr who weigh ≥35 kg

In combination with other ARTs other than protease inhibitors requiring a CYP3A inhibitor, in adolescents and children weighing 25 kg-35 kg

<12 years: Safety and efficacy not established

≥12 years and weight ≥25 kg

  • 1 tablet PO qDay (see following restrictions for choice of other ARTs for children weighing between 25-35 kg)
  • Weight 25-35 kg: Safety and effectiveness of emtricitabine/tenofovir AF coadministered with an HIV-1 protease inhibitor that is administered with either ritonavir or cobicistat have not been established in children who weigh <35 kg

HIV-1 Pre-exposure Prophylaxis

Indicated for at-risk adolescents aged ≥12 yr weighing ≥35 kg to reduce the risk of HIV-1 infection from sex, excluding those who have receptive vaginal sex

<12 years: Safety and efficacy not established

≥12 years and weight ≥35 kg: 1 tablet PO qDay

Dosage Modifications

Renal impairment

  • Mild-to-moderate (CrCl ≥30 mL/min): No dosage adjustment required
  • Severe (CrCl 15 to <30 mL/min): Not recommended
  • CrCl ≤15 mL/min
    • Receiving chronic hemodialysis: On days of hemodialysis, administer daily dose after hemodialysis completion
    • Not receiving chronic hemodialysis: Not recommended
    • Coadministration of HIV-1 protease inhibitor (ie, ritonavir, cobicistat) with or without hemodialysis: Safety and efficacy not established
  • Hepatic impairment

  • Mild-to-moderate (Child Pugh class A or B): No dosage adjustment required
  • Severe (Child Pugh class C): Not studied

Dosing Considerations

For specific dosing recommendations for coadministered third agents for HIV treatment, refer to their respective prescribing information or AIDSinfo guidelines

HIV-1 screening for for HIV-1 PrEP

  • Screen for HIV-1 infection immediately before initiating for HIV-1 PrEP and at least once q3Months during treatment, and upon diagnosis of any other sexually transmitted infections (STIs)
  • If recent (<1 month) exposure to HIV-1 are suspected or clinical symptoms consistent with acute HIV-1 infection are present, use a test approved or cleared by the FDA to aid in the diagnosis of acute or primary HIV-1 infection

Laboratory testing

  • Must have negative HIV-1 test immediately before initiating drug for HIV-1 PrEP
  • Test for hepatitis B virus infection before initiating for HIV treatment or PrEP
  • Assess estimated CrCl, urine glucose and urine protein before initiating therapy and monitor during therapy in all patients

Limitation of use

  • Indication for PrEP does not include use in individuals at risk of HIV-1 from receptive vaginal sex
  • Effectiveness in this population has not been evaluated

HIV-1 Infection (<12 yr) (Orphan)

Orphan designation for treatment of human immunodeficiency virus type 1 (HIV-1) infection in children aged <12 yr

Sponsor

  • Gilead Sciences, Inc; 333 Lakeside Drive; Foster City, California 94404
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Interactions

Interaction Checker

and emtricitabine/tenofovir AF

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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            Contraindicated (2)

            • 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.

            Serious - Use Alternative (2)

            • 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.

            • 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.

            Monitor Closely (63)

            • 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.

            • 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

            • 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.

            • 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.

            • 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.

            • 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.

            • 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.

            • 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.

            • 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.

            • 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.

            • 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.

            • 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.

            • sofosbuvir/velpatasvir

              sofosbuvir/velpatasvir increases levels of tenofovir AF by unspecified interaction mechanism. Use Caution/Monitor. Monitor for tenofovir-associated adverse reactions. .

            • 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.

            • 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.

