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替洛利司他乙酯:一种用于治疗类癌综合征腹泻的新型药物。

Telotristat ethyl: a novel agent for the therapy of carcinoid syndrome diarrhea.

机构信息

Division of Endocrinology, University of Iowa Hospital & VA Medical Center, Iowa City, IA 52242, USA.

Division of Hematology Oncology, University of Iowa Hospital & VA Medical Center, Iowa City, IA 52242, USA.

出版信息

Future Oncol. 2018 May;14(12):1155-1164. doi: 10.2217/fon-2017-0340. Epub 2018 Jan 19.

Abstract

Carcinoid syndrome (CS), characterized by diarrhea and flushing, is present in 20% of patients with neuroendocrine tumors at diagnosis and becomes more frequent with progression. The diarrhea of CS is caused mainly by tumoral secretion of serotonin. It may not be fully controlled by somatostatin analogs, the currently indicated drugs for symptomatic relief. Telotristat ethyl is a novel inhibitor of tryptophan hydroxylase, the rate-limiting enzyme in serotonin biosynthesis. Administration of the drug decreases diarrhea in patients with CS. Telotristat ethyl was approved in February 2017 (USA) and September 2017 (European Commission) for the treatment of CS diarrhea in adults inadequately controlled by somatostatin analog alone. This drug is expected to greatly improve the health and quality of life of patients with CS diarrhea.

摘要

类癌综合征(CS)的特征为腹泻和潮红,20%的神经内分泌肿瘤患者在诊断时存在 CS,且随着疾病进展其发生率会逐渐增高。CS 的腹泻主要由肿瘤分泌的血清素引起。其可能无法被目前用于缓解症状的生长抑素类似物完全控制。曲替瑞林乙酯是色氨酸羟化酶的新型抑制剂,色氨酸羟化酶是血清素生物合成中的限速酶。该药物的使用可减少 CS 患者的腹泻。2017 年 2 月(美国)和 2017 年 9 月(欧盟委员会)批准曲替瑞林乙酯用于治疗生长抑素类似物单独治疗未能充分控制的 CS 腹泻。该药物有望极大地改善 CS 腹泻患者的健康和生活质量。

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