Lu-AA21004,一种多模式血清素能剂,用于治疗抑郁和焦虑。

Idrugs Pub Date : 2010-12-01
Albert Adell
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引用次数: 0

摘要

Lu-AA21004是一种口服的多模式血清素能药物,目前正由灵北公司和武田制药公司开发,用于治疗抑郁症和焦虑症。Lu-AA21004属于一种新的化学类抗抑郁药,双沙基磺胺,具有新的药理特征,具有5-羟色胺能受体5-HT3, 5-HT7和5-HT1A的活性,也具有5-羟色胺转运体的活性。大鼠急性给药Lu-AA21004通过阻断5-HT3受体抑制中隔背核5-羟色胺能神经元的放电活性,与SSRI类抗抑郁药相比,停药后放电活性迅速恢复。II期临床试验结果显示,治疗6周后,抑郁和焦虑症状有所改善。总体而言,Lu-AA21004耐受性良好,与文拉法辛相比,服用Lu-AA21004的患者发生与性功能障碍相关的不良事件的数量较少。Lu-AA21004在重度抑郁症患者中的III期临床试验正在进行中,在广泛性焦虑症患者中的III期试验已经完成。如果这些临床试验的初步结果证明是积极的,那么Lu-AA21004可能为治疗抑郁症和焦虑症的新型多模式疗法铺平道路。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Lu-AA21004, a multimodal serotonergic agent, for the potential treatment of depression and anxiety.

Lu-AA21004, an oral, multimodal serotonergic agent, is currently under development by H Lundbeck and Takeda Pharmaceutical, for the potential treatment of depression and anxiety. Lu-AA21004 belongs to a novel chemical class of antidepressant agents, the bisarylsulfanyl amines, and possesses a novel pharmacological profile, with activity at serotonergic receptors 5-HT3, 5-HT7 and 5-HT1A, and also at the 5-HT transporter. Acute administration of Lu-AA21004 in rats inhibited the firing activity of serotonergic neurons of the dorsal raphe nucleus through 5-HT3 receptor blockade, with rapid recovery of firing activity upon cessation of treatment compared with an antidepressant of the SSRI class. Results from phase II clinical trials have reported improvement in depression and anxiety symptoms after 6 weeks of treatment. Lu-AA21004 was generally well tolerated, with adverse events related to sexual dysfunction occurring in a lower number of patients receiving Lu-AA21004 compared with venlafaxine. Phase III clinical trials with Lu-AA21004 in patients with major depressive disorder are underway and phase III trials in patients with generalized anxiety disorder have been completed. If initial outcomes from these clinical trials prove positive, Lu-AA21004 may pave the way for new multimodal therapies for the treatment of depression and anxiety.

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Idrugs
Idrugs 医学-药学
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