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公开(公告)号：US20240216526A1
公开(公告)日：2024-07-04
申请号：US18551702
申请日：2022-03-15
发明人： Jinkun HUANG , Jiahao GENG , Chaoyang FENG , Junqiang LIU , Yue LU , Lei LI , Chenglong WU , Fang CHEN , Dejian XIE
CPC分类号： A61K47/6889 , A61K47/68031 , A61K47/68033 , A61K47/68037 , A61K47/6849 , A61P35/00 , C07K16/32
摘要： Provided are a dual-drug link assembly unit represented by formula III, or a stereoisomer thereof, or an optical isomer thereof. The dual-drug link assembly unit can be linked to a targeting linker to obtain a dual-drug targeting linker-drug conjugate represented by formula I. The specific structure can effectively reduce the aggregation of the dual-drug targeting linker-drug conjugate, which facilitates process scale-up, thereby improving the efficiency of the targeting effect on tumor cells, reducing the toxic and side effects on normal cells, and at the same time, effectively overcoming drug resistance and achieving a synergistic anti-tumor effect. Compared with DS-8201 which is already on the market, the ADC provided by the present invention significantly improves the inhibition effect on HER2 positive cell strains N87 and SK—BR-3d.
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公开(公告)号：US20240293570A1
公开(公告)日：2024-09-05
申请号：US18631647
申请日：2024-04-10
发明人： Jinkun HUANG , Chenglong WU , Chaoyang FENG
CPC分类号： A61K47/6889 , A61K47/68031 , A61K47/68033 , A61K47/68037 , A61K47/6849 , A61K47/6851 , A61P35/00
摘要： A drug link assembly unit has a specific linker structure. Connecting the drug link assembly unit to an antibody forms a targeted linker-drug conjugate. The targeted linker-drug conjugate having the specific linker structure is low in polymer content and naked antibody percentage and proper in DAR value, exhibits excellent plasma stability, storage stability and anti-tumor effect, and has a wide application prospect in preparation of drugs for preventing and/or treating tumors.
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