²¹²Pb-DOTAM-GRPR1

²¹²Pb-DOTAM-GRPR1 is an investigational targeted alpha therapy (TAT) radiopharmaceutical developed by Orano Med. It is a radioligand conjugate comprising the alpha-particle-emitting radionuclide lead-212 (²¹²Pb), the macrocyclic metal chelator DOTAM (1,4,7,10-tetrakis(carbamoylmethyl)-1,4,7,10-tetraazacyclododecane), and GRPR1, a peptide antagonist that targets the gastrin-releasing peptide receptor (GRPR). GRPR is a G-protein–coupled receptor frequently overexpressed in various solid tumors, including prostate, breast, lung, colorectal, and cervical cancers. Upon binding to GRPR on the surface of cancer cells, the lead-212 isotope decays, emitting high-energy alpha particles that cause lethal double-strand DNA breaks within a short range, thereby minimizing damage to surrounding healthy tissue. The drug is currently being evaluated in a Phase 1 first-in-human clinical trial for patients with recurrent or metastatic GRPR-expressing tumors.

Other names

212Pb-DOTAM-GRPR1