Pasireotide (SOM230) is a multi-receptor ligand somatostatin analogue with high binding affinity for somatostatin receptor subtypes sst(1,2,3) and sst(5). Pasireotide potently suppresses GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. The prolonged inhibition of hormone secretion by pasireotide in animal models and expression of multiple sst receptors in carcinoid tumors suggests that pasireotide may have clinical advantages over octreotide in patients with carcinoid tumors. Direct and indirect antitumor activity has been observed in vitro with pasireotide, including sst receptor-mediated apoptosis and antiangiogenesis, suggesting a possible role for pasireotide in antineoplastic therapy. In summary, preclinical evidence, as well as preliminary results from clinical studies suggests that pasireotide is a promising new treatment for patients with symptoms of metastatic carcinoid tumors refractory or resistant to octreotide, de novo or persistent acromegaly, and that pasireotide has the potential to be the first directed medical therapy for Cushing's disease.

中文翻译：

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Pasireotide（SOM230）：开发，作用机理和潜在应用。

Pasireotide（SOM230）是一种多受体配体生长抑素类似物，对生长抑素受体亚型sst（1,2,3）和sst（5）具有高结合亲和力。帕雷西肽有效抑制GH，IGF-I和ACTH分泌，表明在肢端肥大症和库欣病中具有潜在疗效。在动物模型中，pasireotide对激素分泌的长期抑制和多种sst受体的表达表明，pasireotide在类癌患者中可能比奥曲肽具有临床优势。已在体外观察到使用Pasireotide的直接和间接抗肿瘤活性，包括sst受体介导的细胞凋亡和抗血管生成，表明pasireotide在抗肿瘤治疗中可能发挥作用。总之，临床前证据