IP Library Granted Patent US 10,533,042
Granted Patent B2
US 10,533,042 · App. 15/835,290 · Granted Jan 14, 2020

Peptides and compositions for treatment of joint damage

Inventors: Kristen Johnson (Santee, CA); Jian Shi (San Diego, CA)
Assignee: NOVARTIS AG
C07K14/515A61K31/728A61K35/32A61K38/1709A61K38/1891A61K38/385A61K38/45A61K45/06C07K14/47C12N5/0655C12Q1/6883G01N33/6887A61K38/00C07K2319/30C12N2501/17C12N2506/1346C12Q2600/118C12Q2600/158G01N2333/78G01N2800/105G01N2800/52Y02A50/463
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Quick Facts
Patent No.
US 10,533,042
App. No.
15/835,290
Granted
Jan 14, 2020
Kind
B2
Abstract

The present invention provides new protease resistant polypeptides, as well as compositions and methods for treating, ameliorating or preventing conditions related to joint damage, including acute joint injury and arthritis.

Claims (20)

1. A method of inducing differentiation of mesenchymal stem cells into chondrocytes, the method comprising contacting mesenchymal stem cells with an effective amount of a polypeptide comprising an amino acid sequence that has at least 95% amino acid sequence identity to an amino acid sequence selected from TABLE 1, wherein the polypeptide comprises an amino acid that is a polar amino acid other than K or R at position 423, as determined with reference to SEQ ID NO:1, and wherein the polypeptide has chondrogenic activity.

2. The method of claim 1 , wherein the polypeptide comprises an amino acid sequence that has at least 95% sequence identity to an amino acid sequence selected from any one of SEQ ID NO:30, SEQ ID NO:31, SEQ ID NO:32, SEQ ID NO:33, SEQ ID NO:34, SEQ ID NO:35, SEQ ID NO:36, SEQ ID NO:37, SEQ ID NO:38, SEQ ID NO:39, SEQ ID NO:40, SEQ ID NO:41, SEQ ID NO:14, SEQ ID NO:15, SEQ ID NO:16, SEQ ID NO:17, SEQ ID NO:18, SEQ ID NO:19, SEQ ID NO:20, SEQ ID NO:21, SEQ ID NO:22, SEQ ID NO:23, SEQ ID NO:24, SEQ ID NO:25, SEQ ID NO:26, SEQ ID NO:27, SEQ ID NO:28, or SEQ ID NO:29.

3. The method of claim 1 , wherein the polypeptide comprises an amino acid sequence selected from any one of SEQ ID NO:30, SEQ ID NO:31, SEQ ID NO:32, SEQ ID NO:33, SEQ ID NO:34, SEQ ID NO:35, SEQ ID NO:36, SEQ ID NO:37, SEQ ID NO:38, SEQ ID NO:39, SEQ ID NO:40, SEQ ID NO:41, SEQ ID NO:14, SEQ ID NO:15, SEQ ID NO:16, SEQ ID NO:17, SEQ ID NO:19, SEQ ID NO:20, SEQ ID NO:21, SEQ ID NO:22, SEQ ID NO:24, SEQ ID NO:25, SEQ ID NO:26, SEQ ID NO:27, SEQ ID NO:28, or SEQ ID NO:29.

4. The method of claim 1 , wherein the polypeptide consists of an amino acid sequence that has at least 95% sequence identity to an amino acid sequence selected from any one of SEQ ID NO:30, SEQ ID NO:31, SEQ ID NO:32, SEQ ID NO:33, SEQ ID NO:34, SEQ ID NO:35, SEQ ID NO:36, SEQ ID NO:37, SEQ ID NO:38, SEQ ID NO:39, SEQ ID NO:40, or SEQ ID NO:41, SEQ ID NO:14, SEQ ID NO:15, SEQ ID NO:16, SEQ ID NO:17, SEQ ID NO:18, SEQ ID NO:19, SEQ ID NO:20, SEQ ID NO:21, SEQ ID NO:22, SEQ ID NO:23, SEQ ID NO:24, SEQ ID NO:25, SEQ ID NO:26, SEQ ID NO:27, SEQ ID NO:28, or SEQ ID NO:29.

