近日，迪哲医药公示启动DZD8586美国健康人I期临床试验（NCT05176873），该研究实际启动于2021年12月9日，计划招募64位健康受试者用于安全性、耐受性和PK特征的评价研究。
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2021.11.08 迪哲医药提交国内临床试验申请，待默示许可；
2022.01.05 迪哲医药公告在国内临床试验申请获得批准，即将启动用于复发难治性B细胞非霍奇金淋巴瘤(NHL)治疗的临床研究。
DZD8586是一个口服高选择性，具有血脑屏障穿透性的小分子靶向抑制剂，旨在开发用于治疗中枢神经系统淋巴瘤在内的血液肿瘤疾病。
2020年迪哲医药曾申请过一个BTK抑制剂的专利（WO2021136219），其中实施例1-15主要参照了OSI Pharma（acquired by Astellas Pharma Inc. in 2010）ACK1抑制剂专利报道结构，其他实施例则在此基础上有所改动，具体结构举例如下：
而在PCNSL领域，目前仅有ONO的Tirabrutinib 在日本获批该适应症，附Tirabrutinib文献一篇：
Tirabrutinib (Velexbru®) is an orally administered, small molecule, Bruton's tyrosine kinase (BTK) inhibitor being developed by Ono Pharmaceutical and its licensee Gilead Sciences for the treatment of autoimmune disorders and haematological malignancies. Tirabrutinib irreversibly and covalently binds to BTK in B cells and inhibits aberrant B cell receptor signalling in B cell-related cancers and autoimmune diseases. In March 2020, oral tirabrutinib was approved in Japan for the treatment of recurrent or refractory primary central nervous system lymphoma. Tirabrutinib is also under regulatory review in Japan for the treatment of Waldenström's macroglobulinemia and lymphoplasmacytic lymphoma. Clinical development is underway in the USA, Europe and Japan for autoimmune disorders, chronic lymphocytic leukaemia, B cell lymphoma, Sjogren's syndrome, pemphigus and rheumatoid arthritis. This article summarizes the milestones in the development of tirabrutinib leading to the first approval of tirabrutinib for the treatment of recurrent or refractory primary central nervous system lymphoma in Japan.
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