212Pb-GRPR (or 212Pb-DOTAM-GRPR1) is a radioimmunoconjugate comprised of ²¹²Pb, the metal chelator DOTAM and a GRPR-targeted antagonist. Gastrin-releasing peptide receptor (GRPR) is a G-protein-coupled receptor of the family of bombesin receptors. Its Ligand, gastrin-releasing peptide (GRP), is a peptide that regulates numerous physiologic functions of the gastrointestinal and central nervous systems, and is overexpressed in a number of cancers, including prostate, breast, colon, melanoma and lung.

A Phase I clinical trial has been initiated early 2023.

Target/Mechanism: GRPR

Carrier/Ligand: Bombesin

Radiation Type: Alpha particle (α)