# US 12,599,590 B2 · Veterinary formulations comprising rapamycin and methods of using the same for treating animal disease > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 12,599,590 B2 - Document ID: US12599590B2 - Status: Granted - Kind: B2 - Application number: 17/777,800 - Filed: 2020-12-18 - Published: 2022-12-22 - Granted: 2026-04-14 - Earliest claimed: 2019-12-19 - Assignees: TriviumVet DAC - Applicants: TriviumVet DAC - Inventors: Tom Brennan; Louise Grubb; Liam Byrne; Stuart Fitzgerald - Web page: https://patentgrep.com/patent/US12599590B2 ## CPC - A61K 31/436: the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin - A61P 9/00: Drugs for disorders of the cardiovascular system - A61K 9/2013: {Organic compounds, e.g. phospholipids, fats} - A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates} - A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates} - A61K 9/2031: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers} - A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 9/2077: {Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets} - A61K 9/2813: {Inorganic compounds} - A61K 9/282: {Organic compounds, e.g. fats} - A61K 9/2846: {Poly(meth)acrylates} - A61K 31/675: having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate - 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) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract The present disclosure provides veterinary formulations comprising rapamycin or rapalogs for administration to companion animals and methods of using the formulations to treat cardiac dysfunction, including hypertrophic cardiomyopathy, dilated cardiomyopathy, mitral valve disease, pressure-overload cardiac hypertrophy, cancer, effects of aging, inflammatory disease, and viral infection. ## Claims ### Claim 1 A method for treating hypertrophic cardiomyopathy, dilated cardiomyopathy, mitral valve disease, or pressure-overload cardiac hypertrophy in companion animals, the method comprising: administering to the companion animal in need thereof a composition comprising; an intra-granular part comprising rapamycin, rapalog, or a salt thereof in a dispersion comprising a binder, and a polymer, an extra-granular part comprising a polymer, and a delayed release coating, wherein the composition is administered to the companion animal once per week at a dosing amount of the rapamycin, rapalog, or salt thereof from about 0.025 mg/kg to about 0.75 mg/kg. ### Claim 2 (depends on 1) The method of claim 1, wherein rapamycin, or salt thereof, is administered. ### Claim 3 (depends on 1) The method of claim 1, wherein the rapalog is selected from the group consisting of temsirolimus, everolimus, and ridaforolimus. ### Claim 4 (depends on 1) The method of claim 1, wherein the composition comprises a coating comprising methacrylic acid ethyl acrylate copolymer, talc, titanium dioxide, triethyl citrate, colloidal anhydrous silica, sodium bicarbonate, sodium lauryl sulfate and, one or more colorants. ### Claim 5 (depends on 1) The method of claim 1, wherein the polymer of the rapamycin dispersion and the polymer of the extra-granular part are independently selected from the group consisting of microcrystalline cellulose, hydroxypropyl methylcellulose, polyvinyl pyrrolidone, crospovidone, povidone, polyplasdone, and combinations thereof. ### Claim 6 (depends on 1) The method of claim 1, wherein the binder is selected from the group consisting of poloxamer, glyceryl mono-oleate, alpha-DL-tocopheryl acetate, povidone, citric acid anhydrous, and combinations thereof. ### Claim 7 (depends on 1) The method of claim 1, wherein the dispersion further comprises a sugar. ### Claim 8 (depends on 1) The method of claim 1, wherein the dispersion comprises microcrystalline cellulose, poloxamer, and tocopheryl acetate. ### Claim 9 (depends on 8) The method of claim 8, wherein the dispersion further comprises sucrose, glyceryl mono-oleate, povidone K-30, and citric acid anhydrous. ### Claim 10 (depends on 1) The method of claim 1, wherein the dispersion has a D90 of about 2 to about 30 pm. ### Claim 11 (depends on 10) The method of claim 10, wherein the dispersion has a D90 of about 2 pm to about 5 pm. ### Claim 12 (depends on 1) The method of claim 1, wherein the extra-granular part comprises microcrystalline cellulose, crospovidone, and talc. ### Claim 13 (depends on 1) The method of claim 1, wherein the composition comprises about 1% to about 10% binder, about 40% to about 75% polymer, and about 20% to about 40% sugar, based on the total weight of the composition. ### Claim 14 (depends on 1) The method of claim 1, wherein the intra-granular part comprises rapamycin, rapalog, or a salt thereof, microcrystalline cellulose, crospovidone, and sucrose, wherein the binder comprises poloxamer, glyceryl mono-oleate, alpha-DL-tocopheryl acetate, povidone K-30, or citric acid anhydrous; wherein the extra-granular part comprises microcrystalline cellulose, crospovidone, and talc; and wherein the composition further comprises a coating comprising methacrylic acid ethyl acrylate copolymer, talc, titanium dioxide, triethyl citrate, colloidal anhydrous silica, sodium bicarbonate, sodium lauryl sulfate and, one or more colorants. ### Claim 15 (depends on 1) The method of claim 1, wherein the companion animal is a dog or a cat.