clevudine

Clevudine (Levovir) is a synthetic pyrimidine analogue with activity against hepatitis B virus (HBV). Intracellularly, clevudine is phosphorylated to its active metabolites, clevudine monophosphate and triphosphate. The triphosphate metabolite competes with thymidine for incorporation into viral DNA, thereby causing DNA chain termination and inhibiting the function of HBV DNA polymerase (reverse transcriptase). Clevudine has a long half-life and shows significant reduction of covalently closed circular DNA (cccDNA), therefore the patient is less likely to have a relapse after treatment is discontinued.

Clevudine triphosphate is a TTP analog that is able to inhibit protein priming independently of the deoxynucleoside triphosphate substrate.

Fosclevudine alafenamide (Compound EIDD-02173) is an antiviral agent that acts against HBV (EC50: 1.71 μM).