Radiometals in Theranostics: From Chelate Chemistry to in vivo Studies

Carolyn Anderson - University of Missouri, Columbia

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Meeting ID: 958 6551 0397
Passcode: 417658

Over the past 2-3 decades, research in nuclear medicine imaging and radiopharmaceutical therapy
with radiometals has grown tremendously, with many agents translated to humans, and a few
reaching FDA-approval (e.g. 68Ga/177Lu-dotatate). A renewed interest in alpha- and low-energy
emitters has resulted in innovations in both radionuclide production, as well in the discovery of
new chelators that are versatile for many radiometals. Our lab investigates radiometal-chelates
conjugated to small molecule, peptide, and antibody-based radiopharmaceuticals. The radiometals
Cu-64, Zr-89, Lu-177, and Tb-161 have been labeled to LLP2A, a peptidomimetic with picomolar
affinity for very late antigen 4 (also called integrin 4 1) involved in tumor and immune cell
adhesion and migration. A range of chelators that have been employed for the various radiometals,
affecting the radiolabeling chemistry, in vitro, and in vivo studies. Radiolabeled LLP2A conjugates
are being explored for imaging and therapy in mouse models of melanoma and imaging vasoocclusive
crisis in sickle cell disease. We are also examining how to improve the pharmacokinetics
for radiopharmaceutical therapy. This seminar will discuss advances made in moving LLP2Abased
agents from chemistry to human studies.