Novel heterobimetallic radiotheranostic: preparation, activity, and biodistribution.
A novel Ru(II) (arene) theranostic complex is presented. It is based on a 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid macrocycle bearing a triarylphosphine and can be tracked in vivo by using the γ emission of (153) Sm atoms. Notably, the heteroditopic ligand can be selectively metalated with ruthenium at the phosphorus atom despite the presence of other functionalities that are prone to metal coordination. Subsequent labeling with radionuclides such as (153) Sm can then be performed easily. The resulting heterobimetallic complex exhibits favorable solubility and stability properties in biologically relevant media. It also shows in vitro cytotoxicity in line with that expected for this type of metallodrug, and is nontoxic to the organism as a whole. As a proof of concept, initial studies in healthy mice were performed to obtain information about the uptake, biodistribution, and excretion of the radiolabeled complex.
Institut de Chimie Moléculaire de l'Université de Bourgogne, UMR 6302 CNRS, Université de Bourgogne, 9 avenue A. Savary, BP47870, 21078 Dijon (France).
Louis
L
Adriaenssens
Qiang
Q
Liu
Fanny
F
Chaux-Picquet
Semra
S
Tasan
Michel
M
Picquet
Franck
F
Denat
Pierre
P
Le Gendre
Fernanda
F
Marques
Célia
C
Fernandes
Filipa
F
Mendes
Lurdes
L
Gano
Maria Paula Cabral
MP
Campello
Ewen
E
Bodio
D000818:Animals; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D056831:Coordination Complexes / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D006573:Heterocyclic Compounds, 1-Ring / Q000737:chemistry; D006801:Humans; D007553:Isotope Labeling; D051379:Mice; D010720:Phosphines / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D012428:Ruthenium / Q000737:chemistry*; D014018:Tissue Distribution; D014867:Water / Q000737:chemistry
D056831:Coordination Complexes; D006573:Heterocyclic Compounds, 1-Ring; D010720:Phosphines; D019275:Radiopharmaceuticals; D014867:Water; C071349:1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid; D012428:Ruthenium
heterometallic complexes; macrocycles; phosphines; radiopharmaceuticals; theranostics