Bioactive conjugate, preparation method therefor and use thereof
Patent Information
- Authority / Receiving Office
- RS · RS
- Patent Type
- Patents
- Current Assignee / Owner
- SICHUAN KELUN BIOTECH BIOPHARMACEUTICAL CO LTD
- Filing Date
- 2018-12-10
- Publication Date
- 2026-06-30
AI Technical Summary
Existing bioactive molecule conjugates have insufficient stability and targeting in the body, resulting in side effects and limited therapeutic effects. In particular, the connection method between antibodies and bioactive molecules is prone to hydrolysis or reverse Michael reaction in the body, resulting in non-target drugs. Cell shedding, increased toxicity and insufficient efficacy.
By improving the coupling method between antibodies and biologically active molecules, using linkers and sulfhydryl groups in antibodies to form stable C-S bonds, the stability and drug loading capacity of the conjugates can be improved, and the targeting of tumor tissues can be enhanced, for example, through specific The linker undergoes a nucleophilic substitution reaction with the sulfhydryl group in the antibody to form a new conjugate BT001021, which significantly improves the exposure and therapeutic effect in tumor tissue.
It achieves the stable release of efficient bioactive molecules in tumor tissues, significantly improves the therapeutic effect, reduces the toxicity to normal cells, enhances tumor targeting, and achieves the purpose of increasing efficacy and reducing toxicity.