Stabilized analogues of calcitonin
AssigneeYissum Research Development Company of the Hebrew University of Jerusalem
InventorsNorman MET ANIS, Hiba GHAREEB
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Abstract
The present invention provides stabilized calcitonin analogues that demonstrate improved stability and bioavailability. The present invention also provides pharmaceutical compositions of the stabilized calcitonin analogues as well as their use in methods of treating and preventing calcium-related and bone-related disorders and diseases.
Claims21
-34. (canceled)
A stabilized, bicyclic peptide analogue of calcitonin comprising the amino acid sequence X1-Ser-Asn-Leu-Ser-Thr-X2-Val-Leu-Gly-Lys-Leu-Ser-Gln-Glu-Leu-His-X3-Leu-Gln-Thr-Tyr-Pro-X4-Thr-Asn-Thr-Gly-Ser-Gly-Thr-Pro-NH2 (SEQ ID NO:
- 1), wherein X1 and X2 are independently selected from Cys (C) and modified Cys residues;
- X3 is selected from Lys (K) and a modified Lys comprising a bulky moiety connected to its ε-amine;
- and X4 is selected from Gln (Q) and Arg (R), wherein a first bridge connects positions 1 and 7 and a second bridge connects positions Lys11 and Tyr22, or a derivative thereof comprising 1-3 modifications to SEQ ID NO:
- 1, wherein the stabilized bicyclic calcitonin analogue consists of 29-35 amino acids.
Dependencies are inferred from the claim text.