# US 11,433,091 B2 · Methods and compositions for administration of iron > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,433,091 B2 - Document ID: US11433091B2 - Status: Granted - Kind: B2 - Application number: 15/958,930 - Filed: 2018-04-20 - Published: 2018-08-23 - Granted: 2022-09-06 - Earliest claimed: 2006-01-06 - Assignees: American Regent, Inc. - Applicants: American Regent, Inc. - Inventors: Mary Jane Helenek; Marc L. Tokars; Richard P. Lawrence - Web page: https://patentgrep.com/patent/US11433091B2 ## CPC - A61K 31/7135: Compounds containing heavy metals - A61K 31/715: Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters - A61K 31/721: Dextrans - A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system - A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00) - A61P 7/06: Antianaemics - A61P 9/04: Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure - A61P 13/12: of the kidneys - A61P 19/02: for joint disorders, e.g. arthritis, arthrosis - A61P 35/00: Antineoplastic agents - A61P 35/02: specific for leukemia - C07H 23/00: Compounds containing boron, silicon or a metal, e.g. chelates or vitamin B12 (esters with inorganic acids C07H11/00) - 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 - C07H: SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS (derivatives of aldonic or saccharic acids C07C, C07D; aldonic acids, saccharic acids C07C59/105, C07C59/285; cyanohydrins C07C255/16; glycals C07D; compounds of unknown constitution C07G; polysaccharides, derivatives thereof C08B; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; sugar industry C13) ## Abstract The present invention generally relates to treatment of iron-related conditions with iron carbohydrate complexes. One aspect of the invention is a method of treatment of iron-related conditions with a single unit dosage of at least about 0.6 grams of elemental iron via an iron carbohydrate complex. The method generally employs iron carbohydrate complexes with nearly neutral pH, physiological osmolarity, and stable and non-immunogenic carbohydrate components so as to rapidly administer high single unit doses of iron intravenously to patients in need thereof. ## Claims ### Claim 1 A method of treating a disease, disorder, or condition characterized by iron deficiency or dysfunctional iron metabolism, comprising intravenously administering to a human subject in need thereof an iron carbohydrate complex in a single dosage unit of at least 0.7 grams of elemental iron in 15 minutes, wherein the disease, disorder, or condition is anemia. ### Claim 2 (depends on 1) The method of claim 1, wherein the anemia is iron deficiency anemia. ### Claim 3 (depends on 2) The method of claim 2, wherein the iron deficiency anemia is associated with chronic blood loss; acute blood loss; pregnancy; childbirth; childhood development; psychomotor and cognitive development in children; breath holding spells; heavy uterine bleeding; menstruation; chronic recurrent hemoptysis; idiopathic pulmonary siderosis; chronic internal bleeding; gastrointestinal bleeding; parasitic infections; chronic kidney disease; dialysis; surgery or acute trauma; and chronic ingestion of alcohol, chronic ingestion of salicylates, chronic ingestion of steroids; chronic ingestion of non-steroidal anti-inflammatory agents, or chronic ingestion of erythropoiesis stimulating agents. ### Claim 4 (depends on 1) The method of claim 1, wherein the anemia is anemia of chronic disease. ### Claim 5 (depends on 4) The method of claim 4, wherein the chronic disease is selected from the group consisting of rheumatoid arthritis; cancer; Hodgkin's leukemia; nonHodgkin's leukemia; cancer chemotherapy; inflammatory bowel disease; ulcerative colitis; thyroiditis; hepatitis; systemic lupus erythematosus; polymyalgia rheumatica; scleroderma; mixed connective tissue disease; Sjogren's syndrome; congestive heart failure/cardiomyopathy; and idiopathic geriatric anemia. ### Claim 6 (depends on 1) The method of claim 1, wherein the anemia is due to impaired iron absorption or poor nutrition. ### Claim 7 (depends on 1) The method of claim 1, wherein the anemia is associated with Crohn's Disease; gastric