Hangzhou Dac Biotech Co., Ltd.

Xiaotao Zhuo

Robert Yongxin Zhao

Qingliang Yang

Yuanyuan Huang

Huihui Guo

Hangbo Ye

Xiaomai Zhou

Hongsheng Xie

Shun Gai

Junxiang Jia

Wenjun Li

Xing Li

Chen Lin

Sanxing Sun

Lan Qu

Jun Zheng

Jun Lei

Qianqian Tong

Linyao Zhao

Zhixiang Guo

Yifang Xu

Lu Bai

Yanlei Yang

Zhichang Ye

Xiuzheng Zhang

Xiang Cai

Mingjun Cao

Chengyu Yang

The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.

Conjugate of a tubulysin analog with branched linkers

Hydrophilic linkers are useful for linking drugs to cell-binding ligands in ligand-drug conjugates, such as antibody-drug conjugates. The ligand-drug conjugate includes a cell-binding ligand capable of binding to a particular cell population, and a drug connected to the ligand by a hydrophilic linker. The hydrophilic linker includes one or more hydrophilic groups that render the linker hydrophilic. The hydrophilic linker may also include functional groups at the two termini for coupling to the drug and the cell-binding ligand respectively.

Hydrophilic linkers and ligand-drug conjugates thereof

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Hangzhou, China

Xiaotao Zhuo