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AssigneeHangzhou Institute of Medicine Chinese Academy of Science
InventorsWeihong TAN, Jiaxuan HE, Xiangsheng LIU, Minhui SU, Yanlan LIU, Sitao XIE, Ting FU
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The invention provides a high drug-loading ratio aptamer-drug conjugates (ApDC) and its applications. By using a linker with a dendritic structure and combining solid-phase synthesis with efficient click chemistry reactions, the invention enables the design and efficient synthesis of high drug-loading ratio ApDC. These drugs demonstrate excellent tumor-inhibiting activity in antitumor applications. Moreover, different drug-loading ratios can be designed to achieve higher efficacy for different drugs, resulting in ApDC with enhanced therapeutic effects. The invention exhibits outstanding antitumor effects against malignant tumors such as lung cancer, colorectal cancer, breast cancer, and ovarian cancer, with an inhibition efficiency exceeding 90%.
A high drug-loading aptamer-drug conjugates comprising:
A method for enhancing the antitumor effect in individuals with colorectal cancer, comprising:
A method for enhancing the efficacy of the DNA topoisomerase I inhibitor Dxd to exceed the in vivo antitumor effect of exatecan, characterized in that an aptamer-drug conjugate is injected into the individual, wherein the aptamer-drug conjugates is SAD, with the structural formula being:
Dependencies are inferred from the claim text.