Site-specific multi-payload antibody-drug conjugates and preparation thereof

Glycoengineered antibodies using deglycosylation and transglycosylation reactions enable the creation of multi-payload ADCs with improved stability and efficacy, addressing the limitations of random coupling in existing ADCs by precisely attaching multiple active agents to the antibody Fc domain.

WO2026148079A1PCT designated stage Publication Date: 2026-07-09OBI PHARMA INC +1
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Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
OBI PHARMA INC
Filing Date
2025-12-31
Publication Date
2026-07-09

AI Technical Summary

Technical Problem

Current antibody-drug conjugates (ADCs) suffer from poor in vivo stability and therapeutic efficacy due to random drug coupling, necessitating the development of site-specific coupling technologies for improved stability and efficacy.

Method used

The use of glycoengineered antibodies prepared through deglycosylation and transglycosylation reactions with glycosynthases to create multi-payload antibody conjugates, incorporating bioorthogonal linkers and payloads such as chemotherapeutic agents, cytotoxic agents, and other active compounds, allowing for precise attachment to the antibody Fc domain.

Benefits of technology

The method produces homogeneous multi-payload ADCs with enhanced stability and therapeutic efficacy, effectively targeting various diseases including cancers by delivering multiple active agents to specific antigens.

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Abstract

The present disclosure relates to multi-payload antibody conjugates and preparation methods thereof. The preparation methods utilize an enzymatic site-specific conjugation technology and mutually orthogonal reactions such that highly homogeneous multi-payload antibody conjugates could be produced. The present disclosure further provides antibody-drug conjugates (ADCs) targeting multiple antigens (e.g., TROP2, HER2, Nectin-4, etc.) and pharmaceutical compositions comprising said ADCs. Also described herein are methods of using the ADCs for treatment of diseases such as cancers.
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