卡索匹坦，一种具有止吐和抗恶心活性的神经激肽-1受体拮抗剂。

Casopitant, a neurokinin-1 receptor antagonist with anti-emetic and anti-nausea activities.

作者信息

Navari Rudolph M

机构信息

Indiana University School of Medicine, South Bend, 100 Raclin-Carmichael Hall, South Bend, IN 46617, USA.

出版信息

Curr Opin Investig Drugs. 2008 Jul;9(7):774-85.

PMID:18600583

Abstract

Casopitant, an inhibitor of the neurokinin-1 receptor, and its mesylate salt, are being developed by GlaxoSmithKline plc for the potential treatment of chemotherapy-induced nausea and vomiting (CINV), post-operative nausea and vomiting (PONV), as well as for anxiety, depression and insomnia. Phase II trials are ongoing for anxiety, depression and insomnia, and further results are awaited from phase III trials of CINV and PONV. At the time of publication, it was expected that applications to the FDA for regulatory approval for CINV and PONV would be filed in 2008. Casopitant was previously being developed for the treatment of overactive bladder; however, in September 2007, this indication was no longer listed on the company's product pipeline.

摘要

卡索匹坦是一种神经激肽-1受体抑制剂，其甲磺酸盐正由葛兰素史克公司研发，用于潜在治疗化疗引起的恶心和呕吐（CINV）、术后恶心和呕吐（PONV），以及焦虑、抑郁和失眠。针对焦虑、抑郁和失眠的II期试验正在进行，CINV和PONV的III期试验有待进一步结果。在发表之时，预计将于2008年向美国食品药品监督管理局（FDA）提交CINV和PONV的监管批准申请。卡索匹坦此前曾用于治疗膀胱过度活动症；然而，在2007年9月，该适应症不再列于公司的产品研发计划中。