A Vision for Gastrin-Releasing Peptide Receptor Targeting for Imaging and Therapy: Perspective from Academia and Industry

The gastrin-releasing peptide receptor (GRPR) is overexpressed in various cancers, including prostate cancer, breast cancer, small cell and non–small cell lung cancer, uterine and ovarian cancer, colon cancer, and gastrointestinal stromal tumors. This makes GRPR a multicancer target for theranostics, that is, molecular imaging and therapy. Here, we explore the current state of GRPR-targeted theranostics from bench to bedside, highlighting the preclinical development of various GRPR-targeting compounds and clinical applications. We review the role of GRPR-targeted molecular imaging for all stages of prostate cancer, breast cancer, and other tumors and provide a quo vadis GRPR. We aimed to offer a comprehensive overview of GRPR-targeted theranostics to inform researchers, clinicians, pharma, and regulators of the potential benefits and emerging opportunities in the pursuit of personalized precision cancer care.