Ester-based peptide prodrugs

Details Ester-based peptide prodrugs Ester-based peptide prodrugs

C - Chemistry, Metallurgy

07

K

C07K 14/62 (2006.01) A61K 38/16 (2006.01) A61K 38/26 (2006.01) A61K 38/28 (2006.01) A61P 3/04 (2006.01) A61P 3/10 (2006.01) C07K 1/107 (2006.01) C07K 14/605 (2006.01)

Patent

CA 2713348

Prodrug formulations of bioactive polypeptides are provided wherein the bioactive polypeptide has been modified by the linkage of a dipeptide to the bioactive polypeptide through an ester linkage. The prodrugs disclosed herein in some embodiments have extended half lives of at least 1.5 hours (e.g., at least 10 hours), and more typically greater than 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.

Cette invention concerne des préparations de promédicaments de polypeptides bioactifs où le polypeptide bioactif a été modifié par liaison dun dipeptide au polypeptide bioactif grâce à une liaison ester. Les promédicaments décrits ici dans certains modes de réalisation présentent des demi-vies prolongées dau moins 1,5 heures (par exemple au moins 10 heures), et plus généralement supérieures à 20 heures et inférieures à 70 heures, puis sont convertis en forme active dans des conditions physiologiques par réaction non enzymatique menée par instabilité chimique.

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