# US 12,005,043 B2 · Formulations of AG10 > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 12,005,043 B2 - Document ID: US12005043B2 - Status: Granted - Kind: B2 - Application number: 17/577,479 - Filed: 2022-01-18 - Published: 2022-10-06 - Granted: 2024-06-11 - 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/US12005043B2 ## 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 one or more fillers, one or more disintegrants, and one or more lubricants, wherein said tablet formulation comprises: 40 to 85% by weight of AG10 or a pharmaceutically acceptable salt thereof; 5 to 55% by weight of said one or more fillers; 3 to 8% by weight of said one or more disintegrants; and 0.5 to 3% by weight of said one or more lubricants, and wherein said one or more fillers comprise a high-grade microcrystalline cellulose characterized by cellulose polymers with (i) spherical morphology and porous structure or (ii) needle-like particle shape. ### Claim 2 (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 3 (depends on 1) The tablet formulation of claim 1, comprising about 50% by weight of AG10 or a pharmaceutically acceptable salt thereof. ### Claim 4 (depends on 1) The tablet formulation of claim 1, comprising about 66.7% by weight of AG10 or a pharmaceutically acceptable salt thereof. ### Claim 5 (depends on 1) The tablet formulation of claim 1, comprising about 75% by weight of AG10 or a pharmaceutically acceptable salt thereof. ### Claim 6 (depends on 1) The tablet formulation of claim 1, wherein said one or more fillers comprises about 10 to 50% by weight of said tablet formulation. ### Claim 7 (depends on 1) The tablet formulation of claim 1, wherein said one or more fillers comprises about 15 to 45% by weight of said tablet formulation. ### Claim 8 (depends on 1) The tablet formulation of claim 1, wherein said one or more fillers further comprise silicon dioxide. ### Claim 9 (depends on 1) The tablet formulation of claim 1, wherein said one or more disintegrants comprises about 6% by weight of said tablet formulation. ### Claim 10 (depends on 1) The tablet formulation of claim 1, wherein said one or more disintegrants is croscarmellose sodium. ### Claim 11 (depends on 1) The tablet formulation of claim 1, wherein said one or more lubricants comprises about 1.5% by weight of said tablet formulation. ### Claim 12 (depends on 11) The tablet formulation of claim 11, wherein said one or more lubricants comprise magnesium stearate. ### Claim 13 (depends on 1) The tablet formulation of claim 1, wherein said tablet formulation is at least 75% dissolved after performance of a dissolution test 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 for 10 minutes. ### Claim 14 (depends on 13) The tablet formulation of claim 13, wherein said tablet formulation is at least 85% dissolved after performance of said dissolution. ### Claim 15 (depends on 14) The tablet formulation of claim 14, wherein said tablet formulation is at least 95% dissolved after performance of said dissolution. ### Claim 16 (depends on 13) The tablet formulation of claim 13, wherein said dissolution test is performed at least three months after preparation of said tablet formulation. ### Claim 17 (depends on 1) The tablet formulation of claim 1, further comprising a coating agent. ### Claim 18 (depends on 1) The tablet formulation of claim 1, wherein AG10 is the pharmaceutically acceptable salt form of Formula Ia ### Claim 19 (depends on 1) A method of treating transthyretin amyloid (ATTR) cardiomyopathy comprising administering a tablet formulation of claim 1. ### Claim 20 (depends on 1) A method of treating transthyretin amyloid (ATTR) polyneuropathy comprising administering a tablet formulation of claim 1. ### Claim 21 (depends on 1) The tablet formulation of claim 1, wherein said one or more fillers comprises about 25.8% by weight of said tablet formulation. ### Claim 22 (depends on 1) The tablet formulation of claim 1, wherein said one or more fillers comprises about 42.5% by weight of said tablet formulation. ### Claim 23 A tablet formulation comprising AG10 or a pharmaceutically acceptable salt thereof and one or more fillers, one or more disintegrants, and one or more lubricants, wherein said tablet formulation comprises: 50 to 75% by weight of AG10 or a pharmaceutically acceptable salt thereof; 15 to 45% by weight of said one or more fillers; 3 to 8% by weight of said one or more disintegrants; and 0.5 to 3% by weight of said one or more lubricants, and wherein said one or more fillers comprise a high-grade microcrystalline cellulose characterized by cellulose polymers with (i) spherical morphology and porous structure or (ii) needle-like particle shape. ### Claim 24 (depends on 23) The tablet formulation of claim 23, wherein AG10 is the pharmaceutically acceptable salt form of Formula Ia ### Claim 25 (depends on 23) A method of treating transthyretin amyloid (ATTR) cardiomyopathy comprising administering a tablet formulation of claim 23. ### Claim 26 (depends on 23) A method of treating transthyretin amyloid (ATTR) polyneuropathy comprising administering a tablet formulation of claim 23.