Compound and Method for Selective Radiomarking of Polypeptides by Solid Phase Synthesis

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

This invention provides a novel method and compound for the selective radiolabeling of polypeptides using solid-phase synthesis. The technology enables polypeptides (3-200 amino acids) to be decorated with a special binding group (for various medically important radioisotopes such as 99mTc, 186Re, 188Re, 90Y, 177Lu, etc.), allowing for efficient and automated production of radiolabeled peptides. These compounds are useful in radiopharmaceuticals for imaging (e.g., SPECT, scintigraphy) and therapy.

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

• Preparation of radiolabeled peptides for nuclear medical imaging (e.g., SPECT, PET) to diagnose cancers, cardiovascular diseases, neurological disorders, and other pathologies.
• Production of radiotherapeutic agents for targeted cancer therapy, leveraging the delivery of radioactive isotopes to specific tissues or tumors.
• Development of diagnostic kits for hospitals or imaging centers to produce radiopharmaceuticals quickly and reliably on-site.
• Research and preclinical studies involving the tracing, biodistribution, or targeting of specific peptides or proteins in animals or cell models.
• Aiding drug development through the ability to radiolabel and track biomolecules of interest.

BenefitsContent extracted from patent full text and abstract with AI.

• Enables a simple, reproducible, and efficient method for radiolabeling a broad range of peptides independent of their sequence.
• Reduces the complexity and risk of side reactions compared to conventional solution-phase radiolabeling methods.
• Allows for easy automation and standardization of radiolabeling workflows (solid-phase synthesis compatible with automated peptide synthesizers).
• Permits high radiochemical yields with minimal amounts of radioactive metals, improving safety and cost-effectiveness.
• Results in high-purity radiolabeled products suitable for clinical or preclinical use.
• Can be broadly applied to create radiopharmaceuticals for both imaging and therapy, increasing flexibility in nuclear medicine applications.

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

The invention relates to a compound of the formula (I) T-Pep-BG (I) where, in formula (I), T is a solid support; Pep is a polypeptide bonded covalently to T, where the polypeptide has an amino acid sequence having 3 to 200 amino acids and BG is an uncomplexed binding group for a metal M selected from the group consisting of 99mTc,186Re,188Re, 90Y, 86Y, 177Lu, 68Ga, 67Cu, 64Cu, 67Ga,89Zr,153Sm and 111 In. The invention further relates to a method for preparing the compound of the formula (I) and to uses and kits of the compounds of the formula (I) for production of radiodiagnostic and radiotherapeutic products.