Protein-based carriers for site-specific amine conjugation

IL330213A0Pending Publication Date: 2026-08-01ABLYNX NV
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Patent Information

Application Number
IL330213
Authority / Receiving Office
IL · IL
Patent Type
Applications
Current Assignee / Owner
Priority Date
2023-12-22
Filing Date
2024-12-20
Publication Date
2026-08-01

AI Technical Summary

Technical Problem

Current site-specific conjugation technologies for antibody-drug conjugates (ADCs) are complex and inefficient, leading to heterogeneous products with variable drug loading, which affects the efficacy, safety, and pharmacokinetics of ADCs.

Method used

The development of protein-based carriers comprising immunoglobulin single variable domains (ISVDs) with specific conjugation sites, such as primary amines on lysines or the N-terminus, allowing for site-specific and efficient conjugation of cargos.

Benefits of technology

This approach enables precise control over drug loading, maintaining the binding affinity and specificity of the antibody while optimizing the pharmacokinetics and therapeutic efficacy of the conjugated drugs.

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Abstract

The present technology relates to the field of drug delivery and provides molecules comprising or consisting of at least one ISVD suitable for site-specific conjugation, wherein the ISVD comprises at least one, preferably at least two, attachment point(s) or conjugation site(s). In particular, the technology relates to molecule comprising or consisting of at least one ISVD, wherein the at least one ISVD: - comprises at least one (engineered) lysine at least one solvent accessible position, wherein the solvent accessible position is not located at positions (43, 64, 75) and / or (83) (according to Kabat), preferably wherein the solvent accessible position is not located at positions (43, 64, 75, 83) and / or (97) (according to Kabat), even more preferably wherein the solvent accessible position is not located at positions (19, 43, 64, 75, 83, 97) and / or (105) (according to Kabat); or - comprises only two lysines in its amino acid sequence, wherein the two lysines are located at positions (43, 64, 75) and / or (83) (according to Kabat); - comprises a single lysine, wherein the single lysine is located at position (43, 64, 75) or (83) (according to Kabat); or - does not comprise any lysine in its sequence, preferably does not comprise any primary amine in its sequence.
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