Tumor targeting with polymeric molecules having extended conformation
Patent 5762909 Issued on June 9, 1998. Estimated Expiration Date: 
August 1, 2016. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
August 1, 2016. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.Patent ReferencesHigh molecular compounds having amino groups, and their utilization Amphipathic polychelating compounds and methods of use Adducts of macrocyclic chelants Medical compositions Patent #: 5593658 InventorApplicationNo. 691164 filed on 08/01/1996US Classes:424/9.34, Polypeptide attached to or complexed with the agent (e.g., protein, antibody, etc.)424/1.65, In an organic compound424/9.1, IN VIVO DIAGNOSIS OR IN VIVO TESTING424/9.3Magnetic imaging agent (e.g., NMR, MRI, MRS, etc.)ExaminersPrimary: Kight, JohnAssistant: Jones, Dameron L. Attorney, Agent or FirmInternational ClassesA61K 049/00G01N 031/00 G01N 033/48 AbstractEnhanced drug delivery to tumor tissue is obtained by attaching drug molecules to elongated polypeptide carrier molecules several orders of magnitude longer than wide. These are chosen to have a high net negative charge. The carrier molecules are created by unfolding long polypeptides by a large degree of substitution with steric hindrance molecules, such as diethylene triamine pentaacetic acid (DTPA) with at least 90% substitution. This causes the conformation to be worm-like as evidenced by a measure of persistence length, with a diameter small enough squeeze through the pore structures of tumor tissue but not so small as to pass through pores of vessels in normal tissue. The length is determined by optimizing two processes, blood circulation lifetime, and tumor uptake. The elongated conformation may cause the complex to become entwined with stroma in tumor interstitium and become trapped. The complex molecules provides increased therapeutic benefit in effecting tumor tissue destruction, or may be used in enhancing imaging contrast depending upon the active agent attached to the carrier molecules. The enhanced concentration and retention of the complex molecules within the tumor reduces side effects of the active agent in other tissues.Other References
Field of SearchRADIONUCLIDE OR INTENDED RADIONUCLIDE CONTAINING; ADJUVANT OR CARRIER COMPOSITIONS; INTERMEDIATE OR PREPARATORY COMPOSITIONSRadionuclide or intended radionuclide in an organic compound In an organic compound Attached to peptide or protein of 2+ amino acid units (e.g., dipeptide, folate, fibrinogen, transferrin, sp. enzymes); derivative thereof IN VIVO DIAGNOSIS OR IN VIVO TESTING Magnetic imaging agent (e.g., NMR, MRI, MRS, etc.) Polypeptide attached to or complexed with the agent (e.g., protein, antibody, etc.) X-ray contrast imaging agent (e.g., computed tomography, angiography, etc.) Ultrasound contrast agent PEPTIDES OF 3 TO 100 AMINO ACID RESIDUES 25 or more amino acid residues in defined sequence 24 amino acid residues in defined sequence 15 to 23 amino acid residues in defined sequence 11 to 14 amino acid residues in defined sequence 8 to 10 amino acid residues in defined sequence 6 to 7 amino acid residues in defined sequence 4 to 5 amino acid residues in defined sequence INFRARED Halogen attached directly to the diazine ring by nonionic bonding RADIOACTIVE METAL CONTAINING (At. No. 43, 61 or 84+; or radioactive isotope of another metal) Actinide series metal (At. No. 89+) Containing -C(=X)-, wherein X is chalcogen (e.g., carbonyl containing, etc.) The -C(=X)- is part of a -C(=X)X- group, wherein the X's are the same or diverse chalcogens Technetium containing (At. No. 43; Tc) RARE EARTH METAL CONTAINING (At. No. 21, 39, 57-60 or 62-71) Containing -C(=X)X-, wherein the X's are the same or diverse chalcogens Diagnostic or test agent produces in vivo fluorescence | |
