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tenofovir disoproxil fumarate

Acyclic nucleoside phosphonate · Antiviral, Hepatitis B agent

Acyclic nucleoside phosphonateAntiviral, Hepatitis B agent
CDSCO approved
EXCRETION
not curated
INTERACTIONS
1 major
SEVERE in our sources
PREGNANCY
B
FDA category + note
Top interactionssee all 4
  • DiclofenacSevereTextbookG&G 14e · p1245-1266

Mechanism

Tenofovir disoproxil fumarate is a prodrug that is cleaved to tenofovir in plasma, which is then phosphorylated intracellularly to tenofovir diphosphate. Tenofovir diphosphate inhibits both HIV-1 and HBV reverse transcriptase activities.

Indications

HBV infection in individuals 2 years or older (preferred agent)Indefinite treatment for patients with cirrhosis

Dosing

Adult
300 mg once daily
Pediatric
8 mg/kg, maximum 300 mg daily, for children 2 years or older
Renal adjustment
Reduced in patients with renal impairment (ClCr below 50 mL/min)

Pharmacokinetics

Half-life
17 h (plasma); 6 days (tenofovir diphosphate in peripheral blood); 17 days (tenofovir diphosphate in red blood cells)
Bioavailability
Approximately 25%
Protein binding
Negligible (<8%)
Metabolism
Not metabolized by CYP enzymes
Excretion
Roughly 10% of the dose removed by a 4-h hemodialysis session

Side effects

Common
Abdominal pain (in decompensated cirrhosis)Nausea (in decompensated cirrhosis)Insomnia (in decompensated cirrhosis)Pruritus (in decompensated cirrhosis)Vomiting (in decompensated cirrhosis)Dizziness (in decompensated cirrhosis)Pyrexia (in decompensated cirrhosis)
Serious
  • Nephrotoxicity
  • Bone toxicities
  • Decrease in bone mineral density

Pregnancy & lactation

Pregnancy

B

Drug interactions

Diclofenac
Severe
Textbook

Acute renal insufficiency.

Use with caution.

Source: G&G 14e · p1245-1266

Ledipasvir
Moderate
Textbook

Increased tenofovir exposure, potentially increasing the risk of renal toxicity, especially in HIV-infected individuals taking TDF with a boosting agent.

Patients receiving such combinations require more frequent renal monitoring. Use of TAF instead of TDF is an option for patients taking an antiretroviral regimen, which includes ritonavir and cobicistat.

Source: G&G 14e · p1232, p1238

Sofosbuvir
Moderate
Textbook

Increased tenofovir exposure, potentially increasing the risk of renal toxicity.

Patients receiving such combinations require more frequent renal monitoring. Consider using tenofovir alafenamide fumarate (TAF) instead of TDF in patients on antiretroviral regimens with boosting agents (ritonavir/cobicistat).

Source: G&G 14e · p1232, p1237, p1238

Velpatasvir
Moderate
Textbook

Increased tenofovir exposure, potentially increasing the risk of renal toxicity, especially in HIV-infected individuals taking TDF with a boosting agent.

Patients receiving such combinations require more frequent renal monitoring. Use of TAF instead of TDF is an option for patients taking an antiretroviral regimen, which includes ritonavir and cobicistat.

Source: G&G 14e · p1232, p1238

Related guidelines

Ask House about tenofovir disoproxil fumarate

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Sources: Goodman & Gilman 14e·Verified: 2026-05-10 · House clinical team