Granted Patent
B2
US 12,539,290 · App. 18/650,542 · Granted Feb 3, 2026
Formulations of AG10
Assignee:
EIDOS THERAPEUTICS, INC.
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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 (46)
1 . A table formulation comprising:
a. a core comprising:
about 400 milligram (mg) of 3-(3-(3,5-dimethyl-1H-pyrazol-4-yl) propoxy)-4-fluorobenzoic acid hydrochloride; and
about 1% to about 60% by weight microcrystalline cellulose, wherein the microcrystalline cellulose is UF-702, UF-711, KG-802, KG-1000, or a combination thereof; and
b. optionally, a coating,
wherein the total weight of the core is about 470 mg to about 1000 mg.
2 . The tablet formulation of claim 1 , wherein the core comprises about 5% to about 55% by weight microcrystalline cellulose.
3 . The tablets formulation of claim 1 , wherein the core comprises about 10% to about 50% by weight microcrystalline cellulose.
4 . The tablet formulation of claim 3 , wherein the total weight of the core is about 533 mg to about 800 mg.
5 . The tablet formulation of claim 1 , wherein the core comprises about 15% to about 45% by weight microcrystalline cellulose.
6 . The tablets formulation of claim 5 , wherein the total weight of the core is about 533 mg to about 800 mg.
7 . The tablet formulation of claim 1 , wherein the core comprises about 26% by weight microcrystalline cellulose.
8 . The tablet formulation of claim 1 , wherein the total weight of the core is about 600 mg.
9 . The tablet formulation of claim 8 , wherein the core comprises:
about 400 mg of 3-(3-(3,5-dimethyl-1H-pyrazol-4-yl) propoxy)-4-fluorobenzoic hydrochloride;
about 153.5 mg of the microcrystalline cellulose;
about 36 mg of croscarmellose sodium;
about 1.5 mg of silicon dioxide; and
about 9 mg of magnesium stearate.
10 . The tablet formulation of claim 1 , wherein the tablet formulation is at least 75% dissolved after performance of a dissolution test in a solution of 0.1 N HCl at 37±0.5° C. in an Apparatus-II (Paddles) with a paddle speed of about 50 RPM for 10 minutes.
11 . The tablet formulation of claim 10 , wherein the dissolution test is performed at least three months after preparation of the tablet formulation.
12 . The tablet formulation of claim 10 , wherein the dissolution test is performed at least six months after preparation of the tablet formulation.
13 . The tablet formulation of claim 9 , wherein the tablet formulation is at least 75% dissolved after performance of a dissolution test in a solution of 0.1 N HCl at 37±0.5° C. in an Apparatus-II (Paddles) with a paddle speed of about 50 RPM for 10 minutes.
14 . The tablet formulation of claim 13 , wherein the dissolution test is performed at least three months after preparation of the tablet formulation.
15 . The tablet formulation of claim 13 , wherein the dissolution test is performed at least six months after preparation of the tablet formulation.
16 . The tablet formulation of claim 1 , wherein the tablet formulation is at least 75% dissolved after performance of a dissolution test in 900 mL of a solution of 0.1 N HCl at 37±0.5° C. in an Apparatus-II (Paddles) with a paddle speed of about 75 RPM for 10 minutes.
17 . The tablet formulation of claim 16 , wherein the dissolution test is performed at least three months after preparation of the tablet formulation.
18 . The tablet formulation of claim 16 , wherein the dissolution test is performed at least six months after preparation of the tablet formulation.
19 . The tablet formulation of claim 9 , wherein the tablet formulation is at least 75% dissolved after performance of a dissolution test in 900 mL of a solution of 0.1 N HCl at 37±0.5° C. in an Apparatus-II (Paddles) with a paddle speed of about 75 RPM for 10 minutes.
20 . The tablet formulation of claim 19 , wherein the dissolution test is performed at least three months after preparation of the tablet formulation.
21 . The tablet formulation of claim 19 , wherein the dissolution test is performed at least six months after preparation of the tablet formulation.
22 . The tablet formulation of claim 1 , wherein the coating is present in an amount of about 4% by weight of the core.
23 . The tablet formulation of claim 9 , wherein the coating is present in an amount of about 4% by weight of the core.
24 . The tablet formulation of claim 1 , wherein the microcrystalline cellulose is UF-711.
25 . The tablet formulation of claim 9 , wherein the microcrystalline cellulose is UF-711.
26 . A tablet formulation comprising an intragranular portion, an extragranular portion, and optionally, a coating, wherein
the intragranular portion comprises:
about 400.0 milligrams (mg) of 3-(3-(3,5-dimethyl-1H-pyrazol-4-yl) propoxy)-4-fluorobenzoic acid hydrochloride;
about 93.5 mg of UF-711;
about 18.0 mg of croscarmellose sodium;
about 1.5 mg of silicon dioxide; and
about 4.5 mg of magnesium stearate; and
the extragranular portion comprises:
about 60.0 mg of UF-711;
about 18.0 mg of croscarmellose sodium; and
about 4.5 mg of magnesium stearate.
Assignments (2)
SECURITY INTEREST
Recorded Sep 8, 2025
From: EIDOS THERAPEUTICS, INC.
To: ALTER DOMUS (US) LLC, AS COLLATERAL AGENT
Reel/Frame 072186/0031 →
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Nov 7, 2024
From: JERNELIUS, JESPER; MENNING, MARK MICHAEL
To: EIDOS THERAPEUTICS, INC.
Reel/Frame 069187/0226 →
Continuity (4)
Provisional Application
62765154
· Aug 17, 2018
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