The gastrin-releasing peptide receptor in oncology: a comprehensive review of recent advances in targeted radionuclide theranostics - Report - MDSpire

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

  • 0 min

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Clinical Report: Targeting the Gastrin-Releasing Peptide Receptor in Cancer

Overview

The gastrin-releasing peptide receptor (GRPR) is overexpressed in various malignancies, making it a significant target for molecular imaging and radionuclide therapy. Recent advancements in GRPR-targeted radioligands have shown promising diagnostic and therapeutic potential, although challenges remain in clinical application.

Background

Cancer continues to pose a significant global health challenge, with millions of new cases and deaths each year. Targeting specific receptors, such as GRPR, offers a promising approach for enhancing the precision of cancer imaging and therapy. The aberrant expression of GRPR in several solid tumors highlights its potential as a molecular target in nuclear oncology.

Data Highlights

No numerical data available in the provided source material.

Key Findings

  • GRPR is overexpressed in prostate cancer, breast cancer, lung cancer, and gastrointestinal stromal tumors.
  • GRPR-targeted imaging has shown diagnostic value in prostate cancer and estrogen receptor-positive breast cancer.
  • Advancements in radioligand design and radionuclide selection are enhancing GRPR-mediated oncologic applications.
  • Challenges include receptor heterogeneity, physiologic uptake in normal tissues, and optimization of pharmacokinetics.
  • Future developments may involve ligand engineering and dual-target strategies for improved therapeutic outcomes.

Clinical Implications

GRPR-targeted imaging and therapy may complement existing modalities, providing biologically relevant information for tumor characterization. Clinicians should be aware of the ongoing research and potential applications of GRPR-targeted strategies in precision medicine.

Conclusion

GRPR-targeted theranostics represent a promising area of research in oncology, with ongoing advancements aimed at overcoming existing challenges and enhancing clinical application.

Related Resources & Content

  1. NCCN Guidelines® Insights: Prostate Cancer, Version 5.2026 - PubMed
  2. Diagnostic performance of gastrin-releasing peptide receptor-targeted positron-emission tomography in biochemically recurrent prostate cancer—a systematic review and meta-analysis - PMC
  3. Phase 1 Study of [177Lu]Lu-NeoB in Patients with Advanced Solid Tumors Overexpressing Gastrin-Releasing Peptide Receptor: Preliminary Safety and Dosimetry Results - PMC
  4. The ASCO Post — Pretargeted Dual-Isotope Radionuclide Therapy in Colorectal Cancer
  5. Journal of Gastroenterology — Utilization of Targeted Alpha-Emitter Therapy for Gastroenteropancreatic Neuroendocrine Tumors
  6. Journal of Gastrointestinal Surgery — Surgical Guidance Using Radiotracers for Gastroenteropancreatic Neuroendocrine Tumors: A Comprehensive Review of the Literature
  7. The ASCO Post — Investigational PSMA-Targeted Radioligand Reduced Off-Target Uptake in Prostate Cancer Models
  8. Pretargeted Dual-Isotope Radionuclide Therapy in Colorectal Cancer
  9. Utilization of Targeted Alpha-Emitter Therapy for Gastroenteropancreatic Neuroendocrine Tumors
  10. Surgical Guidance Using Radiotracers for Gastroenteropancreatic Neuroendocrine Tumors: A Comprehensive Review of the Literature
  11. NCCN Guidelines® Insights: Prostate Cancer, Version 5.2026 - PubMed
  12. Diagnostic performance of gastrin-releasing peptide receptor-targeted positron-emission tomography in biochemically recurrent prostate cancer—a systematic review and meta-analysis - PMC
  13. Phase 1 Study of [177Lu]Lu-NeoB in Patients with Advanced Solid Tumors Overexpressing Gastrin-Releasing Peptide Receptor: Preliminary Safety and Dosimetry Results - PMC

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