SPECT quantitation of cobalt-57 bleomycin delivery to human brain tumors.
A newly developed and validated noninvasive quantitative SPECT method was used to measure the in vivo uptake of [57Co]bleomycin (Co-bleo) in 13 human brain tumors and the uptake of [99mTc]glucoheptonate (GH) in 23 brain tumors. Significant differences in tumor uptake were found. The tumor concentration over time, the tumor to blood radio at 30 min and the tumor cumulative concentration of radioactivity showed marked differences even between tumors with the same histology. Only a weak correlation was found between tumor concentration of Co-bleo and of GH. Therefore a simple imaging agent such as GH cannot, at the present time, serve as an indicator of individual tumor uptake and further experience with other agents is still necessary. Contrary to the generally held view, no correlation was found between the concentration of drug in the blood and its tumor concentration. It is suggested therefore that the level of a drug in the blood cannot be used as a criterion of the amount that will penetrate the tumor. Direct SPECT measurement of the concentration of the drug in the tumor itself should be performed. The bioavailability of a drug is critical in order for it to exert it tumoricidal effect. The results, showing marked differences in uptake between brain tumors, suggest that before chemotherapy is administered, uptake of the chemotherapeutic drug in the individual tumor to be treated should be assessed and comparisons should be made between the uptake of a series of drugs to determine which drug would be most efficacious on the basis of its uptake as well as its tumor cell killing potential.
D001682:Biological Availability; D001761:Bleomycin / Q000097:blood / Q000493:pharmacokinetics* / Q000031:analogs & derivatives; D001932:Brain Neoplasms / Q000000981:diagnostic imaging / Q000378:metabolism*; D003037:Cobalt Radioisotopes; D006801:Humans; D015609:Organotechnetium Compounds; D013400:Sugar Acids / Q000097:blood / Q000493:pharmacokinetics; D013667:Technetium / Q000097:blood / Q000493:pharmacokinetics; D014055:Tomography, Emission-Computed
D003037:Cobalt Radioisotopes; D015609:Organotechnetium Compounds; D013400:Sugar Acids; C030187:cobalt bleomycin; D001761:Bleomycin; D013667:Technetium; C100014:technetium Tc 99m gluceptate