Tenofovir
VIREAD
What it isNucleotide reverse-transcriptase inhibitor; HIV infection and chronic hepatitis B.
Why this oneUnlike most HIV NRTIs, it also suppresses hepatitis B and anchors the standard oral PrEP regimens.
What limits itThe disoproxil form can injure renal tubules and bone; alafenamide largely reduces those effects. Stopping either can trigger hepatitis B flare.
FDA-approved for
- HIV infection (2001)
- chronic hepatitis B (2008)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| HIV-1 infection (in combination with other antiretrovirals) | Adults and peds >=35 kg | 300 mg QD | 300 mg QD | 300 mg QD |
| Chronic hepatitis B | Adults and peds >=12 y (>=35 kg) | 300 mg QD | 300 mg QD | 300 mg QD |
| HIV-1 / chronic HBV (weight-banded tablets) | Peds >=2 y, 17 to <35 kg | 8 mg/kg QD (150 mg QD 17-<22 kg; 200 mg QD 22-<28 kg; 250 mg QD 28-<35 kg) | 8 mg/kg QD | 300 mg QD |
Renal CrCl >=50: no adjustment; CrCl 30-49: 300 mg q48h; CrCl 10-29: 300 mg q72-96h; hemodialysis: 300 mg q7d or after ~12 h total dialysis (give post-dialysis); CrCl <10 without HD: no recommendation; peds renal dosing: no data
Hepatic Undefined
In HIV-1, use only as part of an appropriate combination antiretroviral regimen (resistance risk); offer HIV testing to all HBV-infected patients before starting
Instructions
- Take orally QD without regard to food
- Test for HBV and HIV-1 before or when initiating; do not use as sole agent in HIV-1 infection
- Assess serum creatinine, estimated CrCl, urine glucose and urine protein before and during use; add serum phosphorus in chronic kidney disease
- Avoid concurrent or recent nephrotoxic drugs (e.g., high-dose or multiple NSAIDs)
Cautions
- Severe acute HBV exacerbation after discontinuation (boxed) — monitor hepatic function several months after stopping
- New onset or worsening renal impairment, incl. acute renal failure and Fanconi syndrome; adjust interval and monitor renal function if CrCl <50
- HIV-1/HBV coinfection: use only within a combination antiretroviral regimen; test HBV patients for HIV first
- Immune reconstitution syndrome
- Decreases in bone mineral density; consider BMD assessment with pathologic fracture history or osteoporosis risk
- Lactic acidosis / severe hepatomegaly with steatosis — discontinue if suggestive findings
Adverse reactions
- HIV-1 adults (>=10%, Gr 2-4): rash
- Diarrhea
- Nausea
- Headache
- Pain
- Depression
- Asthenia
- HBV compensated: nausea (9%)
- HBV decompensated (>=10%): abdominal pain, insomnia, pruritus, vomiting, dizziness, pyrexia
- Renal: increased creatinine, proximal tubulopathy
- Decreased bone mineral density
Pregnancy Antiretroviral Pregnancy Registry data show no increase in major birth defects vs background (2.3% first-trimester vs 2.7% reference); registry: 1-800-258-4263
Lactation Tenofovir present in human milk; HIV-1: do not breastfeed (transmission risk); HBV: weigh benefits of breastfeeding against risks
⚠ BOXED WARNING
- Severe acute exacerbation of hepatitis B on discontinuation
Cost, est. cash$10–$500/month
Generic entry2015
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityAgent-specific renal, hepatic, hematologic, metabolic and drug-interaction toxicity.
Mechanism of action: Tenofovir ballicule
