[161Tb]-BASED RADIOPEPTIDES

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

This patent describes radiopeptides that use the radioisotope terbium-161 (161Tb), stably bound to a chelator and attached to a peptide that acts as a somatostatin receptor (SSTR) antagonist. These compounds are specifically designed to target tumors, especially neuroendocrine tumors that overexpress somatostatin receptors, by delivering radiation directly to tumor cells. The invention demonstrates improved therapeutic efficacy over currently approved lutetium-177-based therapies, particularly due to the unique emission properties of terbium-161, which include both beta and Auger electrons that can more effectively destroy cancer cells, even when the targeting peptide stays on the cell surface.

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

• Targeted radionuclide therapy for neuroendocrine tumors, such as those of the pancreas, intestine, and lung, that express somatostatin receptor 2 (SSTR2).
• Treatment of metastatic neuroendocrine tumors, including lymph node and liver metastases.
• Therapeutic intervention for tumors resistant or refractory to established therapies using lutetium-177-labeled somatostatin analogues (e.g., Lutathera).
• Potential use in treating other SSTR2-positive cancers (e.g., medullary thyroid cancer, pheochromocytoma, prostate cancer, meningioma, non-Hodgkin lymphoma).
• Companion diagnostic for imaging (SPECT) and selection of patients based on SSTR expression, prior to therapy.

BenefitsContent extracted from patent full text and abstract with AI.

• Superior tumor cell killing efficacy compared to lutetium-177-labeled analogues due to the combined beta and Auger electron emission of terbium-161.
• Selective targeting minimizes radiation exposure of healthy tissues, reducing side effects.
• Higher tumor uptake and prolonged retention in tumor tissue, especially with antagonist peptides that remain on the cell surface.
• Compatibility with established chelators (like DOTA), ensuring stability and ease of preparation in clinical settings.
• Retention of imaging capability for treatment monitoring and dosimetry (gamma emissions of terbium-161 enable SPECT).
• Offers a therapy avenue for patients unresponsive to current standard-of-care radioligand therapies.

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Inventors & Applicants

Patent Abstract

A radiopeptide is provided which comprises (a) a radionuclide, wherein the radionuclide is terbium-161, (b) a chelator coordinating terbium-161, and (c) a peptide or peptide analogue, which is a somatostatin receptor (SSTR) antagonist. The radiopeptide is suitable for use in the treatment of tumor diseases.