Adefovir dipivoxil, CAS number 142340-99-6, is a nucleotide analog reverse transcriptase inhibitor, or “ntRTI”. Previously called bis-POM PMEA, adefovir dipivoxil is used is the treatment of chronic hepatitis B. Also produced under the trade names Hepsera and Preveon, adefovir dipivoxil is approved by the FDA for treatment in patients with active cases of chronic hepatitis B. Adefovir dipivoxil acts as a blocker to the enzyme reverse transcriptase, thus inhibiting the ability of this enzyme to reproduce in affected patients. LGM Pharma is a provider of adefovir dipivoxil for research and development purposes, and provides support for clients throughout the research and development process.
Photo courtesy of Fox Chase Cancer Center
Adefovir dipivoxil has proven it’s efficacy, as well as safety, in clinical studies. In a Phase 2 trial, adefovir dipivoxil proved to be a strong competitor when tested against lamivudine-resistant strains of the hepatitis B virus. The aforementioned trial randomly chose 515 patients with chronic hepatitis B, and also positive for the hepatitis B e antigen. These patients were given an oral tablet of 10 milligrams, 30 milligrams or a placebo of adefovir dipivoxil. After 48 weeks of testing, patients who received either the 10 or 30 milligram dose showed an increase of the HBeAG antibodies. Patients also displayed reduced serum HBV DNA and alanine aminotransferase levels, as well as improved liver function.
The trade name of adefovir dipivoxil, Hepsera (or Preveon), made by Gilead, was the first nucleotide analog to be approved for the indication of chronic and active hepatitis B in patients. Additional research in phase 3 trials of Hepsera indicated improvement in liver function for 64% of patients studied, as compared to 33% of patients who received a placebo. While these are all positive results, there have been side effects noted. Notable negative effects of adefovir dipivoxil include weakness, headache, nausea, abdominal pain, diarrhea and dyspepsia. Severe side effects are not common, but possible. These include lactic acidosis and nephrotoxicity.
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