Beta-L-2'-Deoxy-Nucleosides for the Treatment of Hepatitis B
This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′deoxy-β-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-axyl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2′-deoxy-β-L-erythro pentofuranonucleoside or in combination with another anti-hepatitis B agent.
1 - 12 . (canceled)
13 . A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of β-L-thymidine of the formula:
or a pharmaceutically acceptable salt thereof.
14 . The method of claim 13 , wherein an effective amount of β-L-thymidine of the formula:
is administered.
15 . The method of claim 13 , wherein an effective amount of a pharmaceutically acceptable salt of β-L-thymidine of the formula:
is administered.
16 . The method of claim 13 , wherein β-L-thymidine or a pharmaceutically acceptable salt thereof is administered orally.
17 . The method of claim 16 , wherein a unit dosage form comprising β-L-thymidine or a pharmaceutically acceptable salt thereof is administered orally.
18 . The method of claim 17 , wherein the unit dosage form comprises about 50-1000 mg of β-L-thymidine or a pharmaceutically acceptable salt thereof.
19 . The method of claim 17 , wherein the unit dosage form is a tablet.
20 . The method of claim 19 , wherein the unit dosage form further comprises microcrystalline cellulose, magnesium streate, and/or colloidal silicon dioxide.
21 . The method of claim 13 , wherein β-L-thymidine or a pharmaceutically acceptable salt thereof is administered at the dosage of about 1 to 20 mg/kg of body weight per day.
22 . The method of claim 13 , wherein β-L-thymidine or a pharmaceutically acceptable salt thereof is at least 95% in its designated enantiomeric form.