Combination Therapy to Treat Hepatitis B Virus

• US 20090247487A1
• Filed: 06/12/2009
• Published: 10/01/2009
• Est. Priority Date: 11/02/1998
• Status: Abandoned Application

• Current Assignee: Gilead Sciences Inc.
• Original Assignee: Gilead Sciences Inc.
• Inventors: Furman, Phillip A., Rousseau, Franck, Painter, George R. III, Barry, David W.
• Application Number:
  US12/483,800
• Publication Number:
  US 20090247487A1
• Time in Patent Office: Days
• US Class Current: 514/81
• 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 method for the treatment of hepatitis B virus in a human comprising administering in combination or alternation a synergistically effective amount of β

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

-FTC) or a pharmaceutically acceptable salt, ester, or prodrug thereof with an effective amount of a second anti-hepatitis B agent selected from the group consisting of famciclovir and Bis-POM-PMEA.

2. The method of claim 1, wherein the β

-FTC is in the form of the (−

)-optical isomer.

3. The method of claim 1, wherein the second anti-hepatitis B agent is famciclovir.

4. The method of claim 1, wherein the second anti-hepatitis B agent is Bis-POM-PMEA.

5. 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, ester, or prodrug thereof in a synergistic combination with an effective amount of a second anti-hepatitis B agent selected from the group consisting of famciclovir and Bis-POM-PMEA.

6. The composition of claim 5, wherein the β

-FTC is in the form of the (−

)-optical isomer.

7. The composition of claim 5, wherein the second anti-hepatitis B agent is famciclovir.

8. The composition of claim 5, wherein the second anti-hepatitis B agent is Bis-POM-PMEA.