(ten OF oh vir al a FEN a mide)
- Tenofovir Alafenamide Fumarate
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Vemlidy: 25 mg
Brand Names: U.S.
- Antihepadnaviral, Reverse Transcriptase Inhibitor, Nucleotide (Anti-HBV)
Tenofovir alafenamide, an analog of adenosine 5'-monophosphate, is converted intracellularly by hydrolysis to tenofovir and subsequently phosphorylated to the active tenofovir diphosphate. The active moiety inhibits replication of HBV by inhibiting HBV polymerase.
Tenofovir alafenamide (TAF) is converted intracellularly by hydrolysis to tenofovir, then phosphorylated to the active tenofovir diphosphate.
Feces (31.7%) and urine (<1%)
Time to Peak
Serum: 0.48 hours
Serum: 0.51 hours
80% to plasma proteins
Special Populations: Renal Function Impairment
Tenofovir alafenamide and tenofovir systemic exposures were 1.9-fold and 5.7-fold higher, respectively, in severe renal impairment.
Use: Labeled Indications
Chronic hepatitis B: Treatment of chronic hepatitis B virus (HBV) infection in adults with compensated liver disease
There are no contraindications listed in the US manufacturer's labeling.
Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to tenofovir alafenamide or any component of the formulation
Chronic hepatitis B: Oral: 25 mg once daily
Refer to adult dosing.
Dosing: Renal Impairment
CrCl ≥15 mL/minute: No dosage adjustment necessary.
CrCl <15 mL/minute: Use is not recommended.
Dosing: Hepatic Impairment
Mild impairment (Child-Pugh class A): No dosage adjustment necessary.
Decompensated cirrhosis (Child-Pugh class B or C): Use is not recommended.
Oral: Administer with food.
Store below 30°C (86°F). Dispense in original container.
Acyclovir-Valacyclovir: May increase the serum concentration of Tenofovir Products. Tenofovir Products may increase the serum concentration of Acyclovir-Valacyclovir. Monitor therapy
Adefovir: May diminish the therapeutic effect of Tenofovir Products. Adefovir may increase the serum concentration of Tenofovir Products. Tenofovir Products may increase the serum concentration of Adefovir. Avoid combination
Aminoglycosides: May increase the serum concentration of Tenofovir Products. Tenofovir Products may increase the serum concentration of Aminoglycosides. Monitor therapy
Cabozantinib: MRP2 Inhibitors may increase the serum concentration of Cabozantinib. Monitor therapy
CarBAMazepine: May decrease the serum concentration of Tenofovir Alafenamide. Avoid combination
Cidofovir: May increase the serum concentration of Tenofovir Products. Tenofovir Products may increase the serum concentration of Cidofovir. Monitor therapy
Cobicistat: May enhance the adverse/toxic effect of Tenofovir Products. More specifically, cobicistat may impair proper tenofovir monitoring and dosing. Monitor therapy
Diclofenac (Systemic): May enhance the nephrotoxic effect of Tenofovir Products. Management: Seek alternatives to this combination whenever possible. Avoid use of tenofovir with multiple NSAIDs or any NSAID given at a high dose. Consider therapy modification
Fosphenytoin-Phenytoin: May decrease the serum concentration of Tenofovir Alafenamide. Avoid combination
Ganciclovir-Valganciclovir: Tenofovir Products may increase the serum concentration of Ganciclovir-Valganciclovir. Ganciclovir-Valganciclovir may increase the serum concentration of Tenofovir Products. Monitor therapy
Nonsteroidal Anti-Inflammatory Agents: May enhance the nephrotoxic effect of Tenofovir Products. Management: Seek alternatives to these combinations whenever possible. Avoid use of tenofovir with multiple NSAIDs or any NSAID given at a high dose. Consider therapy modification
Orlistat: May decrease the serum concentration of Antiretroviral Agents. Monitor therapy
OXcarbazepine: May decrease the serum concentration of Tenofovir Alafenamide. Avoid combination
PHENobarbital: May decrease the serum concentration of Tenofovir Alafenamide. Avoid combination
Primidone: May decrease the serum concentration of Tenofovir Alafenamide. Avoid combination
Rifabutin: May decrease the serum concentration of Tenofovir Alafenamide. Avoid combination
RifAMPin: May decrease the serum concentration of Tenofovir Alafenamide. Avoid combination
