Evaluation of 62Cu labeled diacetyl-bis(N4-methylthiosemicarbazone) as a hypoxic tissue tracer in patients with lung cancer.
62Cu labeled diacetyl-bis(N4-methylthiosemicarbazone) (62Cu-ATSM) has been proposed as a generator-produced, positron-emitting tracer for hypoxic tissue imaging. From basic studies, the retention mechanism of 62Cu-ATSM is considered to be closely related to cytosolic/microsomal bioreduction, a possible system for hypoxic bioreductive drug activation. In order to evaluate the characteristics of 62Cu-ATSM, PET studies were performed in 4 normal subjects and 6 patients with lung cancer. 62Cu-ATSM cleared rapidly from the blood with little lung uptake (0.43+/-0.09, uptake ratio; divided by the arterial input function) in normal subjects. Intense tumor uptake of 62Cu-ATSM was observed in all patients with lung cancer (3.00+/-1.50). A negative correlation was observed between blood flow and flow-normalized 62Cu-ATSM uptake in three of four patients. In contrast, 62Cu-ATSM uptake was not related to that of 18F-fluorodeoxyglucose. The negative correlation between blood flow and flow normalized 62Cu-ATSM uptake suggests an enhancement of retention of 62Cu-ATSM by low flow. 62Cu-ATSM is a promising PET tracer for tumor imaging, which might bring new information for chemotherapeutic treatment as well as radiotherapy of hypoxic tumors.
Takahashi
N
N
Department of Radiology, Fukui Medical University, Japan.
Fujibayashi
Y
Y
Yonekura
Y
Y
Welch
M J
MJ
Waki
A
A
Tsuchida
T
T
Sadato
N
N
Sugimoto
K
K
Itoh
H
H
D000230:Adenocarcinoma / Q000000981:diagnostic imaging; D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D001943:Breast Neoplasms / Q000556:secondary; D002294:Carcinoma, Squamous Cell / Q000000981:diagnostic imaging; D056831:Coordination Complexes; D003301:Copper Radioisotopes / Q000493:pharmacokinetics / Q000627:therapeutic use*; D005260:Female; D019788:Fluorodeoxyglucose F18 / Q000493:pharmacokinetics; D016166:Free Radical Scavengers / Q000493:pharmacokinetics; D006801:Humans; D008175:Lung Neoplasms / Q000097:blood / Q000000981:diagnostic imaging* / Q000556:secondary; D008297:Male; D008875:Middle Aged; D009942:Organometallic Compounds / Q000493:pharmacokinetics / Q000627:therapeutic use*; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics / Q000627:therapeutic use; D012016:Reference Values; D012039:Regional Blood Flow; D013882:Thiosemicarbazones / Q000493:pharmacokinetics / Q000627:therapeutic use*; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed
D056831:Coordination Complexes; D003301:Copper Radioisotopes; D016166:Free Radical Scavengers; D009942:Organometallic Compounds; D019275:Radiopharmaceuticals; D013882:Thiosemicarbazones; C089548:copper (II) diacetyl-di(N(4)-methylthiosemicarbazone); D019788:Fluorodeoxyglucose F18