Claims
- 1. A method for treating cancer in a subject, said method comprising administering to said subject an effective amount of a glucose-anti-neoplastic agent conjugate, wherein said glucose-anti-neoplastic agent conjugate has the formula: Glc-L-Z, wherein Glc is 2-deoxy-D-glucose or a 2-deoxy-D-glucose derivative; L is a non-releasable linkage; and Z is an anti-neoplastic agent.
- 2. A method in accordance with claim 1, wherein said 2-deoxy-D-glucose or 2-deoxyglucose derivative is selected from the group consisting of 2-deoxy-D-glucose, 2-deoxy-D-gulose, 2-deoxy-D-galactose, 2-deoxy-2-amino-D-glucose, 2-deoxy-2-amino-D-gulose, 2-deoxy-2-amino-D-galactose, and 2-deoxy-2-amino-D-mannose.
- 3. A method in accordance with claim 1, wherein Z is an anti-neoplastic agent selected from the group consisting of a radionuclide selected from the group consisting of Yttrium-90, Iodine-125, Iodine-131, and Phosphate-32; an iodoaryl group bearing an Iodine-131; hydroxyurea; a ribonucleotide reductase inhibitor that chelates iron; 3-aminopyridine-2-carboxaldehyde thiosemicarabazone; 5-hydroxypyridine-2-carboxaldehyde thiosemicarbazone; camptothecin and its analogs; carboplat and its analogs; DOTA and other radiometal ion chelators; methotrexate and its analogs; mitoxantrone and related anthraquinones; a protein kinase inhibitor; dacarbazine and procarbazine; and mitomycin.
- 4. A method in accordance with claim 1, wherein Z is 4-131iodo-N-2 benzoyl-glucosamine.
- 5. A method in accordance with claim 1, wherein L is a non-releasable linkage having from 2 to 30 atoms selected from the group consisting of C, N, O, P, S and Si.
- 6. A method in accordance with claim 1, wherein said glucose-anti-neoplastic agent conjugate has the formula:
- 7. A method in accordance with claim 1, wherein said glucose-anti-neoplastic agent conjugate has the formula:
- 8. A method in accordance with claim 1, further comprising administering at least one additional anti-neoplastic agent.
- 9. A method of claim 8, wherein said at least one additional anti-neoplastic agent is a member selected from the group consisting of cyclophosphamide, doxorubicin, prednisone and cisplatin.
- 10. A method in accordance with claim 1, wherein said cancer is selected from the group consisting of lung cancer, breast cancer, prostate cancer, colon cancer, ovarian cancer, cervical cancer, esophageal cancer, bladder cancer, brain cancer, head and neck cancer, skin cancer and melanoma.
- 11. A method in accordance with claim 1, wherein said cancer is selected from the group consisting of low grade non-Hodgkin's Lymphoma, intermediate grade non-Hodgkin's Lymphoma, follicular lymphoma, large cell lymphoma, B-cell lymphoma, T-cell lymphoma, Mantle cell lymphoma, Burkitt's lymphoma, NK cell lymphoma and acute lymphoblastic lymphoma.
- 12. A method in accordance with claim 1, wherein said cancer is selected from the group consisting of relapsed cancer and refractory cancer.
- 13. A method in accordance with claim 1, further comprising a preliminary step of reducing glucose ingestion in said subject.
- 14. A glucose-anti-neoplastic agent conjugate having the formula: Glc-L-Z, wherein Glc is 2-deoxyglucose or a 2-deoxyglucose derivative; L a non-releasable linking group; and Z is an anti-neoplastic agent.
- 15. A glucose-anti-neoplastic agent conjugate of claim 14, having the formula:
- 16. A glucose-anti-neoplastic agent conjugate of claim 15, having the formula:
- 17. A glucose-anti-neoplastic agent conjugate of claim 15, wherein Z is an anti-neoplastic agent selected from the group consisting of a radionuclide selected from the group consisting of Yttrium-90, Iodine-125, Iodine-131, and Phosphate-32; an iodoaryl group bearing an Iodine-131; hydroxyurea; a ribonucleotide reductase inhibitor that chelates iron; 3-aminopyridine-2-carboxaldehyde thiosemicarabazone; 5-hydroxypyridine-2-carboxaldehyde thiosemicarbazone; camptothecin and its analogs; carboplat and its analogs; DOTA and other radiometal ion chelators; methotrexate and its analogs; mitoxantrone and related anthraquinones; a protein kinase inhibitor; dacarbazine and procarbazine; and mitomycin.
- 18. A compound of structure:
- 19. A composition comprising a pharmaceutically acceptable carrier and a glucose-anti-neoplastic agent conjugate of claim 15.
- 20. The composition of claim 19 that comprises 4-iodo-N-benzoyl-glucosamine and 4-131iodo-N-benzoylglucosamine.
CROSS-REFERENCES TO RELATED APPLICATIONS
[0001] This application claims priority to U.S. provisional patent application Serial No. 60/429,287, filed Mar. 29, 2002, incorporated herein by reference.
Provisional Applications (1)
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Number |
Date |
Country |
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60429287 |
Mar 2002 |
US |