Insulin vitamin D conjugates
First Claim
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1. A carrier-drug conjugate, comprising a targeting group that is a non-hormonal vitamin D not hydroxylated at the carbon 1 position, conjugated to an insulin peptide at the carbon 3 position of said non-hormonal vitamin D targeting group.
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Abstract
The invention provides non-hormonal vitamin D conjugated to insulin peptides that result in the peptides having increased absorption, bioavailability or circulating half-life when compared to non-conjugated forms. The vitamin D targeting groups are coupled to the insulin peptides via the third carbon on the vitamin D backbone.
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Citations
22 Claims
- 1. A carrier-drug conjugate, comprising a targeting group that is a non-hormonal vitamin D not hydroxylated at the carbon 1 position, conjugated to an insulin peptide at the carbon 3 position of said non-hormonal vitamin D targeting group.
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3. A pharmaceutical composition, comprising a carrier-drug conjugate comprising a targeting group that is a non-hormonal vitamin D not hydroxylated at the carbon 1 position, conjugated via a scaffold at the carbon 3 position to an insulin comprising a first peptide having an amino acid sequence with at least a 90% sequence identity to SEQ ID NO:
- 1 and a second peptide having an amino acid sequence with at least a 90% sequence identity to SEQ ID NO;
2. - View Dependent Claims (4, 5, 6, 7, 8, 9, 10)
- 1 and a second peptide having an amino acid sequence with at least a 90% sequence identity to SEQ ID NO;
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11. A pharmaceutical composition, comprising:
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a) an insulin peptide, b) a stably attached scaffold, c) a targeting group that is a non-hormonal vitamin D not hydroxylated at the carbon 1 position, conjugated at the carbon 3 position, wherein after administration to a first test subject, said insulin peptide has a half-life measured by an enzyme immunoassay (EIA) of blood samples taken at a plurality of time points that is greater than a half-life of said insulin peptide administered to a second test subject without said stably attached scaffold moiety and targeting group as measured by said EIA of blood samples taken at said plurality of time points. - View Dependent Claims (12, 13, 14, 15)
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- 16. A carrier-drug conjugate, comprising a targeting group that is vitamin D that is not hydroxylate at the carbon 1 position non-releasably conjugated to a first insulin peptide, wherein said insulin peptide is conjugated at the carbon 3 position of said vitamin D targeting group.
Specification