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Last Updated: March 29, 2024

Claims for Patent: 8,529,944


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Summary for Patent: 8,529,944
Title:Targeted delivery to human diseases and disorders
Abstract: The present invention provides a system presenting site-specific accumulation through a ligand that specifically targets a receptor overexpressed on the surface of specific cells within a target organ, like, for example, tumor cells and/or vascular cells of tumor blood vessels. Moreover, this invention provides a method where, upon internalization of the previous-mentioned system by the target cells, triggered release at a high rate of the associated agent takes place, permitting efficient intracellular delivery and, thus, increased concentration of the transported cargo at the target site. Overall, this invention provides a method for the diagnosis, prevention and treatment of human diseases and disorders.
Inventor(s): de Almeida Moreira; Joao Nuno Sereno (Coimbra, PT), Caldeira de Moura; Vera L cia Dantas Nunes (Coimbra, PT), de Magalhaes Simoes; Sergio Paulo (Coimbra, PT), Pedroso de Lima; Maria da Conceicao Monteiro (Coimbra, PT)
Assignee: Universidade de Coimbra (Coimbra, PT) Centro de Neurociencias e Biologia Celular (Coimbra, PT)
Application Number:13/467,178
Patent Claims:1. A ligand-targeted delivery system comprising a targeting ligand linked to a support carrying an agent, wherein said targeting ligand binds nucleolin, wherein said support is a pH sensitive liposome, wherein the agent is a therapeutic, diagnostic and/or imaging agent, encapsulated, entrapped or intercalated in the support, and wherein said liposome is capable of the pH dependent intracellular release of said agent.

2. The delivery system of claim 1, suitable for intravenous administration.

3. A ligand-targeted delivery system comprising at least one ligand linked to a support encapsulating an agent, wherein each of the at least one ligands is a peptide comprising the amino acid sequence of SEQ ID NO:1, and wherein each of the at least one ligands specifically binds nucleolin.

4. The delivery system of claim 1 wherein spacer is positioned between the ligand and the support such that the interaction of the ligand with the target is not hindered.

5. The delivery system of claim 4 wherein the spacer comprises a reactive group that is also a means of linking the ligand to the support and wherein the spacer optionally comprises a tag to facilitate recovery or identification of the system.

6. The delivery system of claim 1, wherein the support is a liposome comprising fully hydrogenated soy phosphatidylcholine, methoxy-polyethylene glycol phosphatidylethanolamine, maleimide-polyethylene glycol phosphatidylethanolamine, N-methylpalmitoyloleoylphosphatidylcholine, phosphatidylserine, phosphatidylcholine, palmitoyloleoylphosphatidylcholine, dipalmitoylphosphatidylcholine, distearoylphosphatidylcholine, phosphatidylglycerol, dioleoylphosphatidylethanolamine, cholesteryl hemisuccinate, cholesterol, or a combination thereof.

7. The delivery system of claim 1 wherein the agent is a cytotoxic, an anti-cancer, anti-inflammatory, an anti-angiogenic, an angiolytic, a vascular disrupting agent or a photodynamic therapeutic agent.

8. The delivery system of claim 1 wherein the agent is encapsulated, entrapped, or intercalated within the core of the support.

9. The delivery system of claim 8, wherein the agent is one or more selected from the group consisting of alkylating drugs; cytotoxic antibiotics; antimetabolites; vinca alkaloids; amsacrine; altetarmine; crisantaspase; dacarbazine; temozolomide; hydroxycarbamide (hydroxyurea); pentostatin; platinum compounds; porfimer sodium; procarbazine; razoxane; taxanes; topoisomerase I inhibitors; trastuzumab; tretinoin; SN-38; ET-743; TLK 286; anti-inflammatory agents; antiangiogenic agents or angiolytic agents; ABT-627; Bay 12-9566; Benefin; Bevacizumab; BMS-275291; cartilage-derived inhibitor(CDI); CAI; CD59 complement fragment; CEP-7055; Col 3; Combretastatin A-4; Endostatin (collagenXVIII fragment); Fibronectin fragment; Gro-beta; Halofuginone; Heparinases; Heparin hexasaccharide fragment; HMV833; Human chorionic gonadotropin (hCG); IM-862; Interferon alpha/beta/gamma; Interferon inducible protein (IP-10); Interleukin-12; Kringle 5 (plasminogen fragment); Marimastat; Metalloproteinase inhibitors (TIMPs); 2-Methoxyestradiol; MMI 270 (CGS 27023A); MoAbIMC-1C11; Neovastat; NM-3; Panzem; PI-88; Placental ribonuclease inhibitor; Plasminogen activator inhibitor; Platelet factor-4 (PF4); Prinomastat; Prolactin16kD fragment; Proliferin-related protein (PRP); PTK 787/ZK 222594; Retinoids; Solimastat; Squalamine; SS 3304; SU 5416; 5U6668; SU11248; Tetrahydrocortisol-S; tetrathiomolybdate; thalidomide; Thrombospondin-1(TSP-1); TNP-470; Transforming growth factor-beta (TGF-b); Vasculostatin; Vasostatin (calreticulin fragment); ZD6126; ZD 6474; farnesyl transferase inhibitors (FTI); bisphosphonates; and porphyrins.

