US 12,064,489 B2
Radiolabeled GRPR-antagonists for diagnostic imaging and treatment of GRPR-positive cancer
Theodosia Maina-Nock, Athens (GR); Berthold Artur Nock, Athens (GR); and Marion de Jong Hendriks, TN Vlaardingen (NL)
Assigned to Advanced Accelerator Applications International SA, Geneva (CH)
Filed by Advanced Accelerator Applications International SA, Geneva (CH)
Filed on Jul. 23, 2021, as Appl. No. 17/383,550.
Application 17/383,550 is a continuation of application No. 16/580,990, filed on Sep. 24, 2019, granted, now 11,083,805.
Application 16/580,990 is a continuation of application No. 15/817,776, filed on Nov. 20, 2017, abandoned.
Application 15/817,776 is a continuation of application No. 14/431,096, granted, now 9,839,703, issued on Dec. 12, 2017, previously published as PCT/US2013/061712, filed on Sep. 25, 2013.
Prior Publication US 2021/0346528 A1, Nov. 11, 2021
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 51/08 (2006.01); C07B 59/00 (2006.01)
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.