Conjugates of a cell-binding molecule with camptothecin analogs

Water-soluble camptothecin analogs conjugated with cell-binding molecules address insolubility and aggregation issues, enhancing therapeutic efficacy and safety in targeted therapies.

AU2020444233B2Pending Publication Date: 2026-07-09HANGZHOU DAC BIOTECH CO LTD
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Patent Information

Application Number
AU2020444233
Authority / Receiving Office
AU · AU
Patent Type
Applications
Current Assignee / Owner
Filing Date
2020-06-19
Publication Date
2026-07-09
Estimated Expiration
2040-06-19

AI Technical Summary

Technical Problem

Existing camptothecin analogs used in antibody-drug conjugates (ADCs) face issues with insolubility and aggregation, leading to systemic side-effects and limited clinical success, despite their potential as potent cytotoxic agents.

Method used

Development of water-soluble camptothecin analogs conjugated with cell-binding molecules through specific linkers, ensuring stability in blood circulation and targeted cell death upon release.

Benefits of technology

The conjugates achieve enhanced therapeutic efficacy with reduced side-effects by maintaining solubility and stability, allowing for effective targeted cancer, autoimmune disease, and infectious disease treatment.

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Abstract

Provided are conjugates of camptothecin analogs with a cell-binding molecule of formula (I), wherein R1, R2, R3, R4, R5, X, L, n, m, T and ----- are defined herein. It also provides methods of making the conjugates of camptothecin analogs to a cell-binding agent, as well as methods of using the conjugates in targeted treatment of cancer, infection, and immunological disorders.
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Citation Information

Patent Citations

  • Camptothecin-cell penetrating peptide conjugates and pharmaceutical compositions containing the same

    WO2007113687A2

  • Peptide-containing linkers for antibody-drug conjugates

    WO2018098269A2