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Vemlidy Generic Name & Formulations
Legal Class
Rx
General Description
Tenofovir alafenamide 25mg; tabs.
Pharmacological Class
Nucleoside analogue (reverse transcriptase inhibitor).
How Supplied
Tabs—30
Manufacturer
Generic Availability
NO
Mechanism of Action
Tenofovir alafenamide is a phosphonamidate prodrug of tenofovir (2’-deoxyadenosine monophosphate analog). As a lipophilic cell-permeant compound, tenofovir alafenamide enters primary hepatocytes by passive diffusion and by the hepatic uptake transporters OATP1B1 and OATP1B3. Tenofovir alafenamide is then converted to tenofovir through hydrolysis primarily by carboxylesterase 1 (CES1) in primary hepatocytes. Intracellular tenofovir is subsequently phosphorylated by cellular kinases to the pharmacologically
active metabolite tenofovir diphosphate. Tenofovir diphosphate inhibits HBV replication through incorporation into viral DNA by the HBV reverse transcriptase, which results in DNA chain-termination.
Vemlidy Indications
Indications
Chronic hepatitis B virus (HBV) infection in those with compensated liver disease.
Vemlidy Dosage and Administration
Vemlidy Contraindications
Not Applicable
Vemlidy Boxed Warnings
Boxed Warning
Post-treatment severe acute exacerbation of hepatitis B.
Vemlidy Warnings/Precautions
Warnings/Precautions
Discontinuation of anti-HBV therapy may be associated with severe acute exacerbations of hepatitis B. Closely monitor patients for several months after stopping treatment; if appropriate, anti-HBV therapy may be warranted. HBV and HIV-1 coinfection: not recommended as monotherapy for treatment of HIV-1 infection (risk of developing HIV-1 resistance). Suspend therapy if lactic acidosis or pronounced hepatotoxicity (eg, hepatomegaly, steatosis) occurs. Assess SCr, estimated CrCl, urine glucose, urine protein in all patients, and serum phosphorus (in chronic kidney disease) before initiating and during therapy. Discontinue if significant renal dysfunction or Fanconi syndrome develops. Decompensated hepatic impairment (Child-Pugh B or C) or ESRD (CrCl <15mL/min) not on hemodialysis: not recommended. Elderly. Pregnancy. Nursing mothers.
Vemlidy Pharmacokinetics
Absorption
Time to maximum concentration: 0.48 hour.
Distribution
80% plasma protein bound.
Elimination
Fecal (31.7%), renal (<1%). Half-life: 0.51 hour.
Vemlidy Interactions
Interactions
Concomitant oxcarbazepine, phenobarbital, phenytoin, rifabutin, rifampin, rifapentine, St. John's wort: not recommended. Antagonized by carbamazepine (see Adults). Concomitant drugs that strongly affect P-gp and BCRP activity may lead to changes in TAF absorption. Caution with concomitant nephrotoxic agents. May be potentiated by drugs that decrease renal function or compete for active tubular secretion (eg, acyclovir, cidofovir, ganciclovir, valacyclovir, valganciclovir, aminoglycosides, high-dose or multiple NSAIDs).
Vemlidy Adverse Reactions
Adverse Reactions
Headache, abdominal pain, cough, fatigue, nausea, back pain; new onset or worsening renal impairment.
Vemlidy Clinical Trials
See Literature
Vemlidy Note
Notes
Register pregnant patients in the Antiretroviral Pregnancy Registry (APR) by calling (800) 258-4263.
Vemlidy Patient Counseling
See Literature
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