Diagnosis, Treatment and Prevention of Neurotensin Receptor-Related Conditions

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This patent discloses new radionuclide-labeled compounds with strong selectivity for neurotensin receptor 1 (NTS1), aiming for targeted diagnosis, treatment, and prevention of neurotensin receptor-related conditions, especially certain tumors and hematological cancers. The invention overcomes previous limitations by reducing unwanted binding to dopamine receptors, thus improving accuracy in imaging and effectiveness in targeted cancer therapies. The described compounds can be labeled with imaging or therapeutic radionuclides and are stable, highly selective, and effective in animal tumor models.

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• Non-invasive imaging of NTS1-positive tumors (e.g., prostate, pancreas, colon, small cell lung, thyroid, rectal, pituitary, breast cancers) via PET, SPECT, or other nuclear medicine techniques.
• Targeted radiotherapy for patients with NTS1-overexpressing cancers, delivering localized radiation while sparing healthy tissue.
• Early detection and stratification of cancer based on NTS1 expression level, aiding in personalized medicine strategies.
• Staging and monitoring of neurotensin receptor-related tumors before, during, and after therapies.
• Research tool in preclinical studies to investigate neurotensin receptor function, expression, and its role in cancer progression.

BenefitsContent extracted from patent full text and abstract with AI.

• Highly selective binding to NTS1 with minimal affinity for dopamine receptors, reducing background signals and increasing imaging specificity and therapeutic efficacy.
• Allows precise imaging and targeted radiotherapy, potentially improving patient outcomes and reducing side effects compared to non-targeted approaches.
• Rapid clearance from healthy tissues and high retention in tumors provides clear images and effective tumor dose with minimal toxicity.
• Stable compounds with proven tumor growth inhibition and survival benefit in animal models, supporting their therapeutic potential.
• Flexible labeling with a range of diagnostic and therapeutic radionuclides, enabling use for both diagnosis (imaging) and treatment (therapy).

Technical Classifications (CPCs)

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Patent Abstract

The present invention describes a compound of formula (I) which can be used in the diagnosis, treatment or prevention of neurotensin receptor-related conditions such as tumors and hematological malignancies.