PHARMACEUTICAL COMPOSITION OF A LONG-ACTING DUAL GLP-1 / GIP AGONIST

Claims

The present invention provides a pharmaceutical composition comprising a long-acting dual GLP-1 / GIP agonist, a kit comprising the pharmaceutical composition, and the use of the pharmaceutical composition in the manufacture of a drug for treating diabetes mellitus or obesity.

1. A pharmaceutical composition, wherein the pharmaceutical composition has a pH in the range from approximately 5.0 to approximately 9.0, and the pharmaceutical composition comprises from approximately 0.1 to approximately 50 mg / mL of a polypeptide compound of the following formula I: Y-Aib-EGT-αMePhe-TSDY-Aib-I-Aib-LDKQAQAEFVK 24 -WLLK 28 -GGPSSGAPPPSK formula I (SEQ ID No. 12);wherein 1 K, which is selected from the group consisting of K at position 16, K at position 24, K at position 28 and K at position 40 of formula I, is chemically modified through conjugation of the amino acid ε of the side chain of K with ([2-(2-amino-ethoxy)-ethoxy]-acetyl)a-(γ-Glu)b-CO-(CH2)cZ, wherein each a is independently selected from an integer of 1, 2 and 3, each b is independently selected from an integer of 1, 2 and 3, and each c is independently selected from an integer of 16, 18 and 20, wherein Z is independently selected from the group consisting of -CH3, carboxylic acids or bioisoesters of carboxylic acids, phosphonates or sulfonates, preferably -COOH; and the C-terminal amino acid is amidated as a C-terminal primary amide.