GRPR Expression in Metastatic Cancers: A Review of ...

Section snippets

Physiological GRPR Expression and Dosimetry Data in Healthy Human Tissues

Peripheral physiological expression of GRPR include mostly the pancreas and the gastrointestinal tract.2, 3, 4 Partly due to intravenous infusion, GRPR-targeting radiopharmaceuticals also appears to have a weak antigen (PSMA)-TRT.5

With adequate renal protecting infusion, kidneys absorbed dose are approximately two times lower than other clinically used TRT radiopharmaceuticals such as [177Lu]Lu-PSMA-617 and [177Lu]Lu-DOTATATE.5,6

Radiopharmaceuticals also showed difference in physiological

Prostate Cancer

Prostate cancer is probably the field where GRPR imaging and TRT are currently the most explored. GRPR is overexpressed in 84% of prostate cancer cells8 which makes it an excellent target for TRT, considering PSMA is overexpressed in 90% of them.9 In advanced stages such as metastatic and castration resistant prostate cancer, GRPR expression is overall lower than PSMA, with only 23.5% showing high GRPR expression at late stages.10 Furthermore, GRPR expression seems to be regulated by the action

Innovations in the Development of GRPR-Based Targeted Radionuclide Therapy

GRPR-radioantagonists have been extensively reviewed in.1 In this chapter, innovations that would offer increased dose deposit compared with the standard-of-care 177Lu are be described herein.

Conclusion

The field of GRPR is rapidly evolving and GRPR-TRT should be feasible in several cancers in the near future including prostate cancer, breast cancer, GIST, lung cancer and melanoma. The expression profile of GRPR still need to be refined for better patients’ selection and the cost-effectiveness of this approach.

CRediT authorship contribution statement

Aurélien Callaud: Writing – original draft, Writing – review & editing. Heying Duan: Conceptualization, Writing – original draft, Writing – review & editing. Elif Hindié: Writing – review & editing. Clément Morgat: Conceptualization, Data curation, Writing – original draft, Writing – review & editing. Andrei Iagaru: Conceptualization, Project administration, Writing – review & editing.

Declaration of competing interest

Andrei Iagaru reports scientific advisory board fees from Alpha9Tx, Clarity Pharmaceuticals, and Radionetics Oncology; research grants from GE HealthCare and Novartis; consulting fees from GE HealthCare, Novartis, Progenics Pharmaceuticals, and Telix; and roles on scientific steering committees for Novartis. The remaining authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Acknowledgments

This work was achieved within the frame of the NEWMOON Impulsion of Bordeaux University.