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帕西瑞肽——作用机制与临床应用

Pasireotide - Mechanism of Action and Clinical Applications.

作者信息

Sawicka-Gutaj Nadia, Owecki Maciej, Ruchala Marek

机构信息

Department of Endocrinology, Metabolism, and Internal Medicine, Faculty of Medicine II, Poznan University of Medical Sciences, Poznan, Poland.

Department of Public Health, Faculty of Medicine I, Poznan University of Medical Sciences, Poznan, Poland.

出版信息

Curr Drug Metab. 2018;19(10):876-882. doi: 10.2174/1389200219666180328113801.

DOI:10.2174/1389200219666180328113801
PMID:29595102
Abstract

BACKGROUND

Pasireotide (SOM230) is a multi-receptor ligand somatostatin analogue (SSA) developed as the successor of the first-generation SSAs. Currently, pasireotide is recommended for the treatment of patients with Cushing's disease in whom surgery was unsuccessful, and patients with acromegaly who either remain uncontrolled after surgical therapy or in whom tumor resection is not possible.

METHODS AND RESULTS

Phase II and III clinical trials have shown pasireotide efficacy in these diseases, with a similar rate of adverse events when compared with first-line SSA, although higher incidence of hyperglycemia has been observed.

CONCLUSION

Pasireotide therapy provides biochemical control, tumor volume reduction, and improves the quality of life in patients with those disorders. Furthermore, pasireotide might be considered as second-line therapy in patients with metastatic neuroendocrine tumors, and it also might be effective in other neoplasms with a high expression of somatostatin receptors. In addition, therapy with this novel agent has been effective in prevention of postoperative complications after pancreatectomy. However, considering the diversified responsiveness to this drug in vivo, future studies should identify factors predicting better clinical response to pasireotide.

摘要

背景

帕西瑞肽(SOM230)是一种多受体配体生长抑素类似物(SSA),作为第一代SSA的后继药物而研发。目前,帕西瑞肽被推荐用于治疗手术失败的库欣病患者,以及手术治疗后仍未得到控制或无法进行肿瘤切除的肢端肥大症患者。

方法与结果

II期和III期临床试验已表明帕西瑞肽在这些疾病中具有疗效,与一线SSA相比不良事件发生率相似,尽管已观察到高血糖发生率更高。

结论

帕西瑞肽治疗可实现生化控制、减小肿瘤体积,并改善这些疾病患者的生活质量。此外,帕西瑞肽可被视为转移性神经内分泌肿瘤患者的二线治疗药物,并且它可能对生长抑素受体高表达的其他肿瘤也有效。此外,使用这种新型药物进行治疗已有效预防了胰腺切除术后的并发症。然而,考虑到体内对该药物的反应具有多样性,未来的研究应确定预测对帕西瑞肽有更好临床反应的因素。

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Pasireotide - Mechanism of Action and Clinical Applications.帕西瑞肽——作用机制与临床应用
Curr Drug Metab. 2018;19(10):876-882. doi: 10.2174/1389200219666180328113801.
2
Pasireotide, a multi-somatostatin receptor ligand with potential efficacy for treatment of pituitary and neuroendocrine tumors.帕西瑞肽,一种多生长抑素受体配体,对治疗垂体和神经内分泌肿瘤具有潜在疗效。
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Pasireotide--a somatostatin analog for the potential treatment of acromegaly, neuroendocrine tumors and Cushing's disease.帕西瑞肽——一种用于潜在治疗肢端肥大症、神经内分泌肿瘤和库欣病的生长抑素类似物。
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Pasireotide (SOM230): development, mechanism of action and potential applications.帕西瑞肽(SOM230):研发、作用机制及潜在应用
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Hyperglycemia induced by pasireotide in patients with Cushing's disease or acromegaly.帕瑞肽在库欣病或肢端肥大症患者中诱发的高血糖症。
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Pasireotide (SOM230) demonstrates efficacy and safety in patients with acromegaly: a randomized, multicenter, phase II trial.帕瑞肽(SOM230)治疗肢端肥大症的疗效和安全性:一项随机、多中心、II 期临床试验。
J Clin Endocrinol Metab. 2010 Jun;95(6):2781-9. doi: 10.1210/jc.2009-2272. Epub 2010 Apr 21.

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