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Peer-reviewedCC BYPharmaceutics

CCKBR (Gastrin Receptor) as a Theranostic Target in Oncology: Biological Rationale, Diagnostic Imaging, and Next-Generation Peptide-Based Drug Development.

  • Ming-Cheng Chang1
  • Chun-Tang Chen1
  • Wan-Chi Lee1
  • Yi-Jou Tai2,3
  • Ying-Cheng Chiang2,3,4
4 affiliations
  1. 1Department of Isotope Application Research, National Atomic Research Institute, No. 1000, Wenhua Rd., Longtan Dist., Taoyuan City 325207, Taiwan.
  2. 2Department of Obstetrics and Gynecology, College of Medicine, National Taiwan University, Taipei 100226, Taiwan.
  3. 3Department of Obstetrics and Gynecology, National Taiwan University Hospital, Taipei 100226, Taiwan.
  4. 4Department of Obstetrics and Gynecology, National Taiwan University Hospital Hsin-Chu Branch, Hsinchu City 300195, Taiwan.
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Abstract

Cholecystokinin B receptor (CCKBR) is a promising theranostic target because of its overexpression in several malignancies, including medullary thyroid carcinoma, small-cell lung cancer, gastric cancer, and pancreatic cancer. Its high-affinity ligand binding and efficient receptor-mediated internalization provide a strong biological basis for molecular imaging and peptide receptor radionuclide therapy (PRRT). Recent advances in radiolabeled gastrin and mini-gastrin analogues have improved tumor targeting, metabolic stability, and pharmacokinetic profiles, supporting their application in both diagnostic imaging and radionuclide therapy. This review summarizes the molecular biology and tumor expression of CCKBR, recent progress in SPECT/PET imaging and targeted radionuclide therapy, and advances in ligand and pharmacokinetic engineering. Despite substantial progress, CCKBR-targeted theranostics remain less clinically established than SSTR- or PSMA-based platforms. Major challenges include heterogeneous receptor expression, renal and gastric uptake, limited prospective clinical evidence, and the lack of standardized imaging, dosimetry, and treatment protocols. Addressing these limitations will be essential for the broader clinical translation of CCKBR-targeted theranostics.

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Cite

BibTeXRIS
BibTeX
@article{chang2026cckbr,
  title = {{CCKBR (Gastrin Receptor) as a Theranostic Target in Oncology: Biological Rationale, Diagnostic Imaging, and Next-Generation Peptide-Based Drug Development.}},
  author = {Ming-Cheng Chang and Chun-Tang Chen and Wan-Chi Lee and Yi-Jou Tai and Ying-Cheng Chiang},
  journal = {Pharmaceutics},
  year = {2026},
  month = sep,
  doi = {10.3390/pharmaceutics18101198},
  url = {https://europepmc.org/article/MED/42942730},
  note = {CC BY},
}
RIS
TY  - JOUR
TI  - CCKBR (Gastrin Receptor) as a Theranostic Target in Oncology: Biological Rationale, Diagnostic Imaging, and Next-Generation Peptide-Based Drug Development.
AU  - Ming-Cheng Chang
AU  - Chun-Tang Chen
AU  - Wan-Chi Lee
AU  - Yi-Jou Tai
AU  - Ying-Cheng Chiang
PY  - 2026
DA  - 2026/09/22
JO  - Pharmaceutics
DO  - 10.3390/pharmaceutics18101198
UR  - https://europepmc.org/article/MED/42942730
AB  - Cholecystokinin B receptor (CCKBR) is a promising theranostic target because of its overexpression in several malignancies, including medullary thyroid carcinoma, small-cell lung cancer, gastric cancer, and pancreatic cancer. Its high-affinity ligand binding and efficient receptor-mediated internalization provide a strong biological basis for molecular imaging and peptide receptor radionuclide therapy (PRRT). Recent advances in radiolabeled gastrin and mini-gastrin analogues have improved tumor targeting, metabolic stability, and pharmacokinetic profiles, supporting their application in both diagnostic imaging and radionuclide therapy. This review summarizes the molecular biology and tumor expression of CCKBR, recent progress in SPECT/PET imaging and targeted radionuclide therapy, and advances in ligand and pharmacokinetic engineering. Despite substantial progress, CCKBR-targeted theranostics remain less clinically established than SSTR- or PSMA-based platforms. Major challenges include heterogeneous receptor expression, renal and gastric uptake, limited prospective clinical evidence, and the lack of standardized imaging, dosimetry, and treatment protocols. Addressing these limitations will be essential for the broader clinical translation of CCKBR-targeted theranostics.
SN  - 1999-4923
ER  -