Lilly Bio-Medicines, Eli Lilly and Company, Indianapolis, IN, USA.
Neuropharmacology. 2013 Mar;66:82-6. doi: 10.1016/j.neuropharm.2012.06.002. Epub 2012 Jun 18.
Pomaglumetad methionil (LY2140023 monohydrate, hereafter referred to as LY2140023) is currently in clinical development as a potential new treatment for schizophrenia. If found to be effective, LY2140023 would represent a novel non-dopaminergic based therapy for this disorder that may restore balance to the glutamate dysregulation hypothesized to underlie schizophrenia. This article presents available clinical trial data that describe the safety, tolerability, and efficacy of LY2140023 in patients with schizophrenia. Data indicate that this compound appears to have an efficacy profile consistent with currently available antipsychotic drugs, although confirmation of its efficacy awaits further clinical testing. LY2140023 is generally well tolerated and appears to have a low association with adverse events related to dopamine D2 receptor antagonism and with weight gain, which are commonly seen with current antipsychotics. A potential association of LY2140023 treatment and seizure events has been identified, although an accurate and reliable understanding of the incidence of these events requires further clinical testing, which is underway. Evaluation of the safety, tolerability, and efficacy of LY2140023 is continuing. This article is part of a Special Issue entitled 'Metabotropic Glutamate Receptors'.
培美曲塞甲硫氨酸(LY2140023 一水合物,以下简称 LY2140023)目前正在进行临床试验,作为治疗精神分裂症的潜在新疗法。如果被证明有效,LY2140023 将代表一种新的非多巴胺能治疗方法,可能恢复谷氨酸失调的平衡,这种失调被认为是精神分裂症的基础。本文介绍了描述 LY2140023 在精神分裂症患者中的安全性、耐受性和疗效的可用临床试验数据。数据表明,这种化合物的疗效特征似乎与现有的抗精神病药物一致,尽管其疗效还需要进一步的临床测试来确认。LY2140023 通常具有良好的耐受性,并且与多巴胺 D2 受体拮抗作用和体重增加相关的不良反应的关联度较低,而体重增加是目前抗精神病药物常见的不良反应。已经确定 LY2140023 治疗与癫痫事件之间存在潜在的关联,尽管需要进一步的临床测试来准确可靠地了解这些事件的发生率,目前正在进行中。LY2140023 的安全性、耐受性和疗效的评估正在继续。本文是特刊“代谢型谷氨酸受体”的一部分。