Back to results
US 2009/0023652 A1Published application
Polycationic calcium modulator peptides for the treatment of hyperparathyroidism and hypercalcemic disorders
AssigneeKAI Pharmaceuticals, Inc.
InventorsGregory Bell, Sarah Walter, Felix Karim
Life of this patent
Estimating the term…
Abstract
The present invention provides methods and kits for treating hyperparathyroidism, bone disease and/or hypercalcemic disorders. In particular, methods for lowering serum PTH and serum calcium using polycationic calcium modulator peptides are provided. The calcium modulator peptides can be used to treat subjects having, for example: primary, secondary or tertiary hyperparathyroidism; hypercalcemia of malignancy; metastatic bone disease; or osteoporosis.
Claims27
A method for decreasing parathyroid hormone (PTH) levels in a subject, comprising:
- administering a therapeutically effective amount of a calcium modulator peptide to a subject in need thereof, whereby serum PTH is reduced;
- wherein the calcium modulator peptide comprises:
- a) a polycationic peptide comprising 5 to 20 amino acids which are positively charged at physiological pH, an amino terminus, a carboxy terminus, and a first thiol-containing residue;
- wherein the polycationic peptide is chemically modified at the amino terminus, the carboxy terminus, or both;
- and
- b) a cargo peptide comprising a second thiol-containing residue;
- wherein the second thiol-containing residue is disulfide bonded to the first thiol-containing residue.
4 more elements
A method for decreasing parathyroid hormone (PTH) levels in a subject, comprising:
- administering a therapeutically effective amount of a calcium modulator peptide to a subject in need thereof, whereby serum PTH is reduced;
- wherein the calcium modulator peptide comprises:
- a) a first polycationic peptide comprising at least 3 amino acids which are positively charged at physiological pH, a first amino terminus, a first carboxy terminus, and a first thiol-containing residue;
- wherein the first polycationic peptide is chemically modified at the first amino terminus, the first carboxy terminus, or both;
- and
- b) a second polycationic peptide comprising at least 3 amino acids which are positively charged at physiological pH, a second amino terminus, a second carboxy terminus, and a second thiol-containing residue;
- wherein the second polycationic peptide is chemically modified at the second amino terminus, the second carboxy terminus, or both;
- wherein the calcium modulator peptide comprises 6 to 30 amino acids which are positively charged at physiological pH.
5 more elements
A method for decreasing parathyroid hormone (PTH) levels in a subject, comprising:
- administering a therapeutically effective amount of a calcium modulator peptide to a subject in need thereof, whereby serum PTH is reduced;
- wherein the calcium modulator peptide comprises:
- a polycationic peptide comprising 5 to 20 amino acids which are positively charged at physiological pH, an amino terminus, a carboxy terminus, and a first thiol-containing residue;
- wherein the polycationic peptide is chemically modified at the amino terminus, the carboxy terminus, or both;
- and
- wherein the first thiol-containing residue contains a thiol group which may be present as a free thiol or in a protected form.
3 more elements
A method for treating hypercalcemia, comprising:
- administering a therapeutically effective amount of a calcium modulator peptide to a subject in need thereof, whereby serum calcium is reduced;
- wherein the calcium modulator peptide comprises:
- a) a polycationic peptide comprising 5 to 20 amino acids which are positively charged at physiological pH, an amino terminus, a carboxy terminus, and a first thiol-containing residue;
- wherein the polycationic peptide is chemically modified at the amino terminus, the carboxy terminus, or both;
- and
- b) a cargo peptide comprising a second thiol-containing residue;
- wherein the second thiol-containing residue is disulfide bonded to the first thiol-containing residue.
4 more elements
A method for treating hypercalcemia, comprising:
- administering a therapeutically effective amount of a calcium modulator peptide to a subject in need thereof, whereby serum calcium is reduced;
- wherein the calcium modulator peptide comprises:
- a) a first polycationic peptide comprising at least 3 amino acids which are positively
- charged at physiological pH, a first amino terminus, a first carboxy terminus, and a first thiol-containing residue;
- wherein the first polycationic peptide is chemically modified at the first amino terminus, the first carboxy terminus, or both;
- and
- b) a second polycationic peptide comprising at least 3 amino acids which are positively charged at physiological pH, a second amino terminus, a second carboxy terminus, and a second thiol-containing residue;
- wherein the second polycationic peptide is chemically modified at the second amino terminus, the second carboxy terminus, or both;
- wherein the calcium modulator peptide comprises 6 to 16 amino acids which are positively charged at physiological pH.
6 more elements
A method for treating hypercalcemia, comprising:
- administering a therapeutically effective amount of a calcium modulator peptide to a subject in need thereof, whereby serum calcium is reduced;
- wherein the calcium modulator peptide comprises:
- a polycationic peptide comprising 5 to 20 amino acids which are positively charged at physiological pH, an amino terminus, a carboxy terminus, and a first thiol-containing residue;
- wherein the polycationic peptide is chemically modified at the amino terminus, the carboxy terminus, or both;
- and
- wherein the first thiol-containing residue contains a thiol group which may be present as a free thiol or in a protected form.
3 more elements
A calcium modulator peptide comprising:
- a) a polycationic peptide comprising 5 to 20 amino acids which are positively charged at physiological pH, an amino terminus, a carboxy terminus, and a first thiol-containing residue;
- wherein the polycationic peptide is chemically modified at the amino terminus, the carboxy terminus, or both;
- and
- b) a cargo peptide comprising a second thiol-containing residue;
- wherein the second thiol-containing residue is disulfide bonded to the first thiol-containing residue.
2 more elements
A calcium modulator peptide comprising:
- a) a first polycationic peptide comprising at least 3 amino acids which are positively charged at physiological pH, a first amino terminus, a first carboxy terminus, and a first thiol-containing residue;
- wherein the first polycationic peptide is chemically modified at the first amino terminus, the first carboxy terminus, or both;
- and
- b) a second polycationic peptide comprising at least 3 amino acids which are positively charged at physiological pH, a second amino terminus, a second carboxy terminus, and a second thiol-containing residue;
- wherein the second polycationic peptide is chemically modified at the second amino terminus, the second carboxy terminus, or both;
- wherein the calcium modulator peptide comprises 6 to 16 amino acids which are positively charged at physiological pH.
3 more elements
A calcium modulator peptide comprising:
- a polycationic peptide comprising 5 to 20 amino acids which are positively charged at physiological pH, an amino terminus, a carboxy terminus, and a first thiol-containing residue;
- wherein the polycationic peptide is chemically modified at the amino terminus, the carboxy terminus, or both;
- and
- wherein the first thiol-containing residue contains a thiol group which may be present as a free thiol or in a protected form.
1 more element
Dependencies are inferred from the claim text.