The Sound of Evolution
Sitagliptin
西格列汀
Mechanism of action:
Sitagliptin 是一種二肽基肽酶-4 抑制劑（dipeptidyl peptidase-4 inhibitor）。二肽基肽酶-4（DPP-4）是一種負責分解腸泌素的酵素，腸泌素比如胰高血糖素樣肽-1（glucagon-like peptide-1）和葡萄糖依賴性促胰島素多肽（glucose-dependent insulinotropic polypeptide）等。當 sitagliptin 抑制二肽基肽酶-4 後，使腸泌素不易被分解，在血中濃度與作用時間延長，能促進胰島 β 細胞分泌胰島素；抑制胰島 α 細胞分泌升糖素（glucagon）。
Reference(s):
1. Herman GA et al. (2005). Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses. Clin Pharmacol Ther.
2. Herman GA et al. (2006). Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects. J Clin Pharmacol.
3. Karasik A et al. (2008). Sitagliptin, a DPP-4 inhibitor for the treatment of patients with type 2 diabetes: a review of recent clinical trials. Curr Med Res Opin.