# US 2023/0404918 A1 · Fulvestrant formulations and methods of their use > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2023/0404918 A1 - Document ID: US20230404918A1 - Status: Published application - Kind: A1 - Application number: 18/109,421 - Filed: 2023-02-14 - Published: 2023-12-21 - Earliest claimed: 2017-11-08 - Assignees: Eagle Pharmaceuticals, Inc. - Applicants: Eagle Pharmaceuticals, Inc. - Inventors: Feng-Jing CHEN; Steven L. KRILL; Rama Abu SHMEIS; Adrian HEPNER; Charles WESCOTT; Tara JASKOWSKI; Michael JOYCE - Web page: https://patentgrep.com/patent/US20230404918A1 ## CPC - A61K 9/10: Dispersions; Emulsions - A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)} - A61K 31/519: ortho- or peri-condensed with heterocyclic rings - A61K 31/565: not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol - A61K 31/566: having an oxo group in position 17, e.g. estrone - A61K 47/24: containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids - A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin - A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone} - 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 methods of treating breast cancer including administering aqueous suspensions com-prising solubilized fulvestrant, non-solubilized fulvestrant particles having one or more of an LD Dv(1 0) between about 1.5 and about 2.1 microns, an LD Dv(50) between about 5.5 and about 9.0 microns, and an LD Dv(90) between about 15 and about 35 microns, with the aqueous suspensions further including a surfactant, a polyvinylpyrrolidone, and a sugar alcohol, and a water-soluble excipient. The water-soluble excipient can be an aryl-Ci-6alk-OH, a Ci-6alkyl-OH, a buffering salt, a polysorbate, a polyalkylene glycol, a Ci-i2alkylene glycol, a phosphatidylcholine, or a combination thereof. ## Claims ### Claim 1 An aqueous suspension comprising: solubilized fulvestrant; non-solubilized fulvestrant particles having one or more of: an LD Dv(10) between about 1.5 microns and about 2.1 microns, an LD Dv(50) between about 5.5 microns and about 9.0 microns, and an LD Dv(90) between about 15 microns and about 35 microns; a surfactant; a polyvinylpyrrolidone; and a sugar alcohol; and a water-soluble excipient that is: an aryl-C1-6alk-OH, a C1-6alkyl-OH, a buffering salt, a polysorbate, a polyalkylene glycol, a C1-12alkylene glycol, a phosphatidylcholine, or a combination thereof. ### Claim 2 (depends on 1) The suspension of claim 1, wherein the aqueous suspension comprises between about 0.1% and about 5% (w/w), between about 0.5% and about 5% (w/w), between about 0.5% and about 2.5% (w/w), between about 0.9% and about 1.5% (w/w), about 4% (w/w), or about 1% (w/w) of the aryl-C1-6alk-OH. ### Claim 3 (depends on 1) The suspension of claim 1, wherein the aryl-C1-6alk-OH is benzyl alcohol. ### Claim 4 (depends on 1) The suspension of claim 1, wherein the aqueous suspension comprises between about 1% and about 10% (w/w), between about 5% and about 10% (w/w), between about 2% and about 4% (w/w), about 2% (w/w), about 4% (w/w), about 5% (w/w), or about 8% (w/w) of the C1-6alkyl-OH. ### Claim 5 (depends on 1) The suspension of claim 1, wherein the C1-6alkyl-OH is ethanol. ### Claim 6 (depends on 1) The suspension of claim 1, wherein the buffering salt is NaH2PO4, K2HPO4, KH2PO4, citric acid or a pharmaceutically acceptable salt thereof, tromethane or a pharmaceutically acceptable salt thereof, or a mixture thereof. ### Claim 7 (depends on 1) The suspension of claim 1, wherein the aqueous suspension comprises between about 0.1% to about 2% (w/w), between about 0.25% and about 1.80% (w/w), or about 0.75% (w/w), of the polysorbate. ### Claim 8 (depends on 1) The suspension of claim 1, wherein the polysorbate is polysorbate 20, polysorbate 60, polysorbate 80, or a combination thereof. ### Claim 9 (depends on 1) The suspension of claim 1, wherein the aqueous suspension comprises between about 1% and about 10% (w/w), between about 0.5% and about 8% (w/w), or about 5% (w/w) of the polyalkylene glycol. ### Claim 10 (depends on 1) The suspension of claim 1, wherein the polyalkylene glycol is a polyethylene glycol. ### Claim 11 (depends on 1) The suspension of claim 1, wherein the aqueous suspension comprises between about 0.1% and about 5% (w/w), between about 0.5% and about 4% (w/w), or about 2.5% (w/w) of the C1-12 alkylene glycol. ### Claim 12 (depends on 1) The suspension of claim 1, wherein the C1-12 alkylene glycol is propylene glycol. ### Claim 13 (depends on 1) The suspension of claim 1, wherein the aqueous suspension comprises between about 0.1% and about 5% (w/w), between about 0.1% and about 2% (w/w), or about 0.3% (w/w) of the phosphatidylcholine. ### Claim 14 (depends on 1) The suspension of claim 1, wherein the phosphatidylcholine is lecithin. ### Claim 15 (depends on 1) The suspension of claim 1, wherein the water soluble excipient is an aryl-C1-6alk-OH, a C1-6alkyl-OH, a polysorbate, or a buffering salt, or a combination thereof. ### Claim 16 (depends on 1) The suspension of claim 1, wherein the aqueous suspension has a pH of between about 6.0 and about 8.0, about 7, or about 7.5. ### Claim 17 (depends on 1) The suspension of claim 1, wherein the sugar alcohol is mannitol, xylitol, maltitol, lactitol, maltotriitol, sorbitol, glycerol, or a mixture thereof. ### Claim 18 (depends on 1) The method of claim 1, wherein the total amount of fulvestrant from solubilized fulvestrant and non-solubilized fulvestrant particles in the aqueous suspension is between about 80 mg/mL and about 170 mg/mL or about 100 mg/mL. ### Claim 19 A method of treating breast cancer in a subject, comprising administering to the subject an aqueous suspension comprising: solubilized fulvestrant; non-solubilized fulvestrant particles having one or more of: an LD Dv(10) between about 1.5 microns and about 2.1 microns, an LD Dv(50) between about 5.5 microns and about 9.0 microns, and an LD Dv(90) between about 15 microns and about 35 microns; a surfactant; a polyvinylpyrrolidone; and a sugar alcohol; and a water-soluble excipient that is: an aryl-C1-6alk-OH, a C1-6alkyl-OH, a buffering salt, a polysorbate, a polyalkylene glycol, a C1-12alkylene glycol, a phosphatidylcholine, or a combination thereof.