A novel acylated insulin analog
US-2024374692-A1 · Nov 14, 2024 · US
US8946147B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-8946147-B2 |
| Application number | US-201113702197-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jun 23, 2011 |
| Priority date | Jun 24, 2010 |
| Publication date | Feb 3, 2015 |
| Grant date | Feb 3, 2015 |
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Prodrug formulations of insulin and insulin analogs are provided wherein the insulin peptide has been modified by an amide bond linkage of a dipeptide prodrug element. The prodrugs disclosed herein have extended half lives of at least 10 hours, and more typically greater than 2 hours, 20 hours and less than 70 hours, and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability.
Opening claim text (preview).
What is claimed: 1. An insulin analog comprising the structure: X—Y—Z; wherein Z is an insulin peptide comprising an A chain and a B chain wherein the A chain comprises the sequence GIVEQCCX 1 SICSLYQLENX 2 CX 3 (SEQ ID NO: 3), or an analog thereof comprising a sequence that differs from SEQ ID NO: 3 by 1 to 3 amino acid modifications, selected from positions A5, A8, A9, A10, A14, A15, A17, A18 and the B chain comprises the sequence of X 14 -X 4 LCGX 5 X 6 LVEALX 7 LVCGERGFX…
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