# US 11,439,802 B2 · Ingestible device for delivery of therapeutic agent to the gastrointestinal tract > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,439,802 B2 - Document ID: US11439802B2 - Status: Granted - Kind: B2 - Application number: 17/319,800 - Filed: 2021-05-13 - Published: 2021-09-16 - Granted: 2022-09-13 - Earliest claimed: 2018-11-19 - Assignees: Biora Therapeutics, Inc. - Applicants: Biora Therapeutics, Inc. - Inventors: Jeffrey A. Shimizu; Mitchell Lawrence Jones; Mark Sasha Drlik; Iman Niknia; Nathan John Muller; Tuyen Nguyen; Christopher Loren Wahl; Edward Mudge; Nicholas Mark Salt; Nia Eleri Stevens; Stuart Robert Abercrombie; Christopher Ian Bunce; Nelson Quintana - Web page: https://patentgrep.com/patent/US11439802B2 ## CPC - A61M 31/002: {Devices for releasing a drug at a continuous and controlled rate for a prolonged period of time (artificial gland structures or devices A61F2/022; intra-uterine contraceptive devices A61F6/14; tampons for introducing into the vagina A61F13/20, A61L15/00; suppositories or bougies for intra-vaginal or intra-uterine application A61K9/02; physical forms of medicinal preparations for sustained or differential drug release A61K9/20, A61K9/50)} - A61K 38/1796: {for hormones (for neuromediators A61K38/1787)} - A61K 38/26: Glucagons - A61K 38/28: Insulins - A61M 11/02: operated by air {or other gas} pressure applied to the liquid {or other product} to be sprayed or atomised {(sprayers for horticulture A01G, A01H; killing insects A01M; air humidifying by nozzles F24F6/14, F24F6/18; cooling by spraying F28B, F28C)} - A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants - C07K 16/241: {Tumor Necrosis Factors} - A61M 2210/1042: Alimentary tract (A61M2210/0618 takes precedence) - A61M 2210/106: Small intestine - A61M 2210/1064: Large intestine - A61M: DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY (introducing media into or onto the bodies of animals A61D7/00; means for inserting tampons A61F13/26; devices for administering food or medicines orally A61J; containers for collecting, storing or administering blood or medical fluids A61J1/05); DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY (surgery A61B; chemical aspects of surgical articles A61L); DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR {(Electrotherapy, e.g. producing anaesthesia by the use of alternating or intermittent currents A61N1/36021)} - 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) ## Abstract A method of treating a disease or condition in a subject in need thereof is disclosed. The method comprising: trans-epithelially administering a dispensable substance to the gastrointestinal (GI) tract of the subject by orally administering an ingestible device comprising the dispensable substance to the subject. The ingestible device is configured for trans-epithelial delivery of the dispensable substance to the GI tract of the subject and the dispensable substance comprises a pharmaceutical formulation comprising a therapeutically effective amount of a glucagon receptor agonist or a glucagon-like peptide-1 (GLP-1) receptor agonist. The ingestible device releases the dispensable substance as at least one jet to a desired location of the GI tract of the subject. ## Claims ### Claim 1 A method of treating a disease or condition in a subject in need thereof, the method comprising: trans-epithelially administering a dispensable substance to the gastrointestinal (GI) tract of the subject, wherein the trans-epithelial administration comprises: orally administering an ingestible device comprising the dispensable substance to the subject, wherein the ingestible device is configured for trans-epithelial delivery of the dispensable substance to the GI tract of the subject, and the dispensable substance comprises a pharmaceutical formulation comprising a therapeutically effective amount of a glucagon receptor agonist or a glucagon-like peptide-1 (GLP-1) receptor agonist; and releasing the dispensable substance from the ingestible device as at least one jet to a desired location of the GI tract of the subject; wherein the desired location of the GI tract is the small intestine, wherein the trans-epithelial administration directly delivers the dispensable substance to the submucosa of the GI tract of the subject, and wherein the disease or condition is responsive to treatment with the glucagon receptor agonist or GLP-1 receptor agonist. ### Claim 2 (depends on 1) The method of claim 1, wherein the trans-epithelial administration provides systemic uptake of the glucagon receptor agonist or the GLP-1 receptor agonist that is at least about 20% relative to intravenous or subcutaneous administration of an equal amount of the glucagon receptor agonist or the GLP-1 receptor agonist. ### Claim 3 (depends on 1) The method of claim 1, wherein the glucagon receptor agonist or the GLP-1 receptor agonist has a molecular weight of at least about 1.5 kDa. ### Claim 4 (depends on 1) The method of claim 1, wherein the desired location of the GI tract is the jejunum. ### Claim 5 (depends on 1) The method of claim 1, wherein the trans-epithelial administration provides systemic uptake of the glucagon receptor agonist or the GLP-1 receptor agonist that is at least about 10% relative to intravenous or subcutaneous administration of an equal amount of the glucagon receptor agonist or the GLP-1 receptor agonist. ### Claim 6 (depends on 1) The method of claim 1, wherein the trans-epithelial administration provides an area under the curve (AUC) of the glucagon receptor agonist or the GLP-1 receptor agonist in systemic circulation over time (AUCTE) that is at least about 10% of the AUC in systemic circulation over time provided by intravenous administration of an equal amount of the glucagon receptor agonist or the GLP-1 receptor agonist (AUCIV) or