10. The delivery system of claim 1, wherein intracellular triggered release of the agent is a function of the pH value of the target microenvironment.

11. The delivery system of claim 1 wherein the agent is released through the support destabilization in acidic environment.

12. The delivery system of claim 11 wherein the acidic pH environment comprises the endosome compartment of cells.

13. The delivery system of claim 1 labelled with a radionuclide or a fluorescent molecule.

14. The delivery system of claim 1, wherein the alkylating drugs are one or more of cyclophosphamide, chlorambucil, melphalan, busulfan, lomustine, carmustine, chlormethine (mustine), estramustine, treosulfan, thiotepa, or mitobronitol.

15. The delivery system of claim 1, wherein the cytotoxic antibiotics are one or more of doxorubicin, epirubicin, aclarubicin, idarubicin, daunorubicin, mitoxantrone (mitozantrone), bleomycin, dactinomycin or mitomycin.

16. The delivery system of claim 1, wherein the antimetabolites are one or more of methotrexate, capecitabine, cytarabine, fludarabine, cladribine, gemcitabine, fluorouracil, raltitrexed (tomudex), mercaptopurine, tegafur or tioguaninc.

17. The delivery system of claim 1, wherein the vinca alkaloids are one or more of vinblastine, vincristine, vindesine, vinorelbine or etoposide.

18. The delivery system of claim 1, wherein the platinum compounds are one or more of carboplatin, cisplatin or oxaliplatin.

19. The delivery system of claim 1, wherein the taxanes are one or more of docetaxel or paclitaxel.

20. The delivery system of claim 1, wherein the topoisomerase I inhibitors are one or both of inotecan or topotecan.

21. The delivery system of claim 1, wherein the anti-inflammatory agents are one or more of ibuprofen, aceclofenac, acemetacin, azapropazone, celecoxib, dexketoprofen, diclofenac sodium, diflunisal, cetodolac, fenbufen, fenoprofen, flubiprofen, indomethacin, acetaminocin, piroxicam, rofecoxib, sulindac, tenoxicam, tiaprofenuic acid, aspirin or benorilate.

22. The delivery system of claim 1, wherein the antiangiogenic agents or angiolytic agents are one or more of Angiostatin (plasminogen fragment), antiangiogenic antithrombin III or Angiozyme.

Details for Patent 8,529,944

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Ferring Pharmaceuticals Inc. NOVAREL chorionic gonadotropin For Injection 017016 01/15/1974 ⤷  Try a Trial 2028-05-22
Ferring Pharmaceuticals Inc. NOVAREL chorionic gonadotropin For Injection 017016 12/27/1984 ⤷  Try a Trial 2028-05-22
Ferring Pharmaceuticals Inc. NOVAREL chorionic gonadotropin For Injection 017016 02/15/1985 ⤷  Try a Trial 2028-05-22
Ferring Pharmaceuticals Inc. NOVAREL chorionic gonadotropin For Injection 017016 02/16/1990 ⤷  Try a Trial 2028-05-22
Bel-mar Laboratories, Inc. CHORIONIC GONADOTROPIN chorionic gonadotropin Injection 017054 03/26/1974 ⤷  Try a Trial 2028-05-22
Fresenius Kabi Usa, Llc CHORIONIC GONADOTROPIN chorionic gonadotropin For Injection 017067 03/05/1973 ⤷  Try a Trial 2028-05-22
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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