# US 2018/0021373 A1 · Ruthenium and Indium Binding to Gastrins > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2018/0021373 A1 - Document ID: US20180021373A1 - Status: Published application - Kind: A1 - Application number: 15/548,322 - Filed: 2016-02-04 - Published: 2018-01-25 - Earliest claimed: 2015-02-04 - Assignees: Eupharma Pty Ltd - Applicants: Eupharma Pty Ltd - Inventors: Malvin EUTICK - Web page: https://patentgrep.com/patent/US20180021373A1 ## CPC - A61K 33/24: Heavy metals; Compounds thereof - A61K 33/00: Medicinal preparations containing inorganic active ingredients - A61K 38/2207: {Gastrins; Cholecystokinins [CCK]} - A61K 51/08: Peptides, e.g. proteins {, carriers being peptides, polyamino acids, proteins} - A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants - A61P 7/06: Antianaemics - A61P 13/12: of the kidneys - A61P 35/00: Antineoplastic agents - A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 - C07K 14/72: for hormones {(for neuromediators C07K14/70571)} - G01N 33/575: for cancer - A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00) - C07K 2319/00: Fusion polypeptide - 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 - C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00) - G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q) ## Abstract The present invention relies on the hitherto unrealised high affinity binding of ruthenium and indium to gastrins. Particularly, these metals can be bound directly to the gastrins under mild conditions and so can be used in treatment of conditions associated with elevated gastrin levels and in detection of tumours and other conditions where CCK receptors are over expressed. ## Claims ### Claim 1 A method of treatment or prophylaxis of a condition in a patient associated with elevated concentrations of a non-amidated gastrin including the step of administering an effective amount of a metal selected from indium and ruthenium to the patient. ### Claim 2 A method of modulating the activity of a non-amidated gastrin including the step of binding a metal selected from indium and ruthenium to the non-amidated gastrin. ### Claim 3 (depends on 1) The method of claim 1, wherein the metal is administered to the patient such that the metal binds to the ferric binding site of the non-amidated gastrin. ### Claim 4 (depends on 1) The method of claim 1, wherein the indium and ruthenium are in the In3+ and Ru3+ form. ### Claim 5 (depends on 1) The method of claim 1, wherein the indium and ruthenium are radioisotopes of indium and ruthenium. ### Claim 6 (depends on 1) The method of claim 1, wherein the metal is part of a solution containing the free ions, or the metal is a component of a compound or salt. ### Claim 7 (depends on 1) The method of claim 1, wherein the metal is not bound to a chelate group when it is brought into contact with the non-amidated gastrin. ### Claim 8 (depends on 1) The method of claim 1, wherein the condition is selected from the group consisting of a colorectal carcinoma, a gastrinoma, an islet cell carcinoma, an ovarian tumor, a pituitary tumor, a medullary thyroid carcinoma, an astrocytoma, a small cell lung cancer, a meningioma, an endometrial and ovarian adenocarcinoma, a breast carcinoma, a gastrointestinal stromal tumor, a gastro enteropancreatic tumor, atrophic gastritis, G cell hyperplasia, pernicious anaemia, renal failure, ulcerative colitis, a gastrointestinal ulcer, gastro-oesophageal reflux, gastric carcinoid, and Zollinger-Ellison syndrome. ### Claim 9 (depends on 1) The method of claim 1, wherein the patient is a mammal. ### Claim 10 (depends on 2) The method of claim 2, wherein modulation of the non-amidated gastrin is a reduction in its normal biological activity. ### Claim 11 A method of treatment or prophylaxis of a condition in a patient associated with over-expression of a CCK receptor including the step of administering an effective amount of a metal selected from indium and ruthenium to the patient. ### Claim 12 (canceled) ### Claim 13 (canceled) ### Claim 14 (canceled) ### Claim 15 (canceled) ### Claim 16 (canceled) ### Claim 17 (canceled) ### Claim 18 A complex comprising a gastrin and a metal selected from indium and ruthenium bound or complexed to the ferric binding site of the gastrin. ### Claim 19 (depends on 18) The complex of claim 18, wherein the gastrin is an amidated gastrin or a non-amidated gastrin. ### Claim 20 (depends on 18) The complex of claim 18, wherein the metal is not bound to a chelate group when it is brought into contact with the gastrin. ### Claim 21 (canceled) ### Claim 22 (canceled) ### Claim 23 (canceled) ### Claim 24 (canceled) ### Claim 25 (canceled) ### Claim 26 (canceled) ### Claim 27 (canceled) ### Claim 28 (canceled) ### Claim 29 (depends on 2) The method of claim 2, wherein the indium and ruthenium are in the In3+ and Ru3+ form. ### Claim 30 (depends on 2) The method of claim 2, wherein the indium and ruthenium are radioisotopes of indium and ruthenium. ### Claim 31 (depends on 2) The method of claim 2, wherein the metal is part of a solution containing the free ions or the metal is a component of a compound or salt. ### Claim 32 (depends on 2) The method of claim 2, wherein the metal is not bound to a chelate group when it is brought into contact with the non-amidated gastrin.