Methods for imaging and treatment of somatostatin-receptor positive tumors
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Publication Number
US-12290551-B2
Publication Date
2025-05-06
Expiration Date
Abstract
Methods for treating, identifying and localizing tumors expressing somatostatin receptors (SRs), including methods of enhancing the efficacy of imaging techniques by administration of a heteroaryl-ketone fused azadecalin glucocorticoid receptor modulator (HKGRM) effective to increase SR expression in tumors. HKGRM administration for enhancing SR-based tumor imaging and treating neuroendocrine tumors. HKGRM and somatostatin or somatostatin analog combination therapy for treating and enhancing SR-based tumor imaging.
Core Innovation
The invention relates to methods for localizing a neuroendocrine tumor in a patient by using a glucocorticoid receptor modulator (GRM) to stimulate tumor somatostatin receptor expression, followed by administration of a radiolabeled somatostatin analog and imaging. The approach is configured for a patient hosting a neuroendocrine tumor having a baseline level of somatostatin receptor expression, and is effective to provide an image of the tumor within the patient to support tumor localization.
A key aspect is that the GRM is relacorilant, defined as a heteroaryl-ketone fused azadecalin GRM. Relacorilant is administered as daily doses in an escalating multi-week regimen, and the regimen is described as effective to stimulate the expression of somatostatin receptors (SRs) in the neuroendocrine tumor. After relacorilant, at least one dose of a radiolabeled somatostatin analog is administered and then the patient is imaged.
The invention positions the localization method as avoiding clinically significant endocrine effects. The method is defined as localizing the neuroendocrine tumor without leading to significant increases in cortisol and without increasing the risk of hypokalemia in the patient, and is presented in the context of neuroendocrine tumors relevant to Cushing’s syndrome, including differential diagnosis and treatment selection for ACTH-dependent versus adrenal/exogenous Cushing’s.
Claims Coverage
The partial content identifies one independent claim. It contains four core inventive elements: administering relacorilant to stimulate somatostatin receptor expression, administering radiolabeled somatostatin analog(s), imaging to localize the neuroendocrine tumor, and limiting cortisol increase and hypokalemia risk.
Relacorilant dosing to stimulate tumor somatostatin receptor expression
Administering daily doses of the heteroaryl-ketone fused azadecalin GRM relacorilant in an escalating regimen effective to stimulate the expression of somatostatin receptors (SRs) in said neuroendocrine tumor.
Radiolabeled somatostatin analog administration
Administering at least one dose of a radiolabeled somatostatin analog.
Imaging for tumor localization
Imaging the patient effective to provide an image of the tumor within the patient.
Localization without significant cortisol increase and without hypokalemia risk increase
Localizing the neuroendocrine tumor without leading to significant increases in cortisol and without increasing the risk of hypokalemia in the patient.
Across the independent claim, the inventive core is the sequence of administering relacorilant to stimulate tumor SR expression, administering radiolabeled somatostatin analog(s), and imaging to localize the neuroendocrine tumor, while avoiding significant cortisol increases and increased hypokalemia risk.
Stated Advantages
Localizes a neuroendocrine tumor without leading to significant increases in cortisol.
Localizes a neuroendocrine tumor without increasing the risk of hypokalemia.
Stimulates expression of somatostatin receptors (SRs) in the neuroendocrine tumor to provide an image after radiolabeled somatostatin analog administration.
Documented Applications
Localizing neuroendocrine tumors in patients hosting neuroendocrine tumors, including relevance to Cushing’s syndrome, ACTH-dependent Cushing’s syndrome, and ectopic ACTH syndrome.
Applied to patients with Cushing’s syndrome.
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