Drug intelligence / Profile preview

pradefovir

Development stage
Phase 3
Lead developer
Ligand Pharmaceuticals
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Pradefovir is a liver-targeted, orally administered small molecule prodrug of adefovir, designed for the treatment of chronic hepatitis B virus (HBV) infection. It belongs to a novel series of phosphate and phosphonate prodrugs that are specifically activated in the liver by cytochrome P450 3A4 (CYP3A4), resulting in higher concentrations in hepatic tissue and reduced exposure to other organs such as the kidneys. After activation, pradefovir is converted to adefovir, which is then phosphorylated by cellular kinases into its active diphosphate form. This active metabolite competes with dATP and is incorporated into viral DNA by HBV DNA polymerase, causing chain termination and inhibition of viral replication. Pradefovir has demonstrated efficacy comparable to tenofovir disoproxil fumarate with an improved safety profile due to lower nephrotoxicity risk[1][2][3][6].

Brand names
Hepavir-B
Other names
pradefovir mesylateremofovir mesylate
02

Targets

HBV Pol (Hepatitis B virus polymerase)CYP3A4 (Cytochrome P450 3A4)

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