adefovir

Adefovir is an acyclic nucleoside phosphonate that acts as a reverse transcriptase inhibitor used for treatment of hepatitis B and herpes simplex virus infection.

Adefovir dipivoxil (GS 0840) is a dipivoxil formulation of adefovir, a nucleoside reverse transcriptase inhibitor analog of adenosine with activity against hepatitis B virus (HBV), herpes virus, and human immunodeficiency virus (HIV).

Adefovir monophosphate is an antiviral acyclic nucleoside phosphonate (ANP) analog with activity against hepatitis B virus (HBV), herpes virus, and human immunodeficiency virus (HIV). It is an orally-administered acyclic nucleotide analog reverse transcriptase inhibitor (ntRTI) that works by blocking reverse transcriptase for the treatment of hepatitis B. Adefovir dipivoxil is not effective against HIV-1.

Pradefovir (Remofovir) is a reverse transcriptase inhibitor potentially for treatment of chronic HBV infection. Pradefovir is also a liver-targeted prodrug of adefovir. After metabolic activation, Pradefovir was converted to PMEA (9-(2-phosphonylmethoxyethyl)adenine) in human liver microsomes with a K(m) of 60 microM, a maximum rate of metabolism of 228 pmol/min/mg protein, and an intrinsic clearance of about 359 ml/min.

Pradefovir mesylate (Hepavir B) is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with Km of 60 μM.

Bicyclol (SY801)(SY 801) is an anti-hepatitis drug. Oral administration of bicyclol normalizes the elevated serum transaminases (ALT, AST) by 50% in chronic viral hepatitis B and C, and also has a certain level of inhibiting HBV and HCV replication. In combination therapy of bicyclol with interferon alpha, lamivudine and adefovir dipivoxil in HBV or HCV, bicyclol may reduce YMDD mutant and side effects and increase the anti-viral efficacy.

Morphothiadin (GLS4) is a potent inhibitor on the replication of both wild-type and adefovir-resistant HBV (IC50 of 12 nM).