Institute of Psychiatry and Psychology, Department of Geriatrics, Neuroscience and Orthopedics, Fondazione Policlinico Universitario A. Gemelli IRCCS, Università Cattolica del Sacro Cuore, Rome, Italy.
Department of Science, University of Rome "Roma Tre", Rome, Italy.
CNS Neurol Disord Drug Targets. 2020;19(4):243-247. doi: 10.2174/1871527319666200601145653.
Lumateperone (ITI-007) is a tosylate salt with binding affinities to receptors implicated in the therapeutic actions of antipsychotic medications, including the serotonin 5HT2A receptors, dopamine D2 and D1 receptors and the serotonin transporter. It has a unique mechanism of action because it simultaneously modulates serotonin, dopamine, and glutamate neurotransmission, implicated in serious mental illness. It can be considered a multi-target-directed ligand and a multifunctional modulator of serotoninergic system with possible precognitive, antipsychotic, antidepressant and anxiolytic properties. Lumateperone has been investigated as a novel agent for the treatment of schizophrenia, but it represents a new potential option for other psychiatric and neurological diseases, such as behavioural symptoms of dementia or Alzheimer's disease, sleep disturbances, bipolar depression. Besides, it has demonstrated a favourable safety profile without significant extrapyramidal side effects, hyperprolactinemia or changes in cardiometabolic or endocrine factors versus placebo. Additional studies are warranted to confirm and examine the benefit of lumateperone and possible therapeutic targets. This paper is a comprehensive and thorough summary of the most important findings and potential future role of this particular compound in personalized treatments.
鲁马替培酮（ITI-007）是一种甲苯磺酸盐，与抗精神病药物治疗作用相关的受体具有亲和力，包括 5HT2A 受体、多巴胺 D2 和 D1 受体以及血清素转运体。它具有独特的作用机制，因为它同时调节血清素、多巴胺和谷氨酸神经递质，这与严重的精神疾病有关。它可以被认为是一种多靶点配体和血清素能系统的多功能调节剂，具有潜在的预知、抗精神病、抗抑郁和抗焦虑作用。鲁马替培酮已被研究作为一种新型治疗精神分裂症的药物，但它也可能是其他精神和神经疾病的新选择，如痴呆或阿尔茨海默病的行为症状、睡眠障碍、双相抑郁。此外，与安慰剂相比，它具有良好的安全性，没有明显的锥体外系副作用、高催乳素血症或心血管代谢或内分泌因素的变化。需要进一步的研究来证实和检查鲁马替培酮的益处和可能的治疗靶点。本文全面而深入地总结了这种特殊化合物在个体化治疗中的最重要发现和潜在的未来作用。
