# US 12,109,214 B2 · Formulation and treatment methods > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 12,109,214 B2 - Document ID: US12109214B2 - Status: Granted - Kind: B2 - Application number: 17/361,995 - Filed: 2021-06-29 - Published: 2021-12-23 - Granted: 2024-10-08 - Earliest claimed: 2015-09-29 - Assignees: Prodrugxtend Pty Ltd - Applicants: Prodrugxtend Pty Ltd - Inventors: Timothy Florin; Amirali Popat; Siddharth Jambhrunkar - Web page: https://patentgrep.com/patent/US12109214B2 ## CPC - A61K 31/52: Purines, e.g. adenine - A61K 9/0031: {Rectum, anus} - A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration} - A61K 9/08: Solutions {(composition of solutions A61K47/00)} - A61K 9/20: Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)} - 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 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin} - A61K 9/28: Dragees; Coated pills or tablets {, e.g. with film or compression coating (A61K9/2072 takes precedence, e.g. partially coated tablets A61K9/2072, coated multilayer tablets A61K9/2086, tablets with drug-coated core A61K9/209)} - A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system - 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 invention relates to pharmaceutical compositions comprising 6-thioguanine (6-TG) wherein the composition is formulated for release of 6-TG in the distal intestine. Methods for treating a disease or condition of the distal ileum that responds to 6-TG wherein the 6-TG is released in the distal intestine are also disclosed. ## Claims ### Claim 1 A method for treating inflammatory bowel disease in an individual in need thereof, the method comprising administering a pharmaceutical composition comprising 6-thioguanine (6-TG) and a homogeneous erodible hydrophilic polymer matrix to the individual, wherein the composition is formulated for oral administration, wherein the composition exhibits an in vitro release of at least 35% of the 6-TG at pH 6 to about pH 7.5 after 12 hours. ### Claim 2 (depends on 1) A method according to claim 1, wherein systemic concentrations of 6-TG are low. ### Claim 3 (depends on 1) A method according to claim 1, wherein the 6-TG is metabolised by luminal bacteria or diseased mucosa at a site of inflammation associated with the disease or condition. ### Claim 4 (depends on 1) A method according to claim 1, further comprising administering an additional active agent for treating inflammatory bowel disease. ### Claim 5 (depends on 1) A method according to claim 1, wherein the homogeneous erodible hydrophilic polymer matrix comprises polyethylene oxides. ### Claim 6 (depends on 1) A method according to claim 1, wherein the homogeneous erodible hydrophilic polymer matrix further comprises a hydrophobic polymer. ### Claim 7 (depends on 1) A method according to claim 1, wherein the homogeneous erodible hydrophilic polymer matrix comprises ethyl cellulose. ### Claim 8 (depends on 1) A method according to claim 1, wherein the composition exhibits an in vitro release of at least 50%, 55%, 60%, 65%, 70%, 75%, 80%, 85%, 90%, or 95% of the 6-TG at pH 6 to pH 7.5 after 12 hours. ### Claim 9 (depends on 1) A method according to claim 1, wherein the concentration of 6-TGN in blood leukocytes is low. ### Claim 10 A method for treating inflammatory bowel disease in an individual in need thereof, the method comprising administering a pharmaceutical composition comprising 6-thioguanine (6-TG) and a homogeneous erodible hydrophilic polymer matrix, wherein the composition is formulated for oral administration and to release at least 35% of the 6-TG in the distal intestine of the individual. ### Claim 11 (depends on 10) A method according to claim 10, wherein the composition is formulated to release at least 35% of the 6-TG in the colon of the individual. ### Claim 12 (depends on 10) A method according to claim 10, wherein the homogeneous erodible hydrophilic polymer matrix comprises polyethylene oxides. ### Claim 13 (depends on 10) A method according to claim 10, wherein the homogeneous erodible hydrophilic polymer matrix further comprises a hydrophobic polymer. ### Claim 14 (depends on 10) A method according to claim 10, wherein the homogeneous erodible hydrophilic polymer matrix comprises ethyl cellulose. ### Claim 15 (depends on 10) A method according to claim 10, wherein the composition is formulated to release at least 45% of the 6-TG in the distal intestine. ### Claim 16 (depends on 10) A method according to claim 10, wherein the composition is formulated to release at least 60% of the 6-TG in the distal intestine. ### Claim 17 (depends on 10) A method according to claim 10, wherein systemic concentrations of 6-TG are low. ### Claim 18 (depends on 10) A method according to claim 10, wherein the 6-TG is metabolised by luminal bacteria or diseased mucosa at a site of inflammation associated with the inflammatory bowel disease. ### Claim 19 (depends on 10) A method according to claim 10, further comprising administering an additional active agent for treating inflammatory bowel disease. ### Claim 20 (depends on 10) A method according to claim 10, wherein the concentration of 6-TGN in blood leukocytes is low.