Alpha Radiolabeled Gastrin Analogue and Use Thereof in Methods of Treating Cckb Receptor Positive Disease

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

The patent describes an alpha radiolabeled gastrin analogue, especially a peptide labeled with an alpha-emitting radionuclide such as actinium-225. This compound specifically targets cholecystokinin B receptors (CCKBR), commonly overexpressed in certain cancers. When administered, the analogue delivers targeted alpha radiation to CCKBR-positive cancer cells, efficiently destroying them while minimizing damage to healthy tissues, making it suitable for peptide receptor radionuclide therapy (PRRT) applications against CCKBR-positive tumors.

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

• Targeted treatment of CCKBR-positive cancers, such as medullary thyroid cancer (MTC), small-cell lung cancer (SCLC), and extrapulmonary small-cell carcinoma (EPSCC).
• Therapy for other CCKBR-positive tumors, including gastric, colon, ovarian, breast, pancreatic adenocarcinoma, gliomas, and gastroenteropancreatic neuroendocrine tumors.
• Potential treatment of metastatic and advanced-stage CCKBR-expressing cancers.
• Possible use in combination with other cancer therapies, such as chemotherapy or immunotherapy, for enhanced efficacy.
• Diagnostic applications when labeled with gamma-emitting isotopes, enabling theranostic (therapy and diagnostics) approaches.

BenefitsContent extracted from patent full text and abstract with AI.

• Highly specific targeting of CCKBR-expressing cancer cells, reducing off-target toxicity.
• Improved therapeutic efficacy due to the potent, localized DNA damage from alpha particles.
• Reduced toxicity to healthy tissues, including organs like the stomach and kidneys, compared to previous radiolabeled peptide therapies.
• Effective against tumors not responsive to traditional treatments, such as MTC that does not respond to radioactive iodine.
• Potential for longer patient survival and inhibition of tumor growth, as demonstrated in animal models.
• Supports personalized medicine by targeting patients whose tumors express CCKBR.
• Facilitates safer administration of higher therapeutic doses due to limited radiation damage to non-target tissues.

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Patent Abstract

The present invention relates to an alpha radiolabeled gastrin analogue and its use in peptide receptor radionuclide therapy (PRRT) applications. In particular, the present invention relates to an alpha radiolabeled gastrin analogue, which exhibits excellent biodistribution and therapeutic efficacy while toxicity for healthy tissues is prevented and/or reduced. The present invention also relates to the use of an alpha radiolabeled gastrin analogue in methods of treating CCKB receptor positive diseases.