by subcutaneous administration of an equal amount of the glucagon receptor agonist or the GLP-1 receptor agonist (AUCSC). ### Claim 7 (depends on 1) The method of claim 1, wherein the trans-epithelial administration provides a maximum plasma concentration (Cmax) of the glucagon receptor agonist or the GLP-1 receptor agonist in systemic circulation ((Cmax)TE) that is at least about 10% of the Cmax in systemic circulation provided by intravenous administration of an equal amount of the glucagon receptor agonist or the GLP-1 receptor agonist ((Cmax)IV) or by subcutaneous administration of an equal amount of the glucagon receptor agonist or GLP-1 receptor agonist ((Cmax)SC). ### Claim 8 (depends on 1) The method of claim 1, wherein the pharmaceutical formulation is a liquid solution or suspension. ### Claim 9 (depends on 1) The method of claim 1, wherein a volume of the dispensable substance released from the ingestible device is from about 50 microliters to about 800 microliters. ### Claim 10 (depends on 1) The method of claim 1, wherein releasing the dispensable substance from the ingestible device as at least one jet to a desired location of the GI tract of the subject is at a peak jet power of about 1 Watt to about 3 Watts. ### Claim 11 (depends on 1) The method of claim 1, wherein the disease or condition is a metabolic, endocrine, or cardiovascular disease or condition. ### Claim 12 (depends on 11) The method of claim 11, wherein the metabolic or endocrine disease or condition is selected from the group consisting of diabetes, a liver disease or disorder, obesity, hyperglycemia, hyperlipidemia, hyperinsulinemia, hypercholesterolemia, lipodystrophy, obstructive sleep apnea, nicotine dependence, and a central nervous system (CNS) disorder. ### Claim 13 (depends on 12) The method of claim 12, wherein the liver disease or disorder is selected from the group consisting of compensated liver cirrhosis, liver fibrosis, non-alcoholic steatohepatitis (NASH), and non-alcoholic fatty liver disease (NAFLD). ### Claim 14 (depends on 11) The method of claim 11, wherein the cardiovascular disease or condition is selected from the group consisting of myocardial infarction, stroke, coronary artery diseases (CAD), heart failure, transient ischemic attacks, peripheral arterial disease, aortic disease, aortic aneurysms, congestive heart failure, hypertension, hypertensive heart disease, pulmonary artery hypertension, arrhythmia, and thromboembolism. ### Claim 15 (depends on 1) The method of claim 1, wherein the glucagon receptor agonist or the GLP-1 receptor agonist has a molecular weight of from about 1.5 kDa to about 5 kDa. ### Claim 16 (depends on 1) The method of claim 1, wherein the glucagon receptor agonist or the GLP-1 receptor agonist is selected from the group consisting of semaglutide, dulaglutide, cotadutide, exenatide, liraglutide, tirzepatide, NNC-0090-2746, glucagon, NN-9277, and NN-9423; and biosimilars thereof. ### Claim 17 (depends on 16) The method of claim 16, wherein the glucagon receptor agonist or the GLP-1 receptor agonist is cotadutide or a biosimilar thereof. ### Claim 18 (depends on 16) The method of claim 16, wherein the glucagon receptor agonist or the GLP-1 receptor agonist is liraglutide or a biosimilar thereof. ### Claim 19 (depends on 16) The method of claim 16, wherein the glucagon receptor agonist or the GLP-1 receptor agonist is tirzepatide or a biosimilar thereof. ### Claim 20 A method of treating a disease or condition in a patient, comprising: trans-epithelially administering a pharmaceutical formulation to the gastrointestinal tract of patient via the patient swallowing an ingestible device containing the pharmaceutical formulation; the ingestible device configured for trans-epithelial delivery of the pharmaceutical formulation to the gastrointestinal tract; the pharmaceutical formulation comprising a therapeutically effective amount of a glucagon receptor agonist or a glucagon-like peptide-1 receptor agonist; and releasing the pharmaceutical formulation from the ingestible device in the small intestine as one or more jets to directly deliver the pharmaceutical formulation to the submucosa of the gastrointestinal tract. ### Claim 21 (depends on 20) The method of claim 20 wherein the trans-epithelial administration provides systemic uptake of the glucagon receptor agonist or the GLP-1 receptor agonist that is at least about 25% of the systemic uptake of intravenous or subcutaneous administration of an equal amount of glucagon receptor agonist or GLP-1 receptor agonist. ### Claim 22 (depends on 20) The method of claim 20 wherein the trans-epithelial administration provides an area under the curve (AUC) of the glucagon receptor agonist or the GLP-1 receptor agonist in systemic circulation over time (AUCTE) that is at least about 25% of the AUC in systemic circulation over time provided by intravenous administration of an equal amount of glucagon receptor agonist or GLP-1 receptor agonist (AUCIV) or by subcutaneous administration of an equal amount of glucagon receptor agonist or GLP-1 receptor agonist (AUCsc). ### Claim 23 (depends on 20) The method of claim 20 wherein the trans-epithelial administration provides a maximum plasma concentration (Cmax) of the glucagon receptor agonist or the GLP-1 receptor agonist in systemic circulation ((Cmax)TE) that is at least about 25% of the Cmax in systemic circulation provided by intravenous administration of an equal amount of glucagon receptor agonist or GLP-1 receptor agonist ((Cmax)IV) or by subcutaneous administration of an equal amount of glucagon receptor agonist or GLP-1 receptor agonist ((Cmax)SC). ### Claim 24 (depends on 20) The method of claim 20 wherein a volume of the pharmaceutical formulation released from the ingestible device is about 250 microliters to about 400 microliters.