|Other names||Adefovir dipivoxil|
|Drug class||Nucleotide analog reverse-transcriptase inhibitor (ntRTI)|
|Main uses||Chronic hepatitis B|
|Side effects||Weakness, diarrhea, abdominal discomfort, headache, nausea, kidney problems|
|Elimination half-life||7.5 hours|
|Chemical and physical data|
|Molar mass||273.189 g·mol−1|
|3D model (JSmol)|
Adefovir, sold under the brand name Hepsera, is a medicine used to treat chronic hepatitis B. It may be used in those over the age of 11. It may be effective in those resistant to lamivudine. It is taken by mouth.
Common side effects include weakness, diarrhea, abdominal discomfort, headache, nausea, and kidney problems. Other side effects may include bone fractures, liver problems, and pancreatitis. Safety in pregnancy is unclear. It is a nucleotide analog reverse-transcriptase inhibitor (ntRTI).
Adefovir was approved for medical use in the United States in 2002 and Europe in 2003. It is available as a generic medication. In the United Kingdom a month of medication costs the NHS about £250 as of 2021. This amount in the United States costs about 800 USD.
It is used at a dose of 10 mg per day in those over the age of 11.
Among the adverse or side effects this medication may have on individuals who are administered it are the following:
Mechanism of action
Adefovir works by blocking reverse transcriptase, an enzyme crucial for the HBV to reproduce in the body. It is approved for the treatment of chronic hepatitis B in adults with evidence of active viral replication and either evidence of persistent elevations in serum aminotransferases (primarily ALT) or histologically active disease.
The main benefit of adefovir over lamivudine (the first NRTI approved for the treatment of HBV) is that it takes a much longer period of time for the virus to develop resistance to it.
Adefovir was invented in the Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic by Antonín Holý, and the drug was developed by Gilead Sciences for HIV with the brand name Preveon. However, in November 1999, an expert panel advised the U.S. Food and Drug Administration (FDA) not to approve the drug due to concerns about the severity and frequency of kidney toxicity when dosed at 60 or 120 mg. The FDA followed that advice, refusing to approve adefovir as a treatment for HIV.
Gilead Sciences discontinued its development for HIV treatment in December 1999, but continued to develop the drug for hepatitis B (HBV), where it is effective with a much lower dose of 10 mg. FDA approval for use in the treatment of hepatitis B was granted on September 20, 2002, and adefovir is sold for this indication under the brand name Hepsera. Adefovir became an approved treatment for HBV in the European Union in March 2003.
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