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Last Updated: January 26, 2022

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Claims for Patent: 7,037,889

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Summary for Patent: 7,037,889
Title:Pharmaceutical compositions for sustained drug delivery
Abstract: Sustained delivery formulations comprising a water-insoluble complex of a peptide and a plurality of ligands are disclosed. The formulations of the invention allow for loading of high concentrations of peptide in a small volume and for delivery of a pharmaceutically active peptide for prolonged periods, e.g., one month, after administration of the complex. The complexes of the invention can be milled or crushed to a fine powder. In powdered form, the complexes form stable aqueous suspensions and dispersions, suitable for injection. Methods of making the complexes of the invention, and methods of these complexes are also disclosed.
Inventor(s): Gefter; Malcolm L. (Lincoln, MA)
Assignee: Praecis Pharmaceuticals Inc. (Waltham, MA)
Application Number:09/953,247
Patent Claims:1. A composition comprising: (a) a peptide; (b) a plurality of ligands for said peptide, each of said ligands being negatively or positively charged; and (c) an ionic carrier macromolecule having a charge opposite to the charge of each of said ligands; wherein said plurality of ligands are linked via said macromolecule and wherein said peptide, said plurality of ligands, and said carrier macromolecule together form a water insoluble complex.

2. The composition of claim 1, wherein each of said ligands is a peptidic compound.

3. The composition of claim 1, wherein each of said ligands is a non-peptidic compound.

4. The composition of claim 1, wherein each of said ligands comprises an amino acid sequence bearing a net electronic charge.

5. The composition of claim 1, wherein the peptide is selected from the group consisting of insulin, erythropoietin, growth hormone, bradykinin, parathyroid hormone, adenocorticotrophic hormone, calcitonin, vasopressin, angiotensin, desmopressin, luteinizing hormone-releasing hormone, somatostatin, glucagon, somatomedin, oxytocin, gastrin, secretin, melanocyte stimulating hormone, beta-endorphin, enkephalin, neurotensin, thyroid releasing hormone, and macrophage stimulating factor.

6. The composition of claim 1, wherein the peptide is an LHRH analogue.

7. The composition of claim 6, wherein the LHRH analogue is an LHRH antagonist having the following structure: Ac-D-Nal-4-Cl-D-Phe-D-Pal-Ser-N-Me-Tyr-D-Asn-Leu-Lys(iPr)-Pro-D-Ala.

8. The composition of claim 6, wherein the LHRH analogue is the LHRH agonist Leuprolide having the structure pGlu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro(ethylamide)-Gly.

9. The composition of claim 6, wherein the LHRH analogue is the LHRH antagonist Cetrorelix having the structure Ac-D-Nal-4-Cl-D-Phe-D-Pal-Ser-Tyr-D-Cit-Leu-Arg-Pro-D-Ala.

10. The composition of claim 1, wherein each of said ligands is cationic and the carrier is macromolecule is anionic.

11. The composition of claim 1, wherein each of said ligands is anionic and the carrier macromolecule is anionic.

12. The composition of claim 1, wherein the carrier macromolecule is selected from the group consisting of poly(allylamine, poly(vinylamine), poly(ethyleneimine), N-alkylated, poly(allylamine), N-alkylated poly(vinylamine) and N-alkylated poly(ethyleneimine).

13. The composition of claim 1, wherein the composition provides sustained delivery of the peptide to a subject for at least one week after the composition is administered to the subject.

14. The composition of claim 1, wherein the composition provides sustained delivery of the peptide to a subject for at least two weeks alter the composition is administered to the subject.

15. The composition of claim 1, wherein the composition provides sustained delivery of the peptide to a subject for at least four weeks after the composition is administered to the subject.

16. The composition of claim 1, wherein said peptide is releasable in vivo in a pharmaceutically active form.

17. A composition comprising: (a) a peptide; (b) a plurality of ligands for said peptide, each of said ligands comprising a first region suitable for binding said peptide and a second region that is negatively or positively charged; and (c) an ionic carrier macromolecule having a charge opposite to the charge of said second region in each of said ligands; wherein said peptide, said plurality of ligands, and said carrier macromolecule together form a water insoluble complex.

18. The composition of claim 17, wherein each of said ligands is a peptidic compound.

19. The composition of claim 17, wherein each of said ligands is a non-peptidic compound.

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Serving leading biopharmaceutical companies globally:

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