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目前显示的是标签为“Cullgen”的博文

Cullgen向中国药监局提交CG001419临床试验申请

 近日, Cullgen 终于向国家药监局提交了其TRK降解剂 CG001419 的临床试验申请,在去年初 完成B轮融资 时,既已对外宣布将在去年底提交IND用于在 肿瘤和其他疾病 中进行临床研究。 ________________________ 2022.8 CG001419获得国家药品监督管理局药品审评中心默示许可,用于开展治疗NTRK阳性实体瘤的临床研究。 IND application of CG001419, a TRK protein degrader for cancer and other disease applications from Cullgen, was accepted by China NMPA. #PROTAC #TPD pic.twitter.com/3TQeVa09J0 — Pharmews (@Pharmews) May 26, 2022 此前2020年,Cullgen即在JMC上发表了《 Discovery of First-In-Class Potent and Selective Tropomyosin Receptor Kinase Degraders 》,以CRBN配体连接GNF-8625的PROTAC结构,但截至目前尚未公开报道CG001419结构,是否使用了上述结构尚未可知。 2021年8月,睿跃生物董事长罗楹博士在同写意论坛上做的《从TRK靶向蛋白降解剂开发看PROTAC》中介绍了部分信息,如下: 选择性 与CG1739降解活性对比 安全性数据对比 部分动物模型 疼痛模型

Cullgen公开TYK2降解剂专利《Tyrosine kinase 2 (TYK2) degradation compounds and methods of use》

 近日,Cullgen公开专利一项TYK2-PROTAC降解剂的专利《 Tyrosine kinase 2 (TYK2) degradation compounds and methods of use 》,该专利申请于2020年11月,TYK2靶蛋白配体连接VHL和CRBN配体。该靶点已由BMS验证在PsO适应症的疗效,并于2021年11月向FDA提交上市申请,除此适应症外,BMS的Deucravacitinib还在PsA(Ph3)、SLE(Ph2) 以及UC(Ph2 failed)等领域拓展。 以下是部分实施例结构以及在MOLT-4, NOMO-1 or Jurkat cells降解活性,那么Cullgen会在什么适应症尝试呢? Cullgen实施例内容 ” The preferred benefit to risk ratio of targeting TYK2 has increasingly attracted the interests of academia and pharmaceutical industry. Neutralizing antibodies against IL-12 and IL-23, the main cytokines that signal through TYK2, have been approved for treating psoriasis, psoriatic arthritis and Crohn’s disease. Over the past decade, a variety of TYK2 kinase inhibitors with varying degree of selectivity over other JAK family members have been reported and patented. Some of these TYK2 inhibitors have proceeded into different clinical stages. While TYK2 and other JAK kinase inhibitors hold promises treating a wide range of immunologic and malignant condi...