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Last Updated: April 20, 2024

Claims for Patent: 6,818,630


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Summary for Patent: 6,818,630
Title: Biologically active materials
Abstract:The present disclosure concerns biologically active materials, particularly materials that comprise a biodegradeable polymer linked to a biologically active agent. The disclosure further concerns materials known as polymer-drug conjugates that typically contain a therapeutic agent, for instance a bioactive cytotoxic drug linked to a polymer backbone. The linkage typically is a convalent linkage. However, in some embodiments the disclosure concerns other polymer conjugates including those where the biologically active agent is an imaging agent, such as a tyrosinamide, a diagnostic agent, or a targeting agent, such as biotin.
Inventor(s): Duncan; Ruth (Cardiff, GB), Hreczuk-Hirst; Dale (London, GB), German; Lisa (London, GB)
Assignee: ML Laboratories PLC (London, GB)
Application Number:10/018,608
Patent Claims:1. A polymer drug conjugate comprising: at least one anti-cancer agent; and a dextrin polymer, wherein said dextrin polymer is modified by succinoylation by at least 30 mol % characterised in that the stability of the polymer drug conjugate is enhanced.

2. The polymer drug conjugate according to claim 1, wherein said dextrin is succinoylated from 30% to 40 mol %.

3. The polymer drug conjugate according to claim 2, wherein said dextrin is succinoylated from 32% to 36 mol %.

4. The polymer drug conjugate according to claim 3, wherein said dextrin is succinoylated to about 34 mol %.

5. The polymer drug conjugate according to claim 1, wherein the percentage of .alpha.-1-6 linkages in the dextrin is less than 10%.

6. The polymer drug conjugate according to claim 5, wherein the percentage of .alpha. 1-6 linkages in the dextrin is less than 5%.

7. The polymer drug conjugate according to claim 1, wherein the molecular weight of the dextrin is in an average molecular weight range 1000-200000.

8. The polymer drug conjugate according to claim 7, wherein the molecular weight of the dextrin is in an average molecular weight range 2000-55000.

9. The polymer drug conjugate according to any of claim 1, wherein the dextrin contains more than 15% of polymers of DP greater than 12.

10. The polymer drug conjugate according to claim 9, wherein the dextrin contains more than 50% of polymers of DP greater than 12.

11. A polymer drug conjugate according to claim 1, wherein said anti cancer agent is selected from the group consisting of: cyclophosphamide; melphalan; carmusline; methotrexate, 5-fluorouracil; cytarabine; mercaptopurine; anthracyclines; daunorubicin, doxorubicin; epirubicin; vinca alkaloids; vinblastin; vincristine; dactinomycin; mitomycin C; taxol; L-asparaginase; G-CSF; cisplatin; and, optionally, carboplatin.

12. A pharmaceutical composition, comprising the polymer drug conjugate according to claim 1 and a pharmaceutically acceptable diluent, excipient or carrier.

13. A polymer drug conjugate comprising: at least one biologically active agent; and a dextrin polymer, wherein said dextrin polymer is modified by succinoylation by at least 30 mol % characterised in that the stability of the polymer drug conjugate is enhanced.

14. The polymer conjugate according to claim 13, wherein said agent is an imaging agent.

15. The polymer conjugate according to claim 14, wherein the imaging agent is tyrosinamide.

16. The polymer conjugate according to claim 13, wherein said agent is a diagnostic agent.

17. The polymer conjugate according to claim 13 wherein said agent is a targeting agent.

18. The polymer conjugate according to claim 17 wherein the targeting agent is biotin.

19. A method for treating a cancer in an animal subject, comprising administering to the animal a pharmaceutically effective amount of the polymer drug conjugate according to claim 1, thereby treating the cancer in the subject.

20. The method according to claim 19 wherein said animal is human.

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