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Exenatide, an incretin mimic peptide comprised of 39 amino acid residue, is a new antidiabetic drug approved by FDA in 2005 for the treatment of diabetes mellitus type 2.
The main physiological functions are followings: promote insulin excretion in glucose-dependence manner, restoration of glucose sensitivity to the islets, inhibition of apoptosis of existing cells and increase the number of β cells, inhibition of gastric emptying leads to decreased food intake and reduced body weight. The exenatide therapy has the following advantages to compare with insulin therapy: no hypoglycemia effect, reducing body weight, improving insulin resistance, promoting islets cell function of patients.
Exenatide is developed and marketed (brand name Byetta) by Amylin Pharmaceuticals and Eli Lilly and Company. Due to some historical reasons, there is no compound patent for the drug in many countries. The API of the drug and generics have been developed and currently under clinical trial in China. Beyel Pharmaceutical is capable of manufacturing Exenatide Acetate by solid phase synthesis under GMP compliance.
Essential information
Amino acid sequence:
H-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln–Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2
Molecular formula: C184H282N50O60S
Molecular weight: 4186.61
Quality standard-1
Appearance: White powder
Water content (Karl Fischer): ≤5%
Acetate content (HPLC method):≤5%
Amino acid composition: ±10% theoretical value
Purity (by two HPLC methods): ≥99.0%
Single impurity (by two HPLC methods): ≤0.5%
Total impurity (by two HPLC methods): ≤1.0%
Peptide content (Kjeldahl method): ≥85%
Assay (anhydrous, without acetate): 95%-103%
Bacterial endotoxins: ≤5EU/mg
Package: plastic bottle (peptide special) or glass vial
Short-term storage: avoid from moisture and light at 2-8°C
Long-term storage: avoid from moisture and light at -20°C
Period of validity: 2.0 years
Quality standard-2
Appearance: White powder
Water content (Karl Fischer): ≤7%
Acetate content (HPLC method): ≤7%
Amino acid composition: ±10% theoretical value
Purity (by two HPLC methods): ≥98.0%
Single impurity (by two HPLC methods): ≤1.0%
Total impurity (by two HPLC methods): ≤2.0%
Peptide content (Kjeldahl method): ≥85%
Assay (anhydrous, without acetate): 95%-103%
Bacterial endotoxins: ≤5EU/mg
Package: plastic bottle (peptide special) or glass vial
Short-term storage: avoid from moisture and light at 2-8°C
Long-term storage: avoid from moisture and light at -20°C
Period of validity: 2.0 years