阿洛夫定, Alovudine

3'-Deoxy-3'-fluorothymidine

Clevudine is a β-L-nucleoside analog of thymidine that has antiviral activity. It is active against hepatitis B virus (HBV) in HepG2/2.15 cells with an EC50 value of 0.1 µM. Clevudine (0.01-10 µM) reduces virion DNA in the culture supernatant of primary hepatocytes isolated from a duckling model of chronic HBV infection. Oral administration of clevudine (3 and 10 mg/kg) reduces serum viral load in a woodchuck model of chronic HBV infection.

Clevudine 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 is a pyrimidine 2'-deoxyribonucleoside.

3'-Deoxy-3'-fluorothymidine is a nucleoside analog that is used to diagnose and treat cancer. It is a prodrug that is metabolized intracellularly by deoxycytidine kinase to the 3'-deoxy-3'-fluoro derivative of thymidine, which competes with natural thymidine for incorporation into DNA. Uptake of 18F-flouride (18F-FDG) in tumor cells has been shown to be proportional to the rate constant (k) of cellular uptake. This process can be quantified using positron emission tomography imaging. The cell cycle inhibitor activity of 3'-deoxy-3'-fluorothymidine has also been demonstrated in vitro and in vivo, inhibiting the proliferation of tumor cells and normal cells in culture, respectively.