Radiometallic Complexes of DO3A-Benzothiazole Aniline for Nuclear Medicine Theranostics.
Mol Pharm
; 15(3): 1133-1141, 2018 03 05.
Article
en En
| MEDLINE
| ID: mdl-29381860
ABSTRACT
To develop a radioactive metal complex platform for tumor theranostics, we introduced three radiopharmaceutical derivatives of 1,4,7,10-tetraazacyclododecane-1,4,7-trisacetic acid-benzothiazole aniline (DO3A-BTA, L1) labeled with medical radioisotopes for diagnosis (68Ga/64Cu) and therapy (177Lu). The tumor-targeting ability of these complexes was demonstrated in a cellular uptake experiment, in which 177Lu-L1 exhibited markedly higher uptake in HeLa cells than the 177Lu-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid complex. According to in vivo positron emission tomography imaging, high accumulation of 68Ga-L1 and 64Cu-L1 was clearly visualized in the tumor site, while 177Lu-L1 showed therapeutic efficacy in therapy experiments. Consequently, this molecular platform represents a useful approach in nuclear medicine toward tumor-theranostic radiopharmaceuticals when 68Ga-L1 or 64Cu-L1 is used for diagnosis, 177Lu-L1 is used for therapy, or two of the compounds are used in conjunction with each other.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Radiofármacos
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Benzotiazoles
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Nanomedicina Teranóstica
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Compuestos Heterocíclicos con 1 Anillo
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Compuestos de Anilina
Límite:
Animals
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Female
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Humans
Idioma:
En
Revista:
Mol Pharm
Asunto de la revista:
BIOLOGIA MOLECULAR
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FARMACIA
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FARMACOLOGIA
Año:
2018
Tipo del documento:
Article