Synthesis, biodistribution, and estrogen receptor scintigraphy of indium-111-diethylenetriaminepentaacetic acid-tamoxifen analogue.
This study was aimed at developing a hydrophilic diethylenetriaminepentaacetic acid-tamoxifen (DTPA-Tam) analogue for use in imaging estrogen receptor positive (ER+) lesions. In rat uterine cytosol, the IC50 of DTPA-Tam conjugate was 1 microM and of tamoxifen, 2 microM. Biodistribution, autoradiography, and radionuclide imaging of 111In-DTPA-Tam in breast-tumor-bearing rats showed that tumor-to-tissue ratios increased steadily between 30 min and 48 h. The in vivo response of MCF-7 breast cancer xenografts to tamoxifen and DTPA-Tam in nude mice demonstrated that DTPA-Tam could reduce tumor growth rate. These results indicate that DTPA-Tam, a new hydrophilic ER+ ligand, might be useful in diagnosing ER+ lesions.
Delpassand
E S
ES
Division of Diagnostic Imaging, University of Texas M. D. Anderson Cancer Center, Houston 77030, USA.
Yang
D J
DJ
Wallace
S
S
Cherif
A
A
Quadri
S M
SM
Price
J
J
Joubert
A
A
Inoue
T
T
Podoloff
D A
DA
D000818:Animals; D001345:Autoradiography; D001943:Breast Neoplasms / Q000000981:diagnostic imaging / Q000188:drug therapy / Q000648:ultrastructure; D004958:Estradiol / Q000378:metabolism; D005260:Female; D006801:Humans; D007205:Indium Radioisotopes / Q000737:chemistry; D007700:Kinetics; D008325:Mammary Neoplasms, Experimental / Q000188:drug therapy / Q000532:radiotherapy / Q000648:ultrastructure; D051379:Mice; D008819:Mice, Nude; D004369:Pentetic Acid / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D011877:Radionuclide Imaging; D051381:Rats; D011916:Rats, Inbred F344; D011960:Receptors, Estrogen / Q000032:analysis* / Q000378:metabolism; D013629:Tamoxifen / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology; D014018:Tissue Distribution; D014316:Tritium; D014407:Tumor Cells, Cultured
D007205:Indium Radioisotopes; D011960:Receptors, Estrogen; D013629:Tamoxifen; D014316:Tritium; D004958:Estradiol; D004369:Pentetic Acid