# US 2026/0097014 A1 · Formulations of ag10

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- Number: US 2026/0097014 A1
- Document ID: US20260097014A1
- Status: Published application
- Kind: A1
- Application number: 19/417,131
- Filed: 2025-12-11
- Published: 2026-04-09
- Earliest claimed: 2018-08-17
- Assignees: Eidos Therapeutics, Inc.
- Applicants: Eidos Therapeutics, Inc.
- Inventors: Jesper JERNELIUS; Mark Michael MENNING
- Web page: https://patentgrep.com/patent/US20260097014A1

## CPC

- A61K 31/415: 1,2-Diazoles
- A61K 9/2009: {Inorganic compounds}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/2833: {Organic macromolecular compounds}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

The present disclosure provides high-load tablet formulations of AG10 or a pharmaceutically acceptable salt thereof. In some aspects, provided herein are table formulations of AG10 or a pharmaceutically acceptable salt thereof that include at least 40% or more AG10 by weight and at least one pharmaceutical excipient selected from one or more fillers, one or more binders, one or more disintegrants, and one or more lubricants.

## Claims

### Claim 1

A tablet formulation comprising AG10 or a pharmaceutically acceptable salt thereof and at least one pharmaceutical excipient selected from one or more fillers, one or more binders, one or more disintegrants, and one or more lubricants, wherein
said tablet comprises at least 40% or more by weight of AG10 or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The tablet formulation of claim 1, comprising about 40 to 85% by weight of AG10 or a pharmaceutically acceptable salt thereof.

### Claim 3 (depends on 1)

The tablet formulation of claim 1, comprising about 50 to 75% by weight of AG10 or a pharmaceutically acceptable salt thereof.

### Claim 4 (depends on 1)

The tablet formulation of claim 1, comprising about 50% by weight of AG10 or a pharmaceutically acceptable salt thereof.

### Claim 5 (depends on 1)

The tablet formulation of claim 1, comprising about 66.7% by weight of AG10 or a pharmaceutically acceptable salt thereof.

### Claim 6 (depends on 1)

The tablet formulation of claim 1, comprising about 75% by weight of AG10 or a pharmaceutically acceptable salt thereof.

### Claim 7 (depends on 1, 2, 3, 4, 5, 6)

The tablet formulation of any one of claims 1 to 6, comprising about 1 to 60% by weight of one or more fillers.

### Claim 8 (depends on 7)

The tablet formulation of claim 7, wherein said one or more fillers comprises about 5 to 55% by weight of said tablet formulation.

### Claim 9 (depends on 7)

The tablet formulation of claim 7, wherein said one or more fillers comprises about 10 to 50% by weight of said tablet formulation.

### Claim 10 (depends on 7)

The tablet formulation of claim 7, wherein said one or more fillers comprises about 15 to 45% by weight of said tablet formulation.

### Claim 11 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10)

The tablet formulation of any one of claims 1 to 10, wherein said tablet comprises a high grade microcrystalline cellulose as a filler component.

### Claim 12 (depends on 11)

The tablet formulation of claim 11, wherein said high grade microcrystalline cellulose is characterized by cellulose polymers with spherical morphology and porous structure.

### Claim 13 (depends on 12)

The tablet formulation of claim 12, wherein said high grade microcrystalline cellulose is selected from the group consisting of UF-702 and UF-711.

### Claim 14 (depends on 11)

The tablet formulation of claim 11, wherein said high grade microcrystalline cellulose is characterized by cellulose polymers with needle-like particle shape.

### Claim 15 (depends on 14)

The tablet formulation of claim 14, wherein said high grade microcrystalline cellulose is selected from the group consisting of KG-802 and KG-1000.

### Claim 16 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10)

The tablet formulation of any one of claims 1 to 10, wherein said one or more fillers are selected from a cellulose derivative and an inorganic salt.

### Claim 17 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10)

The tablet formulation of any one of claims 1 to 10, wherein said one or more fillers are microcrystalline cellulose and silicon dioxide.

### Claim 18 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17)

The tablet formulation of any one of claims 1 to 17, comprising about 1 to about 15% by weight of one or more disintegrants.

### Claim 19 (depends on 18)

The tablet formulation of claim 18, wherein said one or more disintegrants comprises about 3 to 8% by weight of said tablet formulation.

### Claim 20 (depends on 18)

The tablet formulation of claim 18, wherein said one or more disintegrants comprises about 6% by weight of said tablet formulation.

### Claim 21 (depends on 18, 19, 20)

The tablet formulation of any one of claims 18 to 20, wherein said one or more disintegrants is croscarmellose sodium.

### Claim 22 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21)

The tablet formulation of any one of claims 1 to 21, comprising about 0.1 to 8% by weight of a lubricant.

### Claim 23 (depends on 22)

The tablet formulation of claim 22, wherein said one or more lubricants comprises about 1.5% by weight of said tablet formulation.

### Claim 24 (depends on 22, 23)

The tablet formulation of claim 22 or claim 23, wherein said one or more lubricants is magnesium stearate.

### Claim 25 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24)

The tablet formulation of any one of claims 1 to 24, wherein said tablet is at least 75% dissolved after 10 minutes in a solution of 0.1N HCl at 37±0.5° C. in an Apparatus-II (Paddles) with a paddle speed of about 50 rpm.

### Claim 26 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24)

The tablet formulation of any one of claims 1 to 24, wherein said tablet is at least 85% dissolved after 10 minutes in a solution of 0.1N HCl at 37±0.5° C. in an Apparatus-II (Paddles) with a paddle speed of about 50 rpm.

### Claim 27 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24)

The tablet formulation of any one of claims 1 to 24, wherein said tablet is at least 95% dissolved after 10 minutes in a solution of 0.1N HCl at 37±0.5° C. in an Apparatus-II (Paddles) with a paddle speed of about 50 rpm.

### Claim 28 (depends on 25, 26, 27)

The tablet formulation of any one of claims 25 to 27, wherein said tablet was prepared at least three months before performing the dissolution test.

### Claim 29 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28)

The tablet formulation of any one of claims 1 to 28, further comprising a coating agent.

### Claim 30 (depends on 29)

The tablet formulation of claim 29, wherein said coating agent is Opadry QX 321A180025.

### Claim 31 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30)

The tablet formulation of any one of claims 1 to 30, wherein AG10 is the pharmaceutically acceptable salt form of Formula Ia
