lutetium-177 CXCR4

Lutetium-177 CXCR4 refers to a class of therapeutic radiopharmaceuticals designed to target the C-X-C chemokine receptor type 4 (CXCR4), with the lead clinical candidate being 177Lu-pentixather (PentixaTher). This agent consists of a high-affinity cyclic peptide antagonist of CXCR4 conjugated to the beta-emitting radioisotope lutetium-177 via a DOTA chelator. CXCR4 is a G-protein coupled receptor that is significantly overexpressed in various hematologic malignancies, such as multiple myeloma and non-Hodgkin lymphoma, as well as several solid tumors, where it promotes tumor cell proliferation, survival, and bone marrow homing. Upon intravenous administration, the drug binds specifically to CXCR4-expressing cells, delivering localized ionizing radiation that induces lethal DNA double-strand breaks. This therapeutic approach is typically part of a theranostic strategy, paired with the PET imaging agent 68Ga-pentixafor to identify patients with sufficient target expression for treatment.

Other names

Lutetium-177 CXCR4Lutetium177 CXCR4Lutetium 177 CXCR4[177Lu]Lu-PentixaTher177Lu-CXCR4