精神分裂症是一种慢性高致残性精神障碍，其病因和病理机制复杂。既往抗精神病药主要通过作用于多巴胺2型受体发挥疗效，对阴性症状和认知损害症状的疗效欠佳且出现较多的不良反应，严重影响患者的治疗依从性和功能康复。因此，作用于新靶点的抗精神病药的研发显得尤为迫切。SEP-363856是基于表型筛选策略发现的一种不与多巴胺2型受体结合的独特抗精神病药，临床前研究数据表明，SEP-363856的疗效可能与激活痕量胺相关受体1和5-羟色胺1A受体有关，该药的发现有望为精神分裂症患者带来新的治疗选择。本文中简要介绍了SEP-363856的研发历程，包括临床前研究结果及最新的临床试验数据，便于读者了解这一新型抗精神病药。“,”Schizophrenia is a common chronic disabling mental disorder with complex etiology and pathological mechanism. Over the past 70 years, antipsychotics have primarily acted on Dn 2 receptors, with poor response to negative symptoms and cognitive impairment and more adverse effects, which have significantly affected patient compliance and functional recovery. Therefore, the development of new-targeted antipsychotic drugs is particularly urgent. SEP-363856 is a non-Dn 2-receptor-binding drug for the treatment of schizophrenia which is found by phenotypic screening strategies, and the pharmacological mechanism has not been fully elucidated. Preclinical data suggest that SEP-363856 may active Trace amine associated receptor 1 (TAAR1) and 5-HTn 1A receptors, and the discovery of this drug shed light on new treatment options for schizophrenic. This review provides an introduction of the development of SEP-363856, including preclinical findings and the latest clinical trial data, to help readers understand this new antipsychotic drug.n