Dual-payload antibody-drug conjugates and use thereof

A dual-load bifunctional CDN conjugate addresses the limitations of CDN-type STING agonists and ADCs by combining immune-activating and cytotoxic molecules, achieving effective and safe tumor suppression through diverse administration routes.

TW202626741APending Publication Date: 2026-07-01TYLIGAND BIOSCIENCE (SHANGHAI) LIMITED
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Patent Information

Application Number
TW114133944
Authority / Receiving Office
TW · TW
Patent Type
Applications
Current Assignee / Owner
Priority Date
2025-08-29
Filing Date
2025-09-04
Publication Date
2026-07-01

AI Technical Summary

Technical Problem

Current CDN-type STING agonists face challenges such as easy degradation by enzymes, short half-life, limited bioavailability, and reliance on intratumoral administration, which restricts their use as systemic immunotherapy, and ADCs face issues like uncontrolled payload release, off-target toxicity, and complex pharmacokinetics.

Method used

Development of a dual-load bifunctional cyclic dinucleotide conjugate drug that combines a CDN STING agonist with a second payload, targeted by specific guide molecules through linker units, forming a single ADC molecule that can be administered via intravenous, subcutaneous, or topical routes.

Benefits of technology

The dual-load conjugate achieves synergistic tumor suppression, improved efficacy, and safety, with enhanced tumor cell endocytosis, and provides immune-activating and cytotoxic mechanisms, expanding administration methods and beneficiary populations.

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Abstract

The present disclosure relates to dual-payload antibody-drug conjugates (ADC), compositions containing the same and therapeutic uses of the same.
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