Combination therapy to treat hepatitis B virus

• US 7,572,800 B2
• Filed: 02/25/2003
• Issued: 08/11/2009
• Est. Priority Date: 11/02/1998
• Status: Expired due to Fees

• Current Assignee: Gilead Sciences Inc.
• Original Assignee: Gilead Sciences Inc.
• Inventors: Painter, George R. III, Barry, David W., Furman, Phillip A., Rousseau, Franck
• Primary Examiner(s): Wang; Shengjun
• Application Number:
  US10/374,363
• Publication Number:
  US 20030158150A1
• Time in Patent Office: 2,359 Days
• Field of Search: 514261-264
• US Class Current: 514/263.23
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/52 Purines, e.g. adenine
• CPC Class Codes: A61K 31/66 Phosphorus compounds
• CPC Class Codes: A61K 31/675 having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• CPC Class Codes: A61K 31/70 Carbohydrates; Sugars; Derivatives thereof sorbitol A61K31/047
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 1/16 for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 31/14 for RNA viruses
• CPC Class Codes: A61P 31/20 for DNA viruses
• CPC Class Codes: A61P 35/00 Antineoplastic agents

Abstract

The present invention is directed to a method for treating hepatitis B virus infection in humans comprising administering a synergistically effective amount of agents having known anti-hepatitis B virus activity in combination or alternation. Specifically, the invention is directed to a method for treating hepatitis B virus infection comprising administering FTC in combination or alternation with penciclovir, famciclovir or Bis-POM-PMEA. Additionally, the invention is directed to a method for treating hepatitis B virus infection comprising administering L-FMAU in combination or alternation with DAPD, penciclovir or Bis-POM-PMEA. The invention is further directed to a method for treating hepatitis B virus infection comprising administering DAPD in combination or alternation with Bis-POM-PMEA.

Claims

1. A pharmaceutical composition for the treatment of hepatitis B virus in a human comprising an effective amount of β

-2-hydroxymethyl-5-(5-fluorocytosin-1-yl) -1,3-oxathiolane (β

-FTC) or a pharmaceutically acceptable salt or ester thereof in a combination with an effective amount of a second anti-hepatitis B agent selected from the group consisting of penciclovir wherein the amounts of β

-FTC and penciclovir produce a synergistic anti-hepatitis B response.

2. The composition of claim 1 wherein the concentration of β

-FTC is proportionately lower than that of the second agent.

3. The composition of claim 1 wherein β

-FTC and the second anti-hepatitis B agent are in a 1;

3 relative molar ratio.

4. The composition of claim 1 wherein β

-FTC and the second anti-hepatitis B agent are in a 1;

10 relative molar ratio.