【全球】首个AI新药进临床，治疗强迫症
2020年1月30日，大日本住友制药与Exscientia Ltd.联合宣布，双方共同开发的新药DSP-1181已在日本启动1期临床，用于治疗强迫症（obsessive-compulsive disorder, OCD）。据悉，这是全球范围内，首个由AI（artificial Intelligence）设计的新药，进入临床。
住友制药，在中枢神经系统疾病领域（CNS）颇有建树，目前治疗精神分裂的Latuda(lurasidone，鲁拉西酮)为其核心品种之一。鲁拉西酮对多巴胺D2、5-羟色胺（5-HT2A）、5-羟色胺（5-HT7）受体均具有亲和力，在这些受体中具有拮抗作用；对5-羟色胺（5-HT1A）受体具有部分激动作用。住友制药是Exscientia的早期合作伙伴之一，双方最早于2014年9月达成开发CNS药物协议。
本次合作，住友制药提供在单胺类G蛋白偶联受体(G protein-coupled receptor)药物发现方面的知识和经验，Exscientia应用Centaur Chemist™AI平台进行药物发现。Exscientia表示，人工智能大大加快了新药候选药物开发的过程。DSP-1181为一款长效的5-羟色胺（5-HT1A）受体激动剂。
据药融圈数据不完全统计，国内从事本领域相关开发的企业有：晶泰科技、深度智耀、未知君、湃隆生物、元气知药、望石智慧、METiS、英飞智药、亿药科技、宇道生物、智药科技、费米子、赛恪科技、南京双运生物、冰洲石、燧坤智能等等。
Sumitomo Dainippon Pharma and Exscientia Joint Development New Drug Candidate Created Using Artificial Intelligence (AI) Begins Clinical Trial
Sumitomo Dainippon Pharma Co., Ltd. (Head office: Osaka, Japan, Representative Director, President and CEO: Hiroshi Nomura) and Exscientia Ltd. (Headquarters: Oxford, UK; CEO: Andrew Hopkins) announce that a phase I clinical study of DSP-1181, that was created using Artificial Intelligence (AI), has been initiated in Japan for the treatment of obsessive-compulsive disorder as an initial indication.
DSP-1181 was created through the joint research by Sumitomo Dainippon Pharma and Exscientia, with Sumitomo Dainippon Pharma providing its experience and knowledge in monoamine GPCR drug discovery and Exscientia applying its Centaur Chemist™ Artificial Intelligence (AI) platform for drug discovery. This project was delivered by the strong synergy of the joint research, requiring less than 12 months to complete the exploratory research phase, just a fraction of the typical average of 4.5 years using conventional research techniques.ref)
DSP-1181 is being progressed as a long-acting and potent serotonin 5-HT1A receptor agonist, and its phase I clinical study to treat obsessive-compulsive disorder as an indication candidate. Through this, Sumitomo Dainippon Pharma has expanded its development pipeline to treat key unmet medical needs in the Psychiatry and Neurology area, one of the company’s three focus research areas.
Toru Kimura, Board of Directors, Senior Executive Officer and Senior Executive Research Director of Sumitomo Dainippon Pharma, said: "We are very excited with the results of the joint research that resulted in the development of candidate compounds in a very short time. Exscientia's sophisticated AI drug discovery technologies combined with our company’s deep experience in monoamine GPCR drug discovery, allowed us to work synergistically, delivering a highly successful outcome. We will continue to work hard to make this clinical study a success so that it may deliver new benefits to patients as soon as possible."
Andrew Hopkins, CEO of Exscientia, said: "We believe that this entry of DSP-1181, created using AI, into clinical studies is a key milestone in drug discovery. This project’s rapid success was through strong alignment of the integrated knowledge and experiences in chemistry and pharmacology on monoamine GPCR drug discovery at Sumitomo Dainippon Pharma with our AI technologies. We are proud that our AI drug discovery platform Centaur Chemist™ has contributed to generate DSP-1181 and look forward to its progression as a treatment for obsessive-compulsive disorder."
Terms:
Monoamine GPCR drug discovery
Drug discovery targeting G protein-coupled receptor (GPCR), endogenous ligands of which are monoamine neurotransmitters such as serotonin, dopamine and norepinephrine
Obsessive-compulsive disorder
OCD is a psychiatric disorder characterized by the presence of obsessions (repetitive and persistence thoughts, images, or urges) and/or compulsions (repetitive behaviors or mental acts). OCD is associated with reduced quality of life as well as high levels of social and occupational impairment as a result of time-consuming (e.g., take more than 1 hour per day) by obsessions or compulsions. The mechanism of OCD has not been clarified, however dysfunction in the orbitofrontal cortex, anterior cingulate cortex, and striatum have been most strongly implicated. The number of patients in Japan and the United States is estimated to be over 1 million and around 3 million, respectively.
参考：
NMPA/CDE；
药融圈数据；
FDA/EMA；
相关公司公开披露；
https://www.exscientia.ai/news-insights/sumitomo-dainippon-pharma-and-exscientia-joint-development;
http://www.ds-pharma.com；
https://www.itmedia.co.jp/news/articles/2002/02/news023.html；
https://www.bbc.com/news/amp/technology-51315462；
https://www.ds-pharma.com/rd/clinical/pipeline.html；等等。
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