Rifapentine: May decrease the serum concentration of Tenofovir Alafenamide. Avoid combination
St John's Wort: May decrease the serum concentration of Tenofovir Alafenamide. Avoid combination
Tipranavir: May decrease the serum concentration of Tenofovir Alafenamide. Avoid combination
1% to 10%:
Central nervous system: Headache (9%), fatigue (6%)
Endocrine & metabolic: Increased LDL cholesterol (4%), glycosuria, increased amylase
Gastrointestinal: Abdominal pain (7%), nausea (5%)
Hepatic: Increased serum ALT, increased serum AST
Neuromuscular & skeletal: Decreased bone mineral density (3% to 6%), back pain (5%), increased serum creatine phosphokinase
Respiratory: Cough (6%)
Concerns related to adverse effects:
• Lactic acidosis/hepatomegaly: Lactic acidosis and severe hepatomegaly with steatosis, sometimes fatal, have been reported with the use of nucleoside analogs, alone or in combination with other antiretrovirals. Suspend treatment in any patient who develops clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity (marked transaminase elevation may/may not accompany hepatomegaly and steatosis).
• Hepatic impairment: Use is not recommended in patients with Child-Pugh class B or C hepatic impairment.
• Hepatitis B acute exacerbation: [US Boxed Warning]: Discontinuation of anti-hepatitis B therapy may result in severe acute exacerbations of hepatitis B. Monitor clinical and laboratory data closely for several months after treatment discontinuation. If clinically indicated, anti-hepatitis B therapy may be resumed.
• HIV-1 and HBV coinfection: Should not be used as a single agent for the treatment of HIV-1 due to resistance development risk.
• Renal impairment: Use is not recommended in patients with CrCl <15 mL/minute.
• Renal toxicity: Cases of acute renal failure and/or Fanconi syndrome have been reported with use of tenofovir prodrugs; patients with preexisting renal impairment and those taking nephrotoxic agents (including NSAIDs) are at increased risk. Assess serum creatinine, estimated creatinine clearance, serum phosphorus, urine protein, and urine glucose prior to initiation of therapy and during therapy. Discontinue therapy in patients that develop clinically significant decreases in renal function or evidence of Fanconi syndrome.
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
• HIV testing: HIV antibody testing should be offered to all HBV infected patients prior to treatment initiation. If HIV testing is positive, institute an appropriate antiretroviral (HIV-1) combination regimen.
Serum creatinine, serum phosphorus, urine glucose, urine protein (prior to initiation and as clinically indicated during therapy); HIV testing (prior to initiation); hepatic function tests; monitor clinical and laboratory data closely for several months following therapy discontinuation.
Limited data has been reported to the antiretroviral registry related to the use of this drug in pregnancy and no pharmacokinetic studies have been completed in pregnant females. Females coinfected with HIV and HBV who are taking tenofovir alafenamide prior to pregnancy should be offered a choice to switch to tenofovir disoproxil fumarate or continue with the current regimen (HHS [perinatal] 2017).
Health care providers are encouraged to enroll pregnant females exposed to antiretroviral medications as early in pregnancy as possible in the Antiretroviral Pregnancy Registry (1-800-258-4263 or http://www.APRegistry.com).
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience headache, abdominal pain, loss of strength and energy, cough, nausea, or back pain. Have patient report immediately to prescriber signs of kidney problems (urinary retention, hematuria, change in amount of urine passed, or weight gain), signs of liver problems (dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or jaundice), signs of lactic acidosis (fast breathing, tachycardia, abnormal heartbeat, vomiting, fatigue, shortness of breath, severe loss of strength and energy, severe dizziness, feeling cold, or muscle pain or cramps), bone pain, muscle pain, muscle weakness, or pain in the extremities (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
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