# US 10,500,246 B2 · Compositions for delivery to and treatment of atherosclerotic plaques > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,500,246 B2 - Document ID: US10500246B2 - Status: Granted - Kind: B2 - Application number: 15/738,000 - Filed: 2016-06-27 - Published: 2018-10-25 - Granted: 2019-12-10 - Earliest claimed: 2015-06-25 - Assignees: Sanford Burnham Prebys Medical Discovery Institute - Applicants: Sanford Burnham Prebys Medical Discovery Institute - Inventors: Erkki Ruoslahti; Tambet Teesalu; Lauri Paasonen - Web page: https://patentgrep.com/patent/US10500246B2 ## CPC - A61K 38/08: Peptides having 5 to 11 amino acids {(A61K38/043 - A61K38/046 take precedence)} - A61K 9/1075: {Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence)} - A61K 9/5115: {Inorganic compounds} - A61K 31/195: having an amino group - A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca - A61K 47/55: the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug - A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis - C07K 7/06: having 5 to 11 amino acids - C07K 7/64: Cyclic peptides containing only normal peptide links - A61K 47/543: {Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine} - A61K 47/643: {Albumins, e.g. HSA, BSA, ovalbumin or a Keyhole Limpet Hemocyanin [KHL]} - 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 Disclosed are compositions and methods for treatment of atherosclerosis and atherosclerotic plaques. In some forms, the compositions and methods can prevent, inhibit, or reduce atherosclerosis. In some forms, the compositions and methods can prevent, inhibit, or reduce atherosclerotic plaques. In particular, compositions comprising a plaque-homing element, a CendR-activating element, and a plaque-inhibiting element are disclosed. ## Claims ### Claim 1 A composition comprising a plaque-homing element, a CendR-activating element, and a plaque-inhibiting element, wherein the plaque-homing element is CXaRGXbRSXcC (SEQ ID NO:3), wherein Xa and Xb, are independently are any amino acid, and, independently, Xc is any amino acid or is absent. ### Claim 2 (depends on 1) The composition of claim 1, wherein the CendR-activating element is a peptide. ### Claim 3 (depends on 1) The composition of claim 1, wherein the CendR-activating element is CGQKRTRGC (SEQ ID NO:2), GNKRTR (SEQ ID NO:7), CKRGAR (SEQ ID NO:9), CKRGSR (SEQ ID NO:10), CKRGNR (SEQ ID NO:11), CXaRGXbR (SEQ ID NO:13), KRGAR (SEQ ID NO:14), KRGSR (SEQ ID NO:15), KRGNR (SEQ ID NO:16), RGXbR (SEQ ID NO:12), XaRGXbR (SEQ ID NO:17), RPARPAR (SEQ ID NO:18), a peptide with the sequence X1X2X3X4 at, or exposable at, the free C-terminal end of the peptide, wherein X1 is R, K or H, wherein X4 is R, K, H, or KG, and wherein X2 and X3 are each, independently, any amino acid), or an extended blood half-life LyP-1, wherein the extended blood half-life LyP-1 comprises the amino acid sequence GNKRTR (SEQ ID NO:7), wherein Xa and Xb independently are any amino acid. ### Claim 4 (depends on 1) The composition of claim 1, wherein the plaque-inhibiting element is a peptide. ### Claim 5 (depends on 1) The composition of claim 1, wherein the plaque-inhibiting element is CGQKRTRGC (SEQ ID NO:2 or an extended blood half-life LyP-1, wherein the extended blood half-life LyP-1 comprises the amino acid sequence GNKRTR (SEQ ID NO:7). ### Claim 6 (depends on 1) The composition of claim 1, wherein one or more of the plaque-homing element, CendR-activating element, and plaque-inhibiting element is a peptide, wherein one or more of the one or more plaque-homing element, CendR-activating element, and plaque-inhibiting element that is a peptide conjugates to albumin in blood. ### Claim 7 (depends on 1) The composition of claim 1, wherein one or more of the plaque-homing element, CendR-activating element, and plaque-inhibiting element is a peptide, wherein one or more of the one or more plaque-homing element, CendR-activating element, and plaque-inhibiting element that is a peptide is conjugated to a lipid. ### Claim 8 (depends on 1) The composition of claim 1, wherein the composition is comprised in a micelle. ### Claim 9 (depends on 1) A method of treating atherosclerosis in a subject in need thereof, the method comprising administering a composition of claim 1 to the subject. ### Claim 10 (depends on 9) The method of claim 9, wherein the subject is at risk of atherosclerosis. ### Claim 11 (depends on 9) The method of claim 9, wherein the subject has atherosclerosis. ### Claim 12 (depends on 1) The composition of claim 1, wherein Xa is K, V, T, R, A, or Q. ### Claim 13 (depends on 1) The composition of claim 1, wherein Xa is K or T. ### Claim 14 (depends on 1) The composition of claim 1, wherein Xa is K. ### Claim 15 (depends on 1) The composition of claim 1, wherein Xb is A, S, G, N, T, or K. ### Claim 16 (depends on 1) The composition of claim 1, wherein Xb is A, S, or N. ### Claim 17 (depends on 1) The composition of claim 1, wherein Xb is A. ### Claim 18 (depends on 1) The composition of claim 1, wherein Xc is T, S, K, A, V, R, L, or absent. ### Claim 19 (depends on 1) The composition of claim 1, wherein Xc is T, S, or K. ### Claim 20 (depends on 1) The composition of claim 1, wherein Xc is T. ### Claim 21 (depends on 1) The composition of claim 1, wherein Xa is K, V, T, R, A, or Q, Xb is A, S, G, N, T, or K, and Xc is T, S, K, A, V, R, L, or absent. ### Claim 22 (depends on 1) The composition of claim 1, wherein Xa is K or T, Xb is A, S, or N, and Xc is T, S, or K. ### Claim 23 (depends on 1) The composition of claim 1, wherein Xa is K, Xb is A, and Xc is T.