Tenofovir

Tenofovir disoproxil fumarate is an acyclic nucleotide analogue of adenosine. It's utilized in combination therapy for the treatment of the human immunodeficiency virus (HIV) and, when used as a single agent, in the treatment of hepatitis B virus (HBV) infection.

Tenofovir

Liver Safety

Despite being a potent antiviral agent, Tenofovir does not seem to be a significant cause of drug-induced liver injury.

Mechanism of Action

Tenofovir (ten of' oh vir) belongs to the class of acyclic nucleotide analogues of adenosine. However, its oral bioavailability is low. This challenge is circumvented by administering its prodrug, tenofovir disoproxil fumarate, which shows better absorption in the gastrointestinal tract. Once inside the cells, it is rapidly hydrolyzed to Tenofovir. This is subsequently phosphorylated to its active form, tenofovir diphosphate. This active form acts as a competitive inhibitor of the HIV reverse transcriptase and HBV polymerase. Additionally, it gets incorporated into the growing DNA strand, leading to chain termination.

FDA Approval Information

The United States Food and Drug Administration (FDA) granted approval for Tenofovir for HIV infection treatment in 2001. By 2008, its use extended to treating hepatitis B. Its primary indications include treatment and prevention of HIV infection, typically in combination with other reverse transcriptase or protease inhibitors. Furthermore, it's approved as a monotherapy for chronic hepatitis B.

Dosage and Administration

Tenofovir can be found under the brand name Viread as 300 mg oral tablets. It is also available in combination with other antiviral agents for HIV infection treatment, typically administered once daily:

• With emtricitabine as Truvada in 300/200 mg oral tablets.
• With emtricitabine and efavirenz as Atripla in 300/200/600 mg oral tablets.
• With emtricitabine and rilpivirine as Complera in 300/200/25 mg oral tablets.
• With emtricitabine, elvitegravir, and cobicistat as Stribild in 300/200/150/150 mg oral tablets.

The recommended dosage for adults is 300 mg taken once daily.

Side Effects

Tenofovir is generally well-tolerated, but side effects, though rare, can occur. These may include:

• Asthenia
• Diarrhea
• Flatulence
• Nausea and vomiting
• Renal dysfunction
• Rash

See Also

• HIV/AIDS
• Hepatitis B
• Antiretroviral Therapy

Antiviral agents

Drugs for HIV Infection, in the Subclass Antiretroviral Agents

• Fusion Inhibitors (HIV)
  • Enfuvirtide, Maraviroc

• Integrase Inhibitors (HIV)
  • Dolutegravir, Elvitegravir, Raltegravir

• Monoclonal Antibodies
  • Ibalizumab

• Nonnucleoside Reverse Transcriptase Inhibitors (HIV)
  • Delavirdine, Efavirenz, Etravirine, Nevirapine, Rilpivirine

• Nucleoside Analogues (HIV)
  • Abacavir, Didanosine, Emtricitabine, Lamivudine, Stavudine, Tenofovir, Zidovudine

• Protease Inhibitors (HIV)
  • Amprenavir, Atazanavir, Darunavir, Fosamprenavir, Indinavir, Lopinavir, Nelfinavir,Ritonavir, Saquinavir, Tipranavir

Drugs for Hepatitis B

• • Alpha Interferon, Adefovir, Emtricitabine, Entecavir, Lamivudine, Telbivudine, Tenofovir

Drugs for Hepatitis C

• Interferon Based Therapies
  • Alpha Interferon and Peginterferon, Ribavirin

HCV NS5A Inhibitors

• Daclatasvir, Elbasvir, Ledipasvir, Ombitasvir, Pibrentasvir, Velpatasvir

HCV NS5B (Polymerase) Inhibitors

• Dasabuvir, Sofosbuvir

HCV Protease Inhibitors

• Asunaprevir, Boceprevir, Glecaprevir, Grazoprevir, Paritaprevir, Simeprevir, Telaprevir, Voxilaprevir

Combination Therapies

• Epclusa, Harvoni, Mavyret, Technive, Viekira Pak, Vosevi, Zepatier

Drugs for Herpes Virus Infections (HSV, CMV, others)

• Acyclovir, Cidofovir, Famciclovir, Foscarnet, Ganciclovir, Valacyclovir, Valganciclovir

Drugs for Influenza

• Amantadine, Oseltamivir, Peramivir, Rimantadine, Zanamivir

• Dailymed label info on Tenofovir
• FDA Tenofovir

Tenofovir Resources
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