The gastrin-releasing peptide receptor in oncology: a comprehensive review of recent advances in targeted radionuclide theranostics
By
YunLong Yang
Jiang Fu
ShengJie Tang
Tao Liu
HaiYang Hu
HaiYang Guo
Long Wen
Yang Yang
ChengKuan Liu
GuiYan Yi
Li Yu
HaiNing Zhou
June 8, 2026
Clinical Scorecard: Targeting the Gastrin-Releasing Peptide Receptor in Cancer: An In-Depth Review of Recent Developments in Radionuclide Theranostics
At a Glance
Category Detail
Condition Key Mechanisms Aberrant expression of gastrin-releasing peptide receptor (GRPR) in various malignancies. Target Population Care Setting
Key Highlights
GRPR is overexpressed in multiple solid tumors, making it a target for imaging and therapy. Recent advances in radioligand design and radionuclide selection enhance GRPR-targeted applications. GRPR-targeted imaging shows diagnostic value in prostate cancer and selected tumors. Challenges include receptor heterogeneity and optimization of pharmacokinetics. Guideline-Based Recommendations
Diagnosis
GRPR-targeted imaging can complement traditional imaging modalities for tumor detection. Management
GRPR-directed radioligand therapy (RLT) supports visualization and treatment of tumors. Monitoring & Follow-up
Integration of imaging-based treatment assessment into a closed-loop precision theranostic framework. Risks
Physiologic uptake in normal tissues and receptor heterogeneity pose challenges. Patient & Prescribing Data
Patients with malignancies expressing GRPR, including prostate and breast cancer.
High-stability antagonists and novel therapeutic radionuclides are being developed to improve therapeutic index.
Clinical Best Practices
Utilize GRPR-targeted imaging for biologically relevant information at the receptor level. Consider dual-targeted constructs. Related Resources & Content
