NAMI-A ((ImH)[trans-RuCl4(dmso-S)(Im)], Im = imidazole) and KP1019/1339 (KP1019
= (IndH)[trans-RuCl4(Ind)2], Ind = indazole; KP1339 = Na[trans-RuCl4(Ind)2]) are two structurally
related ruthenium(III) coordination compounds that have attracted a lot of attention in the medicinal
inorganic chemistry scientific community as promising anticancer drug candidates. This has led to a
considerable amount of studies on their respective chemico-biological features and to the eventual
admission of both to clinical trials. The encouraging pharmacological performances qualified KP1019
mainly as a cytotoxic agent for the treatment of platinum-resistant colorectal cancers, whereas the
non-cytotoxic NAMI-A has gained the reputation of being a very eective antimetastatic drug.
A critical and strictly comparative analysis of the studies conducted so far on NAMI-A and KP1019
allows us to define the state of the art of these experimental ruthenium drugs in terms of the
respective pharmacological profiles and potential clinical applications, and to gain some insight into
the inherent molecular mechanisms. Despite their evident structural relatedness, deeply distinct
biological and pharmacological profiles do emerge. Overall, these two iconic ruthenium complexes
form an exemplary and unique case in the field of medicinal inorganic chemistry.
