Second generation of cisplatin analogs

All these platinum complexes exhibit very strong antitumor activity, suggesting that the platinum oxidation state of either Pt or does not determine the quality of antitumor activity. In general, the activity of platinum(IV) complexes is somewhat smaller than that of platinum(II) complexes. It might well be that the activity of platinum(IV) is, in fact, that of platinum(II), in which case the reduction occurs in vivo, probably by the action of cysteine.  

As already mentioned, the antitumor activity was first ascribed to the cis-complexes of platinum(II), but later on it was found that in some cases trans-configuration can produce an even more pronounced antitumor activity than cw-configuration. 2 

The leaving ligand (X) should not be too labile in the kinetic sense because the complex might become toxic. On the other hand, if the X ligand is kinet-ically too inert, it will become therapeutically inactive. 

The third generation of platinum antitumor agents connects the platinum complex with an adequate molecular carrier. Such a carrier can increase the antitumor activity synergically, and also increase the selectivity toward tumor tissue.  

Recently, an improved version of the photodynamic therapy, which uses a fiber optic cable and specifically triggers the reaction on the desired location, has been published. This is very important because cisplatin is not restricted to cancer cells only. It also attacks healthy cells, which can be minimized by the use of a fiber optic cable. 

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