            Minor (0)

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              Adverse Effects

              1-10%

              Nausea (10%)

              Bone mineral density (BMD) decline >5% (10%)

              Diarrhea (7%)

              Creatine kinase ≥10 x ULN (7%)

              Headache (6%)

              Fatigue (5%)

              LDL-C >190 mg/dL (5%)

              Total cholesterol >300 mg/dL (2%)

              Potmarketing Reports

              Acute renal failure, acute tubular necrosis, proximal renal tubulopathy, and Fanconi syndrome

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              Warnings

              Black Box Warnings

              Post-treatment acute exacerbation of hepatitis B

              • Severe acute exacerbations of hepatitis B (HBV) reported in HBV-infected individuals who discontinued products containing emtricitabine (FTC) and/or tenofovir disoproxil fumarate (TDF) and may occur with discontinuation of drug
              • Monitor hepatic function closely with both clinical and laboratory follow-up for at least several months in individuals infected with HBV who discontinue therapy

              • If appropriate, initiation of antihepatitis B therapy may be warranted

              Risk of drug resistance if prescribed for PrEP in undiagnosed early HIV-1 infection

              • Use for HIV-1 PrEP must only be prescribed to individuals confirmed to be HIV-negative immediately before initiating and reconfirmed at least every 3 months during use
              • Drug-resistant HIV-1 variants have been identified with use for HIV-1 PrEP following undetected acute HIV-1 infection
              • Do not initiate for HIV-1 PrEP if signs or symptoms of acute HIV-1 infection are present unless negative infection status is confirmed

              Contraindications

              Use for HIV-1 PrEP is contraindicated in individuals with unknown or positive HIV-1 status

              Cautions

              All individuals should be tested for the presence of chronic HBV infection before initiating ART therapy or PrEP; emtricitabine/tenofovir AF is not approved for treatment of chronic HBV infection, and safety and efficacy are not established in patients coinfected with HIV-1 and HBV (see Black Box Warnings)

              Use for HIV-1 PrEP to reduce the risk of HIV-1 infection is part of a comprehensive prevention strategy, including adherence to daily administration and safer sex practices, including condoms, to reduce the risk of sexually transmitted infections (STIs); the time from initiation of emtricitabine/tenofovir AF for HIV-1 PrEP to maximal protection against HIV-1 infection is unknown

              Before initiating for PrEP, individuals must be confirmed to be HIV-1 negative; HIV-1 resistance substitutions may emerge in individuals with undetected HIV-1 infection who are taking only emtricitabine/tenofovir AF, which alone does not constitute a complete HIV-1 treatment regimen; while using for PrEP, testing should be repeated at least every 3 months, and upon diagnosis or any other STD

              Immune reconstitution syndrome reported with combination ART therapy, including emtricitabine; during initial phase of combination ART treatment, patients whose immune system responds may develop inflammatory response to indolent or residual opportunistic infections (eg, Mycobacterium avium infection, cytomegalovirus, Pneumocystis jirovecii pneumonia [PCP], or tuberculosis), which may necessitate further evaluation and treatment; autoimmune disorders (eg, Grave disease, polymyositis, Guillain-Barré syndrome) may also emerge

              New-onset or worsening renal impairment reported with tenofovir, including cases of acute renal failure and Fanconi syndrome

              Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, reported with the use of nucleoside analogs, alone or in combination with other ARTs; suspend treatment with clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity

              Worsening renal impairment

              • Postmarketing cases of renal impairment, including acute renal failure, proximal renal tubulopathy (PRT), and Fanconi syndrome reported; while most of these cases were characterized by potential confounders that may have contributed to reported renal events, it is also possible these factors may have predisposed patients to tenofovir-related adverse reactions
              • Not recommended in individuals with estimated creatinine clearance of 15 to below 30 mL/min, or individuals with estimated creatinine clearance below 15 mL/min who are not receiving chronic hemodialysis
              • Individuals taking tenofovir prodrugs who have impaired renal function and those taking nephrotoxic agents including non-steroidal anti-inflammatory drugs are at increased risk of developing renal-related adverse reactions
              • Prior to or when initiating therapy and during treatment on a clinically appropriate schedule, assess serum creatinine, estimated creatinine clearance, urine glucose, and urine protein in all individuals
              • In individuals with chronic kidney disease, also assess serum phosphorus; discontinue drug in individuals who develop clinically significant decreases in renal function or evidence of Fanconi syndrome.

