IP Library Granted Patent US 9,550,837
Granted Patent B2
US 9,550,837 · App. 14/737,488 · Granted Jan 24, 2017

Therapeutic uses of anti-PCSK9 antibodies

Inventors: Mark W. Sleeman (Melbourne, AU); Joel H. Martin (Putnam Valley, NY); Tammy T. Huang (Goldens Bridge, NY); Douglas MacDonald (New York, NY)
Assignee: Regeneron Pharmaceuticals, Inc.
C07K16/40A61K2039/505C07K2317/21C07K2317/56C07K2317/565C07K2317/76C07K2317/92
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Quick Facts
Patent No.
US 9,550,837
App. No.
14/737,488
Granted
Jan 24, 2017
Kind
B2
Abstract

An human antibody or antigen-binding fragment of a human antibody that specifically binds and inhibits human proprotein convertase subtilisin/kexin type 9 (hPCSK9) characterized by the ability to reduce serum LDL cholesterol by 40-80% over a 24, 60 or 90 day period relative to predose levels, with little or no reduction in serum HDL cholesterol and/or with little or no measurable effect on liver function, as determined by ALT and AST measurements.

Claims (10)

1. A method for treating a subject selected from the group consisting of: a subject indicated for LDL apheresis, a subject with a PCSK9 gain of function mutation, and a subject with primary hypercholesterolemia who is statin intolerant or statin uncontrolled, the method comprising administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising an antibody or antigen-binding fragment thereof which specifically binds hPCSK9, wherein the antibody or antigen-binding fragment comprises the heavy and light chain CDRs of a HCVR/LCVR amino acid sequence pair selected from the group consisting of SEQ ID NOs:90/92 and 218/226.

2. The method of claim 1 , wherein the antibody or antigen-binding fragment comprises heavy and light chain CDR amino acid sequences having SEQ ID NOs:220, 222, 224, 228, 230 and 232.

3. The method of claim 2 , wherein the antibody or antigen-binding fragment comprises an HCVR having the amino acid sequence of SEQ ID NO:218 and an LCVR having the amino acid sequence of SEQ ID NO:226.

4. The method of claim 1 , wherein the antibody or antigen-binding fragment comprises heavy and light chain CDR amino acid sequences having SEQ ID NOs:76, 78, 80, 84, 86 and 88.

5. The method of claim 4 , wherein the antibody or antigen-binding fragment comprises an HCVR having the amino acid sequence of SEQ ID NO:90 and an LCVR having the amino acid sequence of SEQ ID NO:92.

6. The method of claim 1 , wherein the antibody or antigen-binding fragment binds to the same epitope on hPCSK9 as an antibody comprising heavy and light chain CDR amino acid sequences having SEQ ID NOs:220, 222, 224, 228, 230 and 232; or SEQ ID NOs: 76, 78, 80, 84, 86 and 88.

7. The method of claim 1 , wherein the antibody or antigen-binding fragment competes for binding to hPCSK9 with an antibody comprising heavy and light chain CDR amino acid sequences having SEQ ID NOs:220, 222, 224, 228, 230 and 232; or SEQ ID NOs: 76, 78, 80, 84, 86 and 88.

8. The method of claim 1 , wherein the subject has familial hypercholesterolemia (FH).

9. The method of claim 8 , wherein the familial hypercholesterolemia is heterozygous familial hypercholesterolemia (heFH).

10. The method of claim 8 , wherein the familial hypercholesterolemia is homozygous familial hypercholesterolemia (hoFH).

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 25, 2015
From: SLEEMAN, MARK W.; MARTIN, JOEL H.; HUANG, TAMMY T.; MACDONALD, DOUGLAS
To: REGENERON PHARMACEUTICALS, INC.
Reel/Frame 035905/0165 →
Continuity (10)
Continuation 13690585 · Nov 30, 2012
Continuation 12949846 · Nov 19, 2010
Division 12637942 · Dec 15, 2009
Provisional Application 61122482 · Dec 15, 2008
Provisional Application 61210566 · Mar 18, 2009
Provisional Application 61168753 · Apr 13, 2009
Provisional Application 61218136 · Jun 18, 2009
Provisional Application 61249135 · Oct 6, 2009
Provisional Application 61261776 · Nov 17, 2009
Related Publication 20150284474A1 · Oct 8, 2015