IP Library › Granted Patent US 12,233,115
Granted Patent B2
US 12,233,115 · App. 18/368,347 · Granted Feb 25, 2025

Long-acting parathyroid hormone

Inventors: Tarik Soliman (Cambridge, MA); Daniel B. Hall (Easton, MA); Rachel Covitz (Allston, MA); Garry Musso (Harwich, MA); Caroline Hill (Jamaica Plain, MA); Ahmet Vakkasoglu (Stoneham, MA); Poul Strange (Princeton Junction, NJ); Tilmann M. Brotz (Berkeley, CA)
Assignee: Extend Biosciences, Inc.
A61K38/29A61K47/551A61K47/60
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Quick Facts
Patent No.
US 12,233,115
App. No.
18/368,347
Granted
Feb 25, 2025
Kind
B2
Abstract

The invention provides a long-acting parathyroid hormone peptide (PTH) that is retained in a subject's blood serum for periods of time that greatly exceed the natural hormone. The long-acting PTH is conjugated to at the carbon 3 position of a non-hormonal vitamin D via a scaffold of discreet length that facilitates its purification, detection, solubility, and efficacy at the PTH receptor (PTHR). The PTH may be conjugated to the non-hormonal vitamin D via a 36 mer poly(ethylene glycol) moiety (PTH-PEG36-VitD). The invention also provides optimized manufacturing methods and formulations. The PTH-PEG36-VitD has a vastly-improved serum half-life and bioavailability when compared to a non-conjugated PTH peptide. PTH-PEG36-VitD also significantly increases serum calcium, reduces urinary calcium, and reduces serum phosphate.

Claims (13)

1. A pharmaceutical composition comprising one or more parathyroid hormone 1-34 (PTH(1-34)) peptide(s) conjugated via a poly(ethylene glycol) (PEG) scaffold to a non-hormonal vitamin D moiety at the carbon 3 position (PTH conjugate); wherein the scaffold is not conjugated to an amine group of the PTH(1-34); wherein the PEG scaffold consist of 36 subunits at a molecular weight of 1,584 Daltons; wherein the PTH conjugate consists of the acetate salt of

and wherein the composition comprises a pharmaceutically acceptable excipient.

2. The pharmaceutical composition of claim 1 , wherein said pharmaceutical composition further comprises mannitol.

3. The pharmaceutical composition of claim 1 , wherein said pharmaceutical composition further comprises Polysorbate 80 (PS80).

4. The pharmaceutical composition of claim 1 , wherein said pharmaceutical composition further comprises methionine at a concentration of between about 0 and 40 mM+/−5 mM.

5. The pharmaceutical composition of claim 1 comprising 10 mM sodium acetate buffer (+/−10%); 3.0% to 4.5% mannitol; 0% to 0.25% Polysorbate 80; and 0 mM to 40 mM methionine.

6. The pharmaceutical composition of claim 1 , wherein said pharmaceutical composition has a pH of about 5.5, and wherein said pharmaceutical composition comprises mannitol and PS80.

7. The pharmaceutical composition of claim 6 , wherein said PTH conjugate is at a concentration of 0.4 mg/ml in about 10 mM sodium acetate buffer (+/−10%), pH about 5.5, about 4.5% mannitol (+/−1.5%), and about 0.25% Polysorbate 80 (+/−0.25%).

8. The pharmaceutical composition of claim 7 , further comprising 0 mM to 40 mM methionine (+/−5 mM).

9. The pharmaceutical composition of claim 7 , further comprising 40 mM methionine (+/−5 mM).

10. The pharmaceutical composition of claim 1 , wherein said pharmaceutical composition has a pH of about 4.0 to about 5.5.

11. The pharmaceutical composition of claim 1 , wherein said pharmaceutical composition has a pH of about 4.0.

12. The pharmaceutical composition of claim 10 , wherein said pharmaceutical composition has a pH of about 5.5.

Assignments (7)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 4, 2025
From: SOLIMAN, TARIK; HALL, DANIEL B.; COVITZ, RACHEL; HILL, CAROLINE; VAKKASOGLU, AHMET
To: EXTEND BIOSCIENCES, INC.
Reel/Frame 069747/0605 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 4, 2025
From: PHARMADIRECTIONS, INC.
To: EXTEND BIOSCIENCES, INC.
Reel/Frame 069747/0639 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 4, 2025
From: STRANGE, POUL
To: PHASE 1 TO 4, LLC
Reel/Frame 069747/0655 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 4, 2025
From: PHASE 1 TO 4, LLC
To: EXTEND BIOSCIENCES, INC.
Reel/Frame 069747/0668 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 4, 2025
From: MUSSO, GARY
To: MUSSO AND ASSOCIATES LLC
Reel/Frame 069747/0672 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 4, 2025
From: MUSSO AND ASSOCIATES LLC
To: EXTEND BIOSCIENCES, INC.
Reel/Frame 069747/0678 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 4, 2025
From: BROTZ, TILMANN M.
To: PHARMADIRECTIONS, INC.
Reel/Frame 069819/0396 →
Continuity (3)
Provisional Application 63464495 · May 5, 2023
Provisional Application 63412291 · Sep 30, 2022
Related Publication 20240139289A1 · May 2, 2024
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