icn 20013

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.