IP Library Granted Patent US 8,742,075
Granted Patent B2
US 8,742,075 · App. 13/073,617 · Granted Jun 3, 2014

Monoclonal antibodies against ANGPTL3

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Quick Facts
Patent No.
US 8,742,075
App. No.
13/073,617
Granted
Jun 3, 2014
Kind
B2
Abstract

Monoclonal antibodies that specifically bind to ANGPTL3 are provided. Monoclonal antibodies that neutralize at least one activity of ANGPTL3 are provided. Methods of treating a disorder of lipid metabolism using neutralizing monoclonal antibodies are provided.

Claims (17)

1. A monoclonal antibody that binds to angiopoietin-like protein 3 (ANGPTL3) and neutralizes at least one activity of ANGPTL3, wherein the antibody binds to a peptide consisting of the amino acid sequence of SEQ ID NO: 9 with at least 3-fold greater affinity than the antibody binds to a peptide consisting of the amino acid sequence of SEQ ID NO: 86, 87, or 88.

2. The antibody of claim 1 , wherein the antibody decreases the level of at least one serum lipid in vivo.

3. The antibody of claim 2 , wherein the at least one serum lipid is selected from serum triglycerides, total cholesterol, and free fatty acids.

4. The antibody of claim 3 , wherein the antibody decreases the level of at least two serum lipids in vivo.

5. The antibody of claim 1 , wherein the antibody binds to mouse ANGPTL3 and human ANGPTL3.

6. The antibody of claim 1 , wherein the antibody is selected from a mouse monoclonal antibody, a humanized monoclonal antibody, and a human monoclonal antibody.

7. The antibody of claim 1 , wherein the antibody is an antibody fragment.

8. The antibody of claim 7 , wherein the antibody fragment is selected from a scFv, a Fab, a Fab′, and a F(ab′) 2 .

9. The monoclonal antibody of claim 1 , wherein the heavy chain comprises a CDR1 as set forth in SEQ ID NO: 35, a CDR2 as set forth in SEQ ID NO: 36, and a CDR3 as set forth in SEQ ID NO: 37; and the light chain comprises a CDR1 as set forth in SEQ ID NO: 44, a CDR2 as set forth in SEQ ID NO: 45, and a CDR3 as set forth in SEQ ID NO: 46.

10. The monoclonal antibody of claim 1 , wherein the heavy chain comprises a CDR1 as set forth in SEQ ID NO: 38, a CDR2 as set forth in SEQ ID NO: 39, and a CDR3 as set forth in SEQ ID NO: 40; and the light chain comprises a CDR1 as set forth in SEQ ID NO: 47, a CDR2 as set forth in SEQ ID NO: 48, and a CDR3 as set forth in SEQ ID NO: 49.

11. The monoclonal antibody of claim 1 , wherein the heavy chain comprises a CDR1 as set forth in SEQ ID NO: 41, a CDR2 as set forth in SEQ ID NO: 42, and a CDR3 as set forth in SEQ ID NO: 43; and the light chain comprises a CDR1 as set forth in SEQ ID NO: 50, a CDR2 as set forth in SEQ ID NO: 51, and a CDR3 as set forth in SEQ ID NO: 52.

12. The monoclonal antibody of claim 1 , wherein the heavy chain comprises a CDR1 as set forth in SEQ ID NO: 53, a CDR2 as set forth in SEQ ID NO: 54, and a CDR3 as set forth in SEQ ID NO: 55; and the light chain comprises a CDR1 as set forth in SEQ ID NO: 56, a CDR2 as set forth in SEQ ID NO: 57, and a CDR3 as set forth in SEQ ID NO: 58.

13. The monoclonal antibody of claim 1 , wherein the heavy chain comprises a CDR1 as set forth in SEQ ID NO: 71, a CDR2 as set forth in SEQ ID NO: 72, and a CDR3 as set forth in SEQ ID NO: 73; and the light chain comprises a CDR1 as set forth in SEQ ID NO: 77, a CDR2 as set forth in SEQ ID NO: 78, and a CDR3 as set forth in SEQ ID NO: 79.

14. The monoclonal antibody of claim 1 , wherein the heavy chain comprises a CDR1 as set forth in SEQ ID NO: 74, a CDR2 as set forth in SEQ ID NO: 75, and a CDR3 as set forth in SEQ ID NO: 76; and the light chain comprises a CDR1 as set forth in SEQ ID NO: 80, a CDR2 as set forth in SEQ ID NO: 81, and a CDR3 as set forth in SEQ ID NO: 82.

15. A pharmaceutical composition comprising the antibody of claim 1 .

16. A method of treating a disorder of lipid metabolism comprising administering to a patient an effective amount of the pharmaceutical composition of claim 15 , wherein the disorder of lipid metabolism is selected from hypertriglyceridemia and hypercholesterolemia.

17. A method of decreasing the level of one or more serum lipids comprising administering to a patient an effective amount of the pharmaceutical composition of claim 15 .

Assignments (5)
RELEASE OF SECURITY INTEREST Recorded May 5, 2026
From: OXFORD FINANCE LLC
To: LEXICON PHARMACEUTICALS, INC.; LEXICON PHARMACEUTICALS
Reel/Frame 075545/0601 →
SECURITY INTEREST Recorded May 4, 2026
From: LEXICON PHARMACEUTICALS, INC.; LEXICON PHARMACEUTICALS (NEW JERSEY), INC.; LION ACQUISITION CORPORATION
To: HERCULES CAPITAL, INC., AS AGENT
Reel/Frame 075498/0899 →
SECURITY INTEREST Recorded Mar 17, 2022
From: LEXICON PHARMACEUTICALS, INC.
To: OXFORD FINANCE LLC, AS COLLATERAL AGENT
Reel/Frame 059432/0709 →
RELEASE OF SECURITY INTEREST Recorded Sep 14, 2020
From: BIOPHARMA CREDIT PLC
To: LEXICON PHARMACEUTICALS, INC.
Reel/Frame 053767/0445 →
SECURITY INTEREST Recorded Dec 20, 2017
From: LEXICON PHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 044958/0377 →