Antibody-drug conjugate (ADC) having linker comprising vlk peptide, and pharmaceutical composition comprising said ADC
By eliminating the uncharged hydrophilic polymer block and incorporating a plasmin cleavage site in the linker, the ADCs enhance cellular uptake and drug release, addressing the limitations of existing ADCs and achieving improved antitumor effects in various cancers, including pancreatic and brain tumors.
Patent Information
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- RIN INST INC
- Filing Date
- 2025-11-26
- Publication Date
- 2026-06-04
AI Technical Summary
Existing antibody-drug conjugates (ADCs) containing a VLK peptide linked by polyethylene glycol (PEG) do not effectively exert antitumor effects in tumor tissue due to inactivation by plasmin inhibitors and the EPR effect, despite being delivered to tumors, and those targeting insoluble fibrin do not achieve optimal internalization and drug release within cells.
ADCs are designed without an uncharged hydrophilic polymer block between the antibody and VLK peptide, incorporating a linker with a plasmin cleavage site and a second spacer to enhance cellular uptake and drug release, targeting insoluble fibrin or other cancer antigens, and utilizing a cytotoxic agent linked via a cleavable linker.
The ADCs demonstrate higher internalization into cells and a more significant antitumor effect compared to controls, effectively treating various cancer types, including pancreatic and brain tumors, even in environments where plasmin is inactivated by plasmin inhibitors.
Smart Images
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