Bone targeting therapeutics

Bone targeting therapeutic conjugates, which combine therapeutic antibodies with bone targeting moieties, address the limitations of current therapies by enhancing bone surface targeting and retention, thereby improving therapeutic efficacy for bone diseases.

WO2025081137A1PCT designated stage expired Publication Date: 2025-04-17THE RGT UNIV OF MICHIGAN
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Patent Information

Application Number
PCT/US2024/051183
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2023-10-12
Filing Date
2024-10-14
Publication Date
2025-04-17

AI Technical Summary

Technical Problem

Current bone-targeted biotherapeutics have limited efficacy and retention on the bone surface, with only one approved therapy for human use, and there is a lack of understanding about the key features necessary for optimal protein delivery.

Method used

Development of bone targeting therapeutic conjugates comprising a therapeutic antibody for treating bone diseases, such as anti-sclerostin, anti-RANKL, or anti-TGFβ antibodies, conjugated with bone targeting moieties like bisphosphonates or acidic oligopeptides, which are site-specifically attached to the antibody using sortase/sortag labeling and click chemistry.

Benefits of technology

The bone targeting therapeutic conjugates demonstrate enhanced pharmacokinetic properties, including increased circulation time and avidity, leading to improved bone surface targeting and retention, which results in increased therapeutic efficacy for bone diseases like osteoporosis, potentially allowing for lower doses and less frequent dosing.

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Abstract

The present disclosure relates to bone targeting therapeutic conjugates and uses thereof. In particular, the disclosure relates to bone targeting therapeutic conjugates comprising a therapeutic antibody for treatment of a bone disease and a bone targeting moiety.
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Citation Information

Patent Citations

  • Anti-sclerostin antibodies

    US20110250205A1

  • Bone-specific delivery of polypeptides

    WO2022159492A1

Cited By

  • Food-borne bone health peptide and application thereof in preparation of products for improving bone mineral density

    CN122483145A