Here, we discovered for the first time a cyclotide ligand of the CCK2R that may for instance be utilized as a stable labelled ligand in imaging applications, as a gut-stable probe, or as a scaffold for designing stabilized peptide ligands of the CCK2R. Thus, our study helped to increase the rich diversity of cyclotides as ligands of GPCR and points to their potential use as starting points for the design of cyclotide-based ligands targeting CCK2R to treat human illnesses such as cancer. Here, CCKBR is linked to cancer.