lutetium Lu 177 DPI-4452 Debio 0228

A radioconjugate composed of the DOTA cyclic peptide DPI-4452, a carbonic anhydrase IX (CAIX; CA9)-targeting ligand, conjugated to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against CAIX-expressing tumor cells. Upon intravenous administration, lutetium Lu 177 DPI-4452 Debio 0228 targets and binds to CAIX-expressing tumor cells. Upon binding, CAIX-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation. CAIX is a hypoxia-inducible transmembrane glycoprotein that catalyzes the reversible reaction and rapid interconversion of carbon dioxide and water to carbonic acid, protons, and bicarbonate ions. Induced by hypoxia, CAIX is overexpressed in various hypoxic tumors and plays a key role in intra- and extracellular pH regulation, cancer cell progression, tumor aggressiveness ad resistance to treatment.