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)

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 <30 mL/min): Not recommended

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

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 <30 mL/min): Not recommended

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

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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            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%)

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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

            • IIf 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

            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
            • Drugs affecting renal function
              • Emtricitabine and tenofovir are primarily excreted by the kidneys by glomerular filtration and active tubular secretion
              • 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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            Formulary

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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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            Code Definition
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