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Lanreotide

蘭瑞肽

Mechanism of action:

Lanreotide 是一種體抑素類似物(somatostatin analog),屬於胜肽激素(peptide hormone)。Lanreotide 對體抑素受體(somatostatin receptor)包含 SSTR2 與 SSTR5 具有高度親和力,這兩種受體在垂體生長激素分泌細胞和神經內分泌腫瘤細胞上表達特別豐富。Lanreotide 能活化 SSTR2 與 SSTR5,透過 Gi/o 蛋白偶聯機制,抑制腺苷酸環化酶(adenylate cyclase),降低細胞內 cAMP 濃度,抑制鈣離子內流,最終使生長激素分泌下降,進而降低胰島素樣生長因子1(IGF-1)濃度。此外,lanreotide 亦可降低部分神經內分泌腫瘤相關的激素分泌,並影響腸道分泌與蠕動,同時可透過體抑素受體相關訊號調節細胞增殖與分泌功能。

​Reference(s):

1. Troconiz IF et al. (2009). Population pharmacokinetic analysis of lanreotide Autogel in healthy subjects: evidence for injection interval of up to 2 months. Clin Pharmacokinet. 


2. Giustina A et al. (2014). Investigational drugs targeting somatostatin receptors for treatment of acromegaly and neuroendocrine tumors. Expert Opin Investig Drugs.

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