CPC A61K 51/088 (2013.01) [A61K 51/08 (2013.01); C07B 59/008 (2013.01)] | 11 Claims |
1. A method of treating a GRPR-positive cancer, the method comprising administering an effective amount of a radiolabeled GRPR-antagonist to a subject, wherein said radiolabeled GRPR-antagonist is of general formula MC-S-P wherein:
M is a radiometal and Cis a metal chelator that binds M, or MC is a Tyr- or prosthetic group bound to a radiohalogen,
S is a spacer covalently linked between C and P, wherein S is covalently attached to the N-terminus of P; and P is DPhe-Gln-Trp-Ala-Val-Gly-His-NH—CH[CH2—CH(CH3)2]2 (SEQ ID NO: 1) wherein the GRPR-positive cancer is selected from prostate cancer, breast cancer, small cell lung cancer, colon carcinoma, gastrointestinal stromal tumors, gastrinoma, renal cell carcinomas, gastroenteropancreatic neuroendocrine tumors, oesophageal squamous cell tumors, neuroblastomas, head and neck squamous cell carcinomas, ovarian cancer, endometrial cancer, and pancreatic cancer.
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