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Linaclotide

利那洛肽

Mechanism of action:

Linaclotide 是一種鳥苷酸環化酶 C 促效劑（guanylate cyclase-C agonist）。Linaclotide 與位於小腸與結腸腸上皮細胞刷狀緣的鳥苷酸環化酶 C 結合，促進細胞內環狀鳥苷酸（cGMP）的生成。cGMP 會活化囊性纖維化穿膜傳導調節蛋白（cystic fibrosis transmembrane conductance regulator）氯離子通道，使氯離子與碳酸氫根離子分泌增加，水分隨之進入腸腔，使糞便軟化並增加腸內容物體積。

​Reference(s):

Busby RW et al. (2013). Pharmacologic properties, metabolism, and disposition of linaclotide, a novel therapeutic peptide approved for the treatment of irritable bowel syndrome with constipation and chronic idiopathic constipation. J Pharmacol Exp Ther.

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