Enzymatic Conjugation of Antibodies

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This invention relates to an enzymatic method for site-specific conjugation of human or humanized antibodies to desired molecules (such as drugs, imaging agents, or other functional groups). The method employs transglutaminase (TGase) enzymes to attach a specially designed linker to a specific glutamine residue in the antibody's constant region (not near the antigen-binding sites). This results in homogeneous and well-defined antibody conjugates, which can be loaded with a predetermined number of payloads (such as cytotoxic drugs or diagnostics), improving both the manufacturing consistency and function of antibody-based therapeutics and diagnostics.

Use CasesContent extracted from patent full text and abstract with AI.

• Creating antibody-drug conjugates for targeted cancer therapies (e.g., attaching cytotoxic drugs only to specific antibody sites).
• Developing antibody-based diagnostic agents by precisely linking imaging molecules (e.g., radioisotopes or fluorescent markers) to antibodies for better disease detection.
• Improving the pharmacokinetics and stability of therapeutic antibodies by attaching polymers like PEG in a controlled manner.
• Developing ex vivo diagnostic assays where antibodies are specifically and reproducibly labeled with detection tags.
• Facilitating research by generating homogeneous antibody conjugates for biological studies.

BenefitsContent extracted from patent full text and abstract with AI.

• Site-specific, controlled conjugation leads to homogeneous antibody conjugates with narrow drug-to-antibody ratio (DAR) distributions, improving safety and efficacy.
• Minimized risk of affecting antibody binding/activity by avoiding modification in the variable (antigen-binding) regions.
• Eliminates the need for random or harsher chemical conjugation methods, resulting in more consistent products.
• Enables attachment of a wide variety of payloads—including drugs, labels, polymers—using bio-orthogonal chemistries.
• Improves scalability and reproducibility in manufacturing antibody conjugates for clinical use.
• Potentially reduces off-target effects and toxicity in antibody-drug conjugate therapeutics, owing to precise payload placement.
• Facilitates regulatory approval by providing well-characterized, consistent bioconjugate products.

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Inventors & Applicants

Patent Abstract

The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.