# US 12,758,609 B2 · Leuprolide acetate compositions and methods of using the same to treat breast cancer > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 12,758,609 B2 - Document ID: US12758609B2 - Status: Granted - Kind: B2 - Application number: 19/345,133 - Filed: 2025-09-30 - Published: 2026-01-29 - Granted: 2026-10-13 - Earliest claimed: 2019-05-27 - Assignees: Tolmar International Limited - Applicants: Tolmar International Limited - Inventors: John Middleton; Avinash Nangia; John Arthur McLane; Terri L. Morton - Web page: https://patentgrep.com/patent/US12758609B2 ## CPC - A61K 38/09: Luteinising hormone-releasing hormone [LHRH] {, i.e. Gonadotropin-releasing hormone [GnRH]}; Related peptides - A61K 9/0024: {Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue (compositions for intravenous administration, normal injectable solutions or dispersions for, e.g. subcutaneous administration A61K9/0019; brain implants A61K9/0085; (coated) prostheses, catheters or stents A61L)} - A61K 31/138: Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine (atenolol A61K31/165; pindolol A61K31/404; timolol A61K31/5377) - A61K 31/4196: 1,2,4-Triazoles - A61K 31/566: having an oxo group in position 17, e.g. estrone - A61K 47/22: Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones - A61K 47/34: Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence) - A61P 35/00: Antineoplastic agents - 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 Compositions and methods for suppressing ovarian function in subjects with hormone receptor-positive breast cancer. ## Claims ### Claim 1 An extended release composition for use in suppressing ovarian function during treatment of hormone receptor-positive breast cancer in pre- or peri-menopausal women, comprising a biodegradable polymer comprising co-polymer segments of poly(lactide-co-glycolide) (PLG) having a lactide to glycolide molar ratio of 70:30 to 80:20, no titratable carboxylic acid groups, and at least one distal end that is hydroxyl-terminated; N-methyl-2-pyrrolidone (NMP); and leuprolide or a pharmaceutically acceptable salt thereof, present in an amount to provide 26 mg to 30 mg of a free base equivalent of leuprolide; wherein the extended release composition has an injection volume of less than 0.5mL; wherein the extended release composition comprises 35-60% by weight of the biodegradable polymer and 50-60% by weight of NMP; and wherein the extended release composition is a 3-monthly formulation formulated to release up to 10 mg/mL leuprolide per month when administered subcutaneously every three months to pre-or peri-menopausal women with hormone receptor-positive breast cancer. ### Claim 2 (depends on 1) The extended release composition of claim 1, wherein the biodegradable polymer has a weight average molecular weight of from 15 kDa to 45 kDa. ### Claim 3 (depends on 1) The extended release composition of claim 1, wherein the biodegradable polymer has a weight average molecular weight of from 17 kDa to 21 kDa. ### Claim 4 (depends on 1) The extended release composition of claim 1, wherein the biodegradable polymer is 1,6-hexanediol-initiated. ### Claim 5 (depends on 1) The extended release composition of claim 1, wherein the biodegradable polymer has a lactide to glycolide molar ratio of 75:25. ### Claim 6 (depends on 1) The extended release composition of claim 1, wherein the biodegradable polymer has a formula wherein Ra is an alkane diradical comprising 4 to 8 carbons and P is a polymeric segment comprising units of lactide, glycolide, or (lactide-co-glycolide). ### Claim 7 (depends on 1) The extended release composition of claim 1, wherein the extended release composition comprises from 28 mg to 32 mg of leuprolide acetate. ### Claim 8 (depends on 1) The extended release composition of claim 1, wherein the extended release composition comprises 30 mg of leuprolide acetate. ### Claim 9 (depends on 1) The extended release composition of claim 1, wherein the extended release composition has an injection volume of 0.375 mL. ### Claim 10 A dual syringe system for use in suppressing ovarian function during treatment of hormone receptor-positive breast cancer in pre-or peri-menopausal women, comprising an extended release composition comprising a biodegradable polymer comprising co-polymer segments of poly(lactide-co-glycolide) (PLG) having a lactide to glycolide molar ratio of 70:30 to 80:20, no titratable carboxylic acid groups, and at least one distal end that is hydroxyl-terminated; N-methyl-2-pyrrolidone (NMP); and leuprolide or a pharmaceutically acceptable salt thereof, present in an amount to provide 26 mg to 30 mg of a free base equivalent of leuprolide; wherein a first syringe comprises the biodegradable polymer and NMP, and a second syringe comprises leuprolide or the pharmaceutically acceptable salt thereof; wherein the extended release composition in the dual syringe system has an injection volume of less than 0.5 mL; wherein the extended release composition comprises 35-60% by weight of the biodegradable polymer and 50-60% by weight of NMP; and wherein the extended release composition is a 3-monthly formulation formulated to release up to 10 mg/mL leuprolide per month when administered subcutaneously every three months to pre-or peri-menopausal women with hormone receptor-positive breast cancer. ### Claim 11 (depends on 10) The dual syringe system of claim 10, wherein the biodegradable polymer has a weight average molecular weight of from 15 kDa to 45 kDa. ### Claim 12 (depends on 10) The dual syringe system of claim 10, wherein the biodegradable polymer has a weight average molecular weight of from 17 kDa to 21 kDa. ### Claim 13 (depends on 10) The dual syringe system of claim 10, wherein the biodegradable polymer is 1,6-hexanediol-initiated. ### Claim 14 (depends on 10) The dual syringe system of claim 10, wherein the biodegradable polymer has a lactide to glycolide molar ratio of 75:25. ### Claim 15 (depends on 10) The dual syringe system of claim 10, wherein the biodegradable polymer has a formula wherein Ra is an alkane diradical comprising 4 to 8 carbons and P is a polymeric segment comprising units of lactide, glycolide, or (lactide-co-glycolide). ### Claim 16 (depends on 10) The dual syringe system of claim 10, wherein the extended release composition comprises from 28 mg to 32 mg of leuprolide acetate. ### Claim 17 (depends on 10) The dual syringe system of claim 10, wherein the extended release composition comprises 30 mg of leuprolide acetate. ### Claim 18 (depends on 10) The dual syringe system of claim 10, wherein the extended release composition in the dual syringe system has an injection volume of 0.375 mL. ### Claim 19 (depends on 10) A kit comprising the dual syringe system of claim 10 and instructions for using the dual syringe system to administer the extended release composition by subcutaneous injection for suppression of ovarian function during treatment of hormone receptor-positive (HR+) breast cancer in pre-or peri-menopausal women. ### Claim 20 (depends on 19) The kit of claim 19, wherein the instructions for using include instructions for administration to a pre-or peri-menopausal woman with HR+ breast cancer. ### Claim 21 (depends on 19) The kit of claim 19, wherein the instructions for using include instructions for administration of the extended release composition every three months to a pre-or peri-menopausal woman with HR+ breast cancer. ### Claim 22 (depends on 19) The kit of claim 19, wherein the instructions for using include instructions for mixing the contents of the first and second syringe together to form a flowable composition for administration to a subject. ### Claim 23 (depends on 19) The kit of claim 19, wherein the instructions for using describe administration of the extended release composition concurrently with tamoxifen or an aromatase inhibitor. ### Claim 24 (depends on 19) The kit of claim 19, wherein upon contact of the extended release composition with a bodily fluid, the NMP dissipates and an in situ solid or semi-solid depot forms.