IP Library Granted Patent US 10,624,958
Granted Patent B2
US 10,624,958 · App. 16/033,948 · Granted Apr 21, 2020

Compositions and methods for treating pathological calcification and ossification

Inventors: Demetrios Braddock (Guilford, CT); Ronald Albright (Guilford, CT)
Assignee: Yale University
A61K38/465A61K38/46C12N9/14C12N9/16C12Y301/04001C12Y306/01009C07K2319/30
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Quick Facts
Patent No.
US 10,624,958
App. No.
16/033,948
Granted
Apr 21, 2020
Kind
B2
Abstract

The present invention includes compositions and methods for treating disease and disorders associated with pathological calcification or pathological ossification by modulating the level or activity of NPP1 or a mutant thereof, or a mutant NPP4 modified to exhibit ATP hydrolase activity similar to the hydrolase activity of NPP1.

Claims (25)

1. A method of treating, reversing, or preventing progression of ossification of the posterior longitudinal ligament (OPLL) in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of a soluble ecto-nucleotide pyrophosphate/phosphodiesterase-1 (ENPP1) polypeptide, wherein the soluble ENPP1 polypeptide lacks a targeting domain, whereby ossification of the posterior longitudinal ligament (OPLL) in the subject is reduced or its progression is prevented or reversed.

2. The method of claim 1 , wherein the soluble ENPP1 polypeptide comprises the somatomedin B, catalytic, and nuclease domains of ENPP1.

3. The method of claim 1 , wherein the soluble ENPP1 polypeptide comprises residues 96-925 of human ENPP1 (SEQ ID NO: 1).

4. The method of claim 1 , wherein the soluble ENPP1 polypeptide is a cleavage product of a precursor ENPP1 polypeptide comprising an ecto-nucleotide pyrophosphate/phosphodiesterase-2 (ENPP2) signal sequence.

5. The method of claim 1 , wherein the soluble ENPP1 polypeptide is a cleavage product of a precursor ENPP1 polypeptide comprising residues 12-30 of ENPP2 (SEQ ID NO: 2) N-terminal to the somatomedin B, catalytic, and nuclease domains of ENPP1.

6. The method of claim 1 , wherein the soluble ENPP1 polypeptide is a cleavage product of a precursor ENPP1 polypeptide lacking residues 77-98 of the ENPP1 transmembrane domain and comprising a signal sequence.

7. The method of claim 1 , wherein the soluble ENPP1 polypeptide is a cleavage product of a precursor ENPP1 polypeptide comprising residues 1-76 of ENPP1 (SEQ ID NO: 1), residues 12-30 of ENPP2 (SEQ ID NO: 2), and residues 96-925 of ENPP1 sequence (SEQ ID NO: 1), wherein the precursor undergoes proteolytic processing to soluble ENPP1.

8. The method of claim 1 , wherein the targeting domain comprises 2 to 20 sequential aspartic acid residues.

9. The method of claim 1 , wherein the soluble ENPP1 polypeptide is a fusion protein comprising a fusion partner comprising an IgG Fc domain.

10. The method of claim 1 , wherein the soluble ENPP1 polypeptide has ATP hydrolytic activity.

11. The method of claim 1 , wherein the soluble ENPP1 polypeptide is administered acutely or chronically.

12. The method of claim 1 , wherein the soluble ENPP1 polypeptide is administered locally, regionally, parenterally, or systemically.

13. The method of claim 1 , wherein the subject is human.

14. A method of treating, reverting, or preventing progression of hypophosphatemic rickets in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of a soluble ecto-nucleotide pyrophosphate/phosphodiesterase-1 (ENPP1) polypeptide, wherein the soluble ENPP1 lacks a targeting domain, whereby hypophosphatemic rickets in the subject is reduced or its progression is prevented or reversed.

15. The method of claim 14 , wherein the soluble ENPP1 polypeptide comprises the somatomedin B, catalytic, and nuclease domains of ENPP1.

16. The method of claim 14 , wherein the soluble ENPP1 polypeptide comprises residues 96-925 of human ENPP1 (SEQ ID NO: 1).

17. The method of claim 14 , wherein the soluble ENPP1 polypeptide is a cleavage product of a precursor ENPP1 polypeptide comprising an ecto-nucleotide pyrophosphate/phosphodiesterase-2 (ENPP2) signal sequence.

18. The method of claim 14 , wherein the soluble ENPP1 polypeptide is a cleavage product of a precursor ENPP1 polypeptide comprising residues 12-30 of ENPP2 (SEQ ID NO: 2) N-terminal to the somatomedin B, catalytic, and nuclease domains of ENPP1.

19. The method of claim 14 , wherein the soluble ENPP1 polypeptide is a cleavage product of a precursor ENPP1 polypeptide lacking residues 77-98 of the ENPP1 transmembrane domain and comprising a signal sequence.

20. The method of claim 14 , wherein the soluble ENPP1 polypeptide is a cleavage product of a precursor ENPP1 polypeptide comprising residues 1-76 of ENPP1 (SEQ ID NO: 1), residues 12-30 of ENPP2 (SEQ ID NO: 2), and residues 96-925 of ENPP1 sequence (SEQ ID NO: 1), wherein the precursor undergoes proteolytic processing to soluble ENPP1.

21. The method of claim 14 , wherein the targeting domain comprises 2 to 20 sequential aspartic acid residues.

22. The method of claim 14 , wherein the soluble ENPP1 polypeptide is a fusion protein comprising a fusion partner comprising an IgG Fc domain.

23. The method of claim 14 , wherein the soluble ENPP1 polypeptide has ATP hydrolytic activity.

24. The method of claim 14 , wherein the soluble ENPP1 polypeptide is administered acutely or chronically.

25. The method of claim 14 , wherein the soluble ENPP1 polypeptide is administered locally, regionally, parenterally, or systemically.

Assignments (1)
SECURITY INTEREST Recorded Apr 27, 2026
From: BIOMARIN PHARMACEUTICAL INC.; AMICUS THERAPEUTICS, INC.
To: CITIBANK, N.A., AS COLLATERAL AGENT
Reel/Frame 075493/0968 →
Continuity (5)
Continuation 15686972 · Aug 25, 2017
Continuation 14765541
Provisional Application 61904786 · Nov 15, 2013
Provisional Application 61764297 · Feb 13, 2013
Related Publication 20180318401A1 · Nov 8, 2018
Cited By (3)
US 12,344,868 US 12,589,137 US 12,698,487