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A Journal on Nuclear Medicine and Molecular Imaging
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The Quarterly Journal of Nuclear Medicine 2000 March;44(1):50-8

Copyright © 2009 EDIZIONI MINERVA MEDICA

language: English

New radiopharmaceuticals for receptor scintigraphy and radionuclide therapy

Virgolini I., Traub T., Leimer M., Novotny C., Pangerl T., Ofluoglu S., Halvadjieva E., Smith-Jones P., Flores J., Li S. R., Angelberger P., Havlik E., Andreae F., Raderer M., Kurtaran A., Niederle B., Dudczak R.

From the Department of Nuclear Medicine University of Vienna, Vienna, Austria


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In ­vitro ­data ­have dem­on­strat­ed a ­high ­amount of recep­tors for var­i­ous hor­mones and pep­tides on malig­nant ­cells of neu­ro­en­do­crine ori­gin. Among ­these, bind­ing ­sites for mem­bers of the SST-fam­i­ly (hSSTR1-5) are fre­quent­ly ­found, and ­their expres­sion has led to ther­a­peu­tic and diag­nos­tic ­attempts to spe­cif­i­cal­ly tar­get ­these recep­tors. Receptor scin­tig­ra­phy ­using radio­lab­eled pep­tide ­ligands has prov­en its effec­tive­ness in clin­i­cal prac­tice. In addi­tion, ­initial ­results ­have indi­cat­ed a clin­i­cal poten­tial for recep­tor-tar­get­ed radio­ther­a­py. Based on som­a­tos­ta­tin (SST) recep­tor (R) rec­og­ni­tion, the nov­el radio­phar­ma­ceu­ti­cals 111In/90Y-­DOTA-lan­re­o­tide devel­oped at the University of Vienna as ­well as 111In/90Y-­DOTA-DPhe1-Tyr3-octre­o­tide (NOVAR­TIS) ­both ­have pro­vid­ed prom­is­ing ­data for diag­no­sis and treat­ment of hSSTR-pos­i­tive ­tumors. ­SSTR scin­tig­ra­phy ­using 111In-­DTPA-DPhe1-octre­o­tide has a ­high pos­i­tive pre­dic­tive val­ue for the ­vast major­ity of neu­ro­en­do­crine ­tumors and has ­gained its ­place in the diag­nos­tic ­work-up as ­well as fol­low-up of ­patients. We ­have ­used 111In-­DOTA-lan­re­o­tide scin­tig­ra­phy in 166 ­patients ­since 1997 and ­have ­seen pos­i­tive ­results in 93% of ­patients. In 42 ­patients ­with neu­ro­en­do­crine ­tumors com­par­a­tive ­data ­were ­obtained. As ­opposed to 111In-­DTPA-DPhe1-octre­o­tide and 111In-­DOTA-DPhe1-Tyr3-octre­o­tide, dis­crep­an­cies in the scin­ti­graph­ic ­results ­were ­seen in ­about one ­third of ­patients con­cern­ing ­both the ­tumor ­uptake as ­well as ­tumor ­lesion detec­tion. Initial ­results ­both ­with 90Y-­DOTA-lan­re­o­tide as ­well as 90Y-­DOTA-DPhe1-Tyr3-octre­o­tide has point­ed out the clin­i­cal poten­tial of radio­nu­clide recep­tor-tar­get­ed radio­ther­a­py. This new ther­a­py ­couid ­offer pal­li­a­tion and dis­ease con­trol at a ­reduced ­cost. The ­final pep­tide ther­a­py strat­e­gy is ­most prob­ably cheap­er ­than con­ven­tion­al radio­ther­a­pies or pro­longed chem­o­ther­a­pies. Overall, recep­tor-medi­at­ed radio­ther­a­py ­with 90Y-­DOTA-lan­re­o­tide/90Y-­DOTA-DPhe1-Tyr3-octre­o­tide ­might ­also be effec­tive in ­patients refrac­to­ry to con­ven­tion­al strat­e­gies.

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