surgery; ingestion of drug products that inhibit iron absorption; and chronic use of calcium. ### Claim 8 (depends on 1) The method of claim 1, wherein the single dosage unit of elemental iron is at least 0.8 grams; at least 0.9 grams; at least 1.0 grams; at least 1.1 grams; at least 1.2 grams; at least 1.3 grams; at least 1.4 grams; at least 1.5 grams; at least 1.6 grams; at least 1.7 grams; at least 1.8 grams; at least 1.9 grams; at least 2.0 grams; at least 2.1 grams; at least 2.2 grams; at least 2.3 grams; at least 2.4 grams; or at least 2.5 grams. ### Claim 9 (depends on 8) The method of claim 8, wherein the single dosage unit of elemental iron is at least 1.0 grams. ### Claim 10 (depends on 9) The method of claim 9, wherein the single dosage unit of elemental iron is at least 1.5 grams. ### Claim 11 (depends on 10) The method of claim 10, wherein the single dosage unit of elemental iron is at least 2.0 grams. ### Claim 12 (depends on 11) The method of claim 11, wherein the single dosage unit of elemental iron is at least 2.5 grams. ### Claim 13 (depends on 1) The method of claim 1, wherein administration of the single dose is repeated. ### Claim 14 (depends on 1) The method of claim 1, wherein the iron carbohydrate complex is an iron carboxymaltose, iron mannitol, iron polyisomaltose, iron polymaltose, iron gluconate, iron sorbitol, or an iron hydrogenated dextran. ### Claim 15 (depends on 14) The method of claim 14, wherein the iron carbohydrate complex is an iron carboxymaltose complex. ### Claim 16 (depends on 15) The method of claim 15, wherein the iron carboxymaltose complex is polynuclear iron (III)-hydroxide 4(R)-(poly-(1→4)-O-α-D-glucopyranosyl)-oxy-2(R),3(R),5(R),6-tetrahydroxy-hexanoate. ### Claim 17 (depends on 1) The method of claim 1, wherein the single unit dose of iron carbohydrate complex is intravenously infused at a concentration of about 1000 mg elemental iron in about 215 ml of diluent. ### Claim 18 (depends on 1) The method of claim 1, further comprising a second administration of the iron carbohydrate complex upon recurrence of at least one symptom of the disease or disorder. ### Claim 19 (depends on 1) The method of claim 1, further comprising a second administration of the iron complex 1 day to 12 months after the first administration. ### Claim 20 A method of treating a disease, disorder, or condition characterized by iron deficiency or dysfunctional iron metabolism, comprising administering to a subject in need thereof an iron carbohydrate complex in a single dosage unit of at least 0.7 grams of elemental iron in less than 15 minutes, wherein the disease, disorder, or condition is anemia. ### Claim 21 (depends on 20) The method of claim 20, wherein the single dosage unit of elemental iron is at least 0.8 grams; at least 0.9 grams; at least 1.0 grams; at least 1.1 grams; at least 1.2 grams; at least 1.3 grams; at least 1.4 grams; at least 1.5 grams; at least 1.6 grams; at least 1.7 grams; at least 1.8 grams; at least 1.9 grams; at least 2.0 grams; at least 2.1 grams; at least 2.2 grams; at least 2.3 grams; at least 2.4 grams; or at least 2.5 grams. ### Claim 22 (depends on 20) The method of claim 20, wherein the single dosage unit of elemental iron is administered in less than 10 minutes. ### Claim 23 (depends on 20) The method of claim 20, wherein the single dosage unit of elemental iron is administered in less than 5 minutes. ### Claim 24 (depends on 20) The method of claim 20, wherein the single dosage unit of elemental iron is administered in less than 2 minutes. ### Claim 25 (depends on 20) The method of claim 20, wherein the single dosage unit of elemental iron is administered intravenously. ### Claim 26 (depends on 20) The method of claim 20, wherein the iron carbohydrate complex is an iron carboxymaltose, iron mannitol, iron polyisomaltose, iron polymaltose, iron gluconate, iron sorbitol, or an iron hydrogenated dextran. ### Claim 27 (depends on 26) The method of claim 26, wherein the iron carbohydrate complex is an iron carboxymaltose complex. ### Claim 28 (depends on 26) The method of claim 26, wherein the iron carbohydrate complex is an iron polyisomaltose complex.