Granted Patent B2

US 12,472,147 · App. 18/185,584 · Granted Nov 18, 2025

Inventors: Andrew Bristol (Rockville, MD); Ray Stapleton (Rockville, MD); Michael Kaleko (Rockville, MD); Christian Furlan Freguia (Rockville, MD); Steven Hubert (Rockville, MD); Cristina Freire (Rockville, MD); James Gubbins (Rockville, MD)

Assignee: Theriva Biologics, Inc.

A61K9/2846A61K9/19A61K9/2009A61K9/2013A61K9/2018A61K9/2027A61K9/2054A61K9/2095A61K9/2866A61K9/2886A61K9/2893A61K38/465C12N9/16C12Y301/03001C12N15/52C12N15/63

Abstract

Claims (30)

1 . A pharmaceutical formulation in the form of a tablet comprising:

37-43% by weight alkaline phosphatase (AP)-based agent, wherein the AP-based agent comprises an amino acid sequence at least 95% identical to the amino acid sequences set forth in SEQ ID NOs: 1-17;

37-43% by weight sugar;

6-12% by weight buffer salts;

7-13% by weight Ludipress (lactose, povidone, and crospovidone); and

0.5-1.5% by weight magnesium stearate,

and a pharmaceutical acceptable carrier or vehicle.

2 . The formulation of claim 1 , further comprising an enteric coating.

3 . The formulation of claim 2 , wherein the enteric coating comprises Eudragit L 30 D 55 (poly(methacrylic acid-ethyl acrylate copolymer) 1:1).

4 . The formulation of claim 1 , further comprising two coatings.

5 . The formulation of claim 4 , wherein the first coating comprises a HPC subcoat and the second coating comprises an enteric coating.

6 . The formulation of claim 5 , wherein the enteric coating comprises Eudragit L 30 D 55 (poly(methacrylic acid-ethyl acrylate copolymer) 1:1).

7 . A formulation in the form of a tablet comprising:

40% by weight alkaline phosphatase (AP)-based agent, wherein the AP-based agent comprises an amino acid sequence at least 95% identical to the amino acid sequences set forth in SEQ ID NOs: 1-17;

40% by weight sugar;

9% by weight buffer salts;

10% by weight Ludipress (lactose, povidone, and crospovidone); and

1% by weight magnesium stearate,

and a pharmaceutical acceptable carrier or vehicle.

8 . The formulation of claim 7 , further comprising an enteric coating.

9 . The formulation of claim 8 , wherein the enteric coating comprises Eudragit L 30 D 55 (poly(methacrylic acid-ethyl acrylate copolymer) 1:1).

10 . The formulation of claim 7 , further comprising two coatings.

11 . The formulation of claim 10 , wherein the first coating comprises a HPC subcoat and the second coating comprises an enteric coating.

12 . The formulation of claim 11 , wherein the enteric coating comprises Eudragit L 30 D 55 (poly(methacrylic acid-ethyl acrylate copolymer) 1:1).

13 . The formulation of claim 1 , wherein the AP-based agent is intestinal alkaline phosphatase (IAP).

14 . The formulation of claim 1 , wherein the AP-based agent comprises an amino acid sequence having at least 95% identity with SEQ ID NO: 2.

15 . The formulation of claim 1 , wherein at least 40% of the AP-based agent is released within 30 minutes.

16 . The formulation of claim 1 , wherein the activity of the AP-based agent is maintained at least at 60% until 36 weeks of storage.

17 . The formulation of claim 1 , wherein the sugar is sucrose.

18 . The formulation of claim 1 , wherein the buffer salts are one or more of Tris, MgCl 2 , and ZnSO 4 .

Assignments (4)

Continuity (3)

References Cited (158)