5. The method of claim 1 , wherein the polypeptide consists of an amino acid sequence selected from any one of SEQ ID NO:30, SEQ ID NO:31, SEQ ID NO:32, SEQ ID NO:33, SEQ ID NO:34, SEQ ID NO:35, SEQ ID NO:36, SEQ ID NO:37, SEQ ID NO:38, SEQ ID NO:39, SEQ ID NO:40, or SEQ ID NO:41, SEQ ID NO:14, SEQ ID NO:15, SEQ ID NO:16, SEQ ID NO:17, SEQ ID NO:19, SEQ ID NO:20, SEQ ID NO:21, SEQ ID NO:22, SEQ ID NO:24, SEQ ID NO:25, SEQ ID NO:26, SEQ ID NO:27, SEQ ID NO:28, or SEQ ID NO:29.

6. The method of claim 1 , wherein the amino acid at position 423 of the polypeptide is Q or S.

7. The method of claim 1 , wherein the amino acid at position 423 of the polypeptide is Q.

8. The method of claim 1 , wherein the amino acid at position 423 of the polypeptide is S.

9. The method of claim 1 , wherein the polypeptide is PEGylated.

10. The method of claim 1 , wherein the polypeptide is fused to a heterologous peptide selected from any one of human serum albumin (HSA), an immunoglobulin heavy chain constant region (Fc), a polyhistidine, a glutathione S transferase (GST), a thioredoxin, a protein A, a protein G, or a maltose binding protein (MBP), or a fragment thereof.

11. The method of claim 1 , wherein the method is performed in vivo and the stem cells are present in a human subject, and wherein the polypeptide is administered to the joint of the subject.

12. The method of claim 11 , wherein the subject has arthritis.

13. The method of claim 11 , wherein the subject has articular cartilage damage.

14. The method of claim 12 , wherein the arthritis is osteoarthritis, trauma arthritis, or autoimmune arthritis.

15. The method of claim 12 , wherein the arthritis is osteoarthritis.

16. The method of claim 11 , further comprising administering to the subject one or more additional chondrogenic factors.

17. The method of claim 11 , further comprising administering to the subject hyaluronic acid or a derivative thereof.

18. The method of claim 11 , further comprising administering to the subject an agent selected from oral salmon calcitonin, SD-6010 (iNOS inhibitor), vitamin D3 (choliecalciferol), collagen hydrolyzate, FGF18, BMP7, rusalatide acetate, avocado soy unsaponifiables (ASU), kartogenin, a steroid, and a non-steroidal anti-inflammatory agent (NSAID).

19. The method of claim 11 , further comprising performing a surgical procedure to an affected joint in the subject.

20. The method of claim 11 , further comprising performing one or more procedures selected from bone marrow stimulation, cartilage replacement, autologous chondrocyte implantation (ACI), or matrix-induced autologous chondrocyte implantation (MACI), to the subject.

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 26, 2019
From: JOHNSON, KRISTEN; SHI, JIAN
To: NOVARTIS INSTITUTE FOR FUNCTIONAL GENOMICS, INC.
Reel/Frame 049586/0952 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 26, 2019
From: NOVARTIS INSTITUTE FOR FUNCTIONAL GENOMICS, INC.
To: IRM LLC.
Reel/Frame 049586/0986 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 26, 2019
From: JOHNSON, KRISTEN; SHI, JIAN
To: NOVARTIS INSTITUTE FOR FUNCTIONAL GENOMICS, INC.
Reel/Frame 049587/0015 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 26, 2019
From: NOVARTIS INSTITUTE FOR FUNCTIONAL GENOMICS, INC.
To: IRM LLC
Reel/Frame 049587/0046 →
MERGER Recorded Jun 26, 2019
From: IRM LLC
To: NOVARTIS INTERNATIONAL PHARMACEUTICAL LTD.
Reel/Frame 049587/0051 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 26, 2019
From: NOVARTIS INTERNATIONAL PHARMACEUTICAL LTD.
To: NOVARTIS AG
Reel/Frame 049587/0061 →
Continuity (4)
Division 15052029 · Feb 24, 2016
Division 14201694 · Mar 7, 2014
Provisional Application 61775400 · Mar 8, 2013
Related Publication 20180194823A1 · Jul 12, 2018