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ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Nucleoside and nucleotide reverse transcriptase inhibitors
tenofovir alafenamide
J05AF13
Forms & Strengths
- Oral tablets: 25 mg
- Available in multiple fixed-dose combination tablets (e.g., with emtricitabine, elvitegravir/cobicistat, bictegravir, darunavir/cobicistat)
Adult Dosing
- HIV-1 infection: 25 mg orally once daily (as part of combination antiretroviral therapy)
- Chronic Hepatitis B virus (HBV) infection: 25 mg orally once daily with food
Pediatric Dosing
- HIV-1 infection (pediatric patients >= 6 years of age and weighing >= 25 kg): 25 mg orally once daily
- Chronic HBV infection (pediatric patients >= 12 years of age and weighing >= 35 kg): 25 mg orally once daily
Indications
- Treatment of HIV-1 infection in combination with other antiretroviral agents in adults and pediatric patients weighing >= 25 kg
- Treatment of chronic hepatitis B virus infection in adults and pediatric patients aged >= 12 years and weighing >= 35 kg
Mechanism of Action
- Tenofovir alafenamide (TAF) is a phosphoramidate prodrug of tenofovir (2'-deoxyadenosine monophosphate analogue)
- Enters cells where it is hydrolyzed by cathepsin A and carboxylesterase 1 to form tenofovir
- Tenofovir is subsequently phosphorylated by cellular kinases to the active metabolite, tenofovir diphosphate
- Tenofovir diphosphate inhibits HIV-1 reverse transcriptase and HBV polymerase by competing with natural substrate deoxyadenosine triphosphate and by DNA chain termination
Contraindications
- Previous hypersensitivity reaction to tenofovir alafenamide
Adverse Reactions
- Headache
- Nausea
- Fatigue
- Diarrhea
- Abdominal pain
- Rash
- Increased LDL cholesterol
- Elevated transaminases
Drug Interactions
- P-glycoprotein inducers (e.g., rifampin, St. John's wort, carbamazepine) significantly decrease TAF concentrations and are generally not recommended
- Anticonvulsants (e.g., phenobarbital, phenytoin) may decrease TAF plasma concentrations
- Strong inhibitors of P-gp and BCRP (e.g., cyclosporine) may increase absorption of TAF
Curated Content: Needs Vetting Before Put to Clinical Use