Indium bleomycin

The major uses of lndlum-111 in medicine are listed in Table 2. Indium-111 labeled DTPA is the preferred agent for the study of cerebral spinal fluid kinetics (cisternography)( ). Indium-labeled bleomycin has been used for tumor scanning C2.), although citrate has achieved greater clinical use. It appears that indium bleomycin is in fact a weak chelate and the in vivo distribution is very similar to that of indium transferrin. 

Haslett, C., Shen, A.S., Feldsien, D.C., Allen, D., Henson, P.M. and Cherniack, R.M. (1989b). " Indium-labelled neutrophil flux into the lungs of bleomycin-treated rabbits assessed non-invasively by external scintigraphy. Am. Rev. Respir. Dis. 140, 756-763. 

The 29Si NMR spectra of (138), where M = Ga, In, R = SiMe Bu2, are consistent with preferential localisation of negative charge on the terminal silicon atom.641 The 1-D and 2-D 111 NMR studies on the indium(III)-bleomycin A2 (InBLM) show that the BLM is coordinated to In(III) through five N atoms, to give a distorted tetragonal pyramidal structure.642... 

The role of metal speciation in bleomycin uptake and cytotoxicity has been studied extensively. The relatively high amounts of copper in the blood, however,suggest that exogenous or endogenous metals in the blood do not markedly alter the uptake or activity of bleomycin. Nonetheless, a number of other metals can bind to bleomycin including indium and cobalt, and formulating bleomycin with these ex vivo can significantly reduce the cytotoxicity of bleomycin (Lyman et al. 1986). Complexes of this type have been used, however, to examine tumor cell uptake of bleomycin compounds. 

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