# US 11,078,245 B2 · Colon and pancreas cancer peptidomimetics > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,078,245 B2 - Document ID: US11078245B2 - Status: Granted - Kind: B2 - Application number: 16/697,231 - Filed: 2019-11-27 - Published: 2020-05-28 - Granted: 2021-08-03 - Earliest claimed: 2010-09-23 - Assignees: Precision Biologics, Inc. - Applicants: Precision Biologics, Inc. - Inventors: Xue-Ping Wang - Web page: https://patentgrep.com/patent/US11078245B2 ## CPC - C07K 14/4727: {Mucins, e.g. human intestinal mucin} - A61K 39/0011: {Cancer antigens} - A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca - A61K 47/64: Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent (peptidic linkers A61K47/65) - A61K 47/643: {Albumins, e.g. HSA, BSA, ovalbumin or a Keyhole Limpet Hemocyanin [KHL]} - A61K 47/645: {Polycationic or polyanionic oligopeptides, polypeptides or polyamino acids, e.g. polylysine, polyarginine, polyglutamic acid or peptide TAT} - A61K 47/646: {the entire peptide or protein drug conjugate elicits an immune response, e.g. conjugate vaccines} - C07K 14/4748: {Tumour specific antigens; Tumour rejection antigen precursors [TRAP], e.g. MAGE} - C07K 16/3092: {against tumour-associated mucins} - G01N 33/57525: of the liver or pancreas - G01N 33/57535: of the large intestine, e.g. colon, rectum or anus - 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) - A61K 2039/505: {comprising antibodies} - C07K 2317/34: Identification of a linear epitope shorter than 20 amino acid residues or of a conformational epitope defined by amino acid residues - C07K 2317/732: Antibody-dependent cellular cytotoxicity [ADCC] - C07K 2319/00: Fusion polypeptide - G01N 2333/4725: Mucins, e.g. human intestinal mucin - 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) - 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) - 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 invention relates to a peptidomimetic of an NPC-1 epitope on the MUC5AC protein which is differentially expressed in pancreatic and colorectal cancer, and diagnostic and therapeutic usages. Further, antibodies that selectively bind the NPC-1 epitope peptidomimetics and may be used in diagnostic and therapeutic methods. ## Claims ### Claim 1 An isolated polypeptide comprising a polypeptide having at least 80% identity to the amino acid sequence SLEPEX1DWX2FRYX3NY (SEQ ID NO: 3), wherein X1 is E or D; X2 is W or Y; and X3 is T or I; or any one of the amino acid sequences of SEQ ID NOs: 6 or 7. ### Claim 2 (depends on 1) A composition comprising the polypeptide of claim 1. ### Claim 3 (depends on 2) The composition of claim 2, further comprising a pharmaceutically acceptable carrier, diagnostically acceptable carrier, adjuvant, or excipient. ### Claim 4 (depends on 1) A composition for treating cancer comprising an effective amount of the polypeptide of claim 1. ### Claim 5 (depends on 1) A diagnostic kit comprising the polypeptide of claim 1. ### Claim 6 (depends on 1) A fusion protein comprising the polypeptide of claim 1. ### Claim 7 (depends on 6) The fusion protein of claim 6, wherein said fusion protein further comprises a detectable label covalently or non-covalently directly or indirectly attached thereto. ### Claim 8 (depends on 7) The fusion protein of claim 7, wherein the detectable label is selected from the group consisting of polyHis tag, FLAG tag, MBP, GST, and GFP. ### Claim 9 (depends on 1) A conjugate comprising the polypeptide of claim 1, directly or indirectly conjugated to (a) a cytotoxic agent, (b) a therapeutic agent, (c) a label, (d) a carbohydrate, (e) a carrier, (f) a immunoglobulin or immunoglobulin fragment, or (g) an immunomodulatory agent. ### Claim 10 (depends on 9) The conjugate of claim 9, wherein the cytotoxic agent is selected from the group consisting of a moiety that inhibits DNA, RNA, or protein synthesis, a radionuclide, ribosomal inhibiting protein, 212Bi, 131I, 188Re, 90Y, vindesine, methotrexate, adriamycin, cisplatin, pokeweed antiviral protein, Pseudomonas exotoxin A, ricin, diphtheria toxin, ricin A chain, and cytotoxic phospholipase enzyme; wherein the label is selected from the group consisting of a chemiluminescent label, paramagnetic label, MRI contrast agent, fluorescent label, bioluminescent label, and a radioactive label; wherein the label is a paramagnetic label selected from the group consisting of aluminum, manganese, platinum, oxygen, lanthanum, lutetium, scandium, yttrium, and gallium; wherein the carbohydrate is selected from the group consisting of mannose, fucose, glucose, GlcNAs, and maltose; and/or wherein the carrier is selected from the group consisting of Keyhole Limpet Hemocyanin (KLH), diphtheria toxoid, cholera toxoid, ovalbumin, bovine serum albumin (BSA), Pseudomonas exoprotein A, and microbial outer membrane proteins (MPS). ### Claim 11 (depends on 1) An isolated nucleic acid encoding a polypeptide according to claim 1. ### Claim 12 (depends on 11) A method of making a peptidomimetic polypeptide, said method comprising culturing a host cell comprising the nucleic acid of claim 11 in a suitable medium such that said peptidomimetic polypeptide is produced, wherein said nucleic acid is operably linked to a promoter; or said method comprising introducing a recombinant expression vector comprising the nucleic acid of claim 11 into an in vitro transcription/translation system, wherein said nucleic acid is operably linked to a promoter. ### Claim 13 (depends on 1) A method for treating cancer comprising administering to a subject in need thereof an effective amount of a polypeptide of claim 1, thereby eliciting an anti-cancer immune response in said subject. ### Claim 14 (depends on 13) The method of claim 13, wherein said polypeptide is administered in combination with an antibody, a lymphokine, or a hematopoietic growth factor, wherein said polypeptide is administered simultaneously or sequentially with said antibody, lymphokine, or hematopoietic growth factor. ### Claim 15 (depends on 13) The method of claim 13, wherein said cancer is lung, breast, ovarian, stomach, pancreas, uterine, esophageal, colorectal, or liver cancer. ### Claim 16 (depends on 15) The method of claim 15, wherein said cancer is a stage 1, 2, 3, or 4 cancer and/or wherein said cancer had metastasized. ### Claim 17 (depends on 13) The method of claim 13, wherein the patient expresses detectable levels of a NPC-1 epitope. ### Claim 18 (depends on 17) The method of claim 17, wherein the antigen is detected in a tumor biopsy sample or in the blood, stool, urine, or lymph fluid. ### Claim 19 (depends on 1) A method for activating dendritic cells comprising removing dendritic cells from a patient, contacting said cells cx vivo with an effective amount of the polypeptide of claim 1, and reintroducing said activated dendritic cells into said patient. ### Claim 20 (depends on 1) A method for activating antigen-specific immunity comprising administering to a patient an effective amount of a polypeptide of claim 1.