Linker Technology for Reduced Renal Retention

Simple SummaryContent extracted from patent full text and abstract with AI.

This invention discloses a new class of cleavable chemical linkers designed for attaching therapeutic or diagnostic payloads (such as drugs or imaging agents) to proteins, especially small protein or peptide-based pharmaceuticals. These linkers are engineered to be enzymatically cleaved by specific renal (kidney) enzymes, promoting faster elimination of the payload and thus reducing kidney retention. This is particularly important for radiolabeled drugs (used in cancer diagnostics or therapy), which often accumulate in the kidneys and may cause toxicity. The new linkers offer improved safety and efficacy by lowering kidney exposure while maintaining disease-targeting activity.

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

• Targeted delivery of radiopharmaceuticals for cancer therapy with reduced kidney toxicity.
• Improved molecular imaging agents for cancer, fibrosis, or autoimmune diseases, minimizing renal background signal.
• Development of safer antibody-drug conjugates or peptide therapies that require fast renal clearance.
• Theranostic (combined therapy and diagnostic) agents in oncology that require efficient tumor targeting and minimal renal retention.
• Use in diagnostic imaging of pathological extracellular matrix proteins, such as fibronectin, in oncology and fibrotic diseases.

BenefitsContent extracted from patent full text and abstract with AI.

• Significantly reduces renal retention of therapeutic or diagnostic agents, lowering the risk of kidney toxicity.
• Maintains or enhances target tissue (e.g., tumor) accumulation for effective imaging or therapy.
• Versatile linker design compatible with a variety of payloads (including radionuclides, drugs, fluorescent dyes) and protein carriers (antibodies, peptides, nanobodies).
• Cleavable by natural renal enzymes, ensuring efficient and specific removal in the kidneys.
• Potential to enable higher or repeated dosing of targeted therapies, expanding treatment options.
• Improves safety profile for radiopharmaceuticals and protein-based therapies, potentially shortening regulatory pathways.

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

The present invention relates to a linker of the present invention, a protein-payload conjugate of the present invention, payload-linker conjugate of the present invention and their respective therapeutic and diagnostic uses. The linkers, protein-payload conjugates and payload-linker conjugates of the present invention as particularly useful due to their reduced renal retention.