Abstract
After nearly 20 years of research on the use of ruthenium in the fight against cancer, only two Ru(III) coordination complexes have advanced to clinical trials. During this time, the field has produced excellent candidate drugs with outstanding in vivo and in vitro activity; however, we have yet to find a ruthenium complex that would be a viable alternative to platinum drugs currently used in the clinic. We aimed to explore what we have learned from the most prominent complexes in the area, and to challenge new concepts in chemical design. Particularly relevant are studies involving NKP1339, NAMI-A, RM175, and RAPTA-C, which have paved the way for current research. We explored the development of the ruthenium anticancer field considering that the mechanism of action of complexes no longer focuses solely on DNA interactions, but explores a diverse range of cellular targets involving multiple chemical strategies.
Highlights
Cancer is a major health burden in the developed world
This space is currently addressed with the use of platinum(II) coordination complexes, namely Cisplatin (CDDP), Oxaliplatin and Carboplatin, alongside Nedaplatin and Lobaplatin, which are restricted to selected markets
The prevalence of platinum resistance in the clinic, both intrinsic and acquired [3,4,5], is an escalating clinical concern, especially considering that platinum drugs are currently used in over half of all chemotherapy regimens [3]. This has sparked the development of a new generation of cytotoxics based on different metals, and corresponding coordination complexes, which excel in cellular selectivity and retain their use against a wide range of malignancies, while exhibiting unique mechanism(s) of action
Summary
Many breakthroughs in biological targeted approaches have occurred (immunological therapy), an unmet clinical need remains for a large section of the patient population, so wide-spectrum chemotherapy agents are still required This space is currently addressed with the use of platinum(II) coordination complexes, namely Cisplatin (CDDP), Oxaliplatin and Carboplatin (worldwide approval), alongside Nedaplatin and Lobaplatin, which are restricted to selected markets. The prevalence of platinum resistance in the clinic, both intrinsic and acquired [3,4,5], is an escalating clinical concern, especially considering that platinum drugs are currently used in over half of all chemotherapy regimens [3] This has sparked the development of a new generation of cytotoxics based on different metals, and corresponding coordination complexes, which excel in cellular selectivity and retain their use against a wide range of malignancies, while exhibiting unique mechanism(s) of action.
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