              Drug interaction overview

              • Not for administration with other drugs containing emtricitabine or tenofovir DF, or containing tenofovir AF
              • Tenofovir AF
                • Tenofovir AF is a substrate of P-gp, BCRP, OATP1B1, and OATP1B3
                • Drugs that strongly affect P-gp and BCRP activity may lead to changes in tenofovir AF absorption
                • Drugs that induce P-gp activity are expected to decrease tenofovir AF absorption, resulting in decreased plasma concentration, which may lead to loss of therapeutic effect and development of resistance
                • Coadministration with drugs that inhibit P-gp and BCRP may increase tenofovir AF absorption and plasma concentration
              • Effects in renal function
                • Emtricitabine and tenofovir are primarily excreted by the kidneys by glomerular filtration and active tubular secretion
                • Postmarketing cases of renal impairment, including acute renal failure, proximal renal tubulopathy (PRT), and Fanconi syndrome reported with tenofovir AF-containing products reported
                • Coadministration of emtricitabine/tenofovir AF with drugs that reduce renal function or compete for active tubular secretion may increase emtricitabine/tenofovir AF; thereby, increasing risk for adverse effects
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              Pregnancy

              Pregnancy

              Pregnancy exposure registry monitors pregnancy outcomes in women exposed to drug during pregnancy; healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263

              There are insufficient human data on use during pregnancy to inform a drug-associated risk of birth defects and miscarriage; tenofovir alafenamide (TAF) use in women during pregnancy has not been evaluated; however, emtricitabine (FTC) use during pregnancy has been evaluated in a limited number of women reported to the APR

              Available data from APR show no difference in risk of overall major birth defects for FTC (2.4%) compared with background rate for major birth defects of 2.7% in a U.S. reference population of Metropolitan Atlanta Congenital Defects Program (MACDP); the rate of miscarriage is not reported in the APR

              Lactation

              The Centers for Disease Control and Prevention recommend that HIV-infected mothers not breastfeed infants, to avoid risking postnatal transmission of HIV

              FTC has been shown to be present in human breast milk; not known if TAF is present in human breast milk; tenofovir has been shown to be present in milk of lactating rats and rhesus monkeys after administration of TDF; not known if TAF is present in animal milk

              Not known if drug combination affects milk production or has effects on breastfed child; because of 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 if they are receiving therapy

              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

              Emtricitabine: Nucleoside reverse transcriptase inhibitor (NRTI); following phosphorylation, interferes with HIV viral DNA polymerase and inhibits viral replication; cytosine analogue

              Tenofovir 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

              Emtricitabine

              • Peak plasma time: 3 hr
              • Peak plasma concentration: 2.1 mcg/mL
              • Trough plasma concentration: 0.1 mcg/mL
              • AUC: 11.7 mcg•hr/mL

              Tenofovir

              • Peak plasma time: 1 hr
              • Peak plasma concentration: 0.16 mcg/mL
              • AUC: 0.21 mcg•hr/mL

              Distribution

              Emtricitabine

              • Protein bound: <4%

              Tenofovir

              • Protein bound: 80%
              • Vd: 1.2-1.3 L/kg

              Metabolism

              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

              Elimination

              Emtricitabine

              • Half-life: 10 hr
              • Dialyzable: 30% removed by hemodialysis
              • Excretion: 70% urine; 13.7% feces

              Tenofovir

              • Half-life: 0.51 hr
              • Excretion: 31.7% feces; <1% urine
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              Administration

              Oral Administration

              For oral use only

              Swallow 1 capsule once daily with or without food

              Storage

              Store <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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              The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

              Tier Description
              1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
              2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
              3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
              4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              NC NOT COVERED – Drugs that are not covered by the plan.
              Code Definition
              PA Prior Authorization
              Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
              QL Quantity Limits
              Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
              ST Step Therapy
              Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
              OR Other Restrictions
              Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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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.