Cu-ATSM: a radiopharmaceutical for the PET imaging of hypoxia.
Copper(II)-diacetyl-bis(N(4)-methylthiosemicarbazone), Cu-ATSM, labeled with a positron emitting isotope of copper ((60)Cu, (61)Cu, (62)Cu or (64)Cu) has been shown, in vitro and in vivo, to be selective for hypoxic tissue. In silico studies have explored the mechanism of its hypoxia selectivity, and clinical studies with this agent have shown non-invasive imaging data that is predictive of a cancer patients' response to conventional therapy. This Perspective discusses the evolution of Cu-ATSM, how its selectivity can be improved upon, and where this metal-ligand platform could be taken in the future.
Vāvere
Amy L
AL
Department of Radiology, Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO 63110, USA.
Lewis
Jason S
JS
D056831:Coordination Complexes; D006801:Humans; D000860:Hypoxia / Q000000981:diagnostic imaging*; D015394:Molecular Structure; D009369:Neoplasms / Q000000981:diagnostic imaging / Q000628:therapy; D009942:Organometallic Compounds / Q000737:chemistry; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000737:chemistry; D013882:Thiosemicarbazones / Q000737:chemistry
D056831:Coordination Complexes; D009942:Organometallic Compounds; D019275:Radiopharmaceuticals; D013882:Thiosemicarbazones; C089548:copper (II) diacetyl-di(N(4)-methylthiosemicarbazone)