Emtricitabine And Tenofovir Alafenamide

Brand Names: Descovy

Drug Class: Human Immunodeficiency Virus Nucleoside Analog Reverse Transcriptase Inhibitor

Overview

11 DESCRIPTION DESCOVY (emtricitabine and tenofovir alafenamide) is a fixed dose combination tablet containing emtricitabine (FTC) and tenofovir alafenamide (TAF) for oral administration. FTC, a synthetic nucleoside analog of cytidine, is an HIV nucleoside analog reverse transcriptase inhibitor (HIV NRTI).

Mechanism of Action

12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action DESCOVY is a fixed dose combination of antiretroviral drugs emtricitabine (FTC) and tenofovir alafenamide (TAF) [see Microbiology (12.4) ] . 12.2 Pharmacodynamics Cardiac Electrophysiology In a thorough QT/QTc study in 48 healthy participants, TAF at the recommended dose or at a dose approximately 5 times the recommended dose, did not affect the QT/QTc interval and did not prolong the PR interval. The effect of the other component of DESCOVY, FTC, or the combination of FTC and TAF on the QT interval is not known. 12.3 Pharmacokinetics Absorption, Distribution, Metabolism, and Excretion The pharmacokinetic (PK) properties of the components of DESCOVY are provided in Table 7 .

Indications

  • 1 INDICATIONS AND USAGE HIV-1 Treatment ( 1.1 ): DESCOVY is a two-drug combination of emtricitabine (FTC) and tenofovir alafenamide (TAF), both HIV nucleoside analog reverse transcriptase inhibitors (NRTIs), and is indicated: in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and adolescent patients weighing at least 35 kg. for the treatment of HIV-1 infection in pediatric patients weighing at least 14 kg to less than 35 kg in combination with other antiretroviral agents, including darunavir and cobicistat but not other protease inhibitors that...

Common Doses

  • 200 mg
  • 25 mg
  • 120 mg
  • 15 mg

Dosage

2 DOSAGE AND ADMINISTRATION Testing: Prior to or when initiating DESCOVY, test for hepatitis B virus infection. Prior to or when initiating DESCOVY, and during use 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. ( 2.1 ) HIV-1 Screening: Screen all individuals for HIV-1 infection immediately prior to initiating DESCOVY for HIV-1 PrEP and at least once every 3 months while taking DESCOVY, and upon diagnosis of any other...

Black Box Warning

WARNING: POST-TREATMENT ACUTE EXACERBATION OF HEPATITIS B and RISK OF DRUG RESISTANCE WITH USE OF DESCOVY FOR HIV-1 PRE-EXPOSURE PROPHYLAXIS (PrEP) IN UNDIAGNOSED EARLY HIV-1 INFECTION Severe acute exacerbations of hepatitis B (HBV) have been reported in individuals with HBV who have discontinued products containing emtricitabine (FTC) and/or tenofovir disoproxil fumarate (TDF) and may occur with discontinuation of DESCOVY. Hepatic function should be monitored closely with both clinical and laboratory follow-up for at least several months in individuals with HBV who discontinue DESCOVY.

Contraindications

  • 4 CONTRAINDICATIONS DESCOVY for HIV-1 PrEP is contraindicated in individuals with unknown or positive HIV-1 status [see Warnings and Precautions (5.2) ]. DESCOVY for HIV-1 PrEP is contraindicated in individuals with unknown or positive HIV-1 status. ( 4 )

Side Effects

  • 6 ADVERSE REACTIONS The following adverse reactions are discussed in other sections of the labeling: Severe Acute Exacerbations of Hepatitis B [see Warnings and Precautions (5.1) ] . Immune Reconstitution Syndrome [see Warnings and Precautions (5.3) ] . New Onset or Worsening Renal Impairment [see Warnings and Precautions (5.4) ] . Lactic Acidosis/Severe Hepatomegaly with Steatosis [see Warnings and Precautions (5.5) ]. In participants with HIV-1, the most common adverse reaction (incidence greater than or equal to 10%, all grades) was nausea. ( 6.

Interactions

  • 7 DRUG INTERACTIONS Consult the Full Prescribing Information prior to and during use for potential drug interactions. ( 7 , 12.3 ) 7.1 Potential for Other Drugs to Affect One or More Components of DESCOVY TAF, a component of DESCOVY, is a substrate of P-gp, BCRP, OATP1B1, and OATP1B3. Drugs that strongly affect P-gp and BCRP activity may lead to changes in TAF absorption (see Table 6 ). Drugs that induce P-gp activity are expected to decrease the absorption of TAF, resulting in decreased plasma concentration of TAF, which may lead to loss of therapeutic effect of DESCOVY and development of...