Antibody-drug conjugates for delivering cytotoxic drugs

JP2026517709APending Publication Date: 2026-06-02BIOHAVEN THERAPEUTICS LTD
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
BIOHAVEN THERAPEUTICS LTD
Filing Date
2024-04-23
Publication Date
2026-06-02

AI Technical Summary

Technical Problem

Existing antibody-drug conjugate technologies for delivering cytotoxic drugs to cancer cells suffer from inefficiencies in conjugation, resulting in heterogeneous drug-antibody ratios, drug leakage, and the need for extensive antibody modification, leading to aggregation and toxicity issues.

Method used

Development of site-specific antibody-drug conjugates using brentuximab or its biosimilars, with targeted conjugation to specific lysine residues (K246 or K248) in the IgG heavy chain, utilizing monomethyl auristatin D, E, or F as cytotoxic agents, to create homogeneous and stable conjugates.

Benefits of technology

The solution provides predictable drug-antibody ratios, reduces drug leakage, and minimizes antibody modification, enhancing therapeutic efficacy and safety by ensuring consistent delivery to cancer cells.

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Abstract

Formula (RI): LG-RG-L RM A compound having the structure -MOI, or a salt thereof, is provided, wherein LG is a group comprising a target-binding moiety that binds to brentuximab or its biosimilar analog, and L RM The linking group comprises formula (I), and the MOI is a target moiety containing monomethyl auristatin D (MMAD), monomethyl auristatin E (MMAE), or monomethyl auristatin F (MMAF). Also provided are a conjugate of a compound having the structure of formula (RI) with brentuximab or its biosimilar analog, and a method for using the same to treat various cancer conditions. JPEG2026517709000146.jpg3960
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