Larger role for Ruthenium anti-cancer agents predictedThis new article by Korean researchers makes several references to
TLD1433. The only ruthenium anti-cancer agent in clinical trials besides
TLD1433, is
NKP1339, which is not a photodynamic compound and has shown only moderate tumour reduction along with some serious safety issues.
Ruthenium Complexes as Anticancer Agents: A Brief History and Perspectives Dovepress
open access to scientific and medical research
Published 3 December 2020 Volume 2020:14 Pages 5375—5392
Authors: Sang Yeul Lee, Chul Young Kim, Tae-Gyu Nam
Department of Pharmacy and Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, Gyeonggi-do 15588, Republic of Korea
Abstract: Platinum (Pt)-based anticancer drugs such as cisplatin have been used to treat various cancers. However, they have some limitations including poor selectivity and toxicity towards normal cells and increasing chemoresistance. Therefore, there is a need for novel metallo-anticancers, which has not been met for decades. Since the initial introduction of ruthenium (Ru) polypyridyl complex, a number of attempts at structural evolution have been conducted to improve efficacy. Among them, half-sandwich Ru-arene complexes have been the most prominent as an anticancer platform. Such complexes have clearly shown superior anticancer profiles such as increased selectivity toward cancer cells and ameliorating toxicity against normal cells compared to existing Pt-based anticancers. Currently, several Ru complexes are under human clinical trials. For improvement in selectivity and toxicity associated with chemotherapy, Ru complexes as photodynamic therapy (PDT), and photoactivated chemotherapy (PACT), which can selectively activate prodrug moieties in a specific region, have also been investigated. With all these studies on these interesting entities, new metallo-anticancer drugs to at least partially replace existing Pt-based anticancers are anticipated. This review covers a brief description of Ru-based anticancer complexes and perspectives.
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".....A number of Ru complexes have shown superior anticancer profiles such as increased selectivity toward cancer cells and ameliorating toxicity against normal cells compared to existing Pt-based anticancer drugs. As a result, four Ru-based anticancer agents, NAMI-A, KP1019 and NKP1339, and TLD1433 have entered clinical trials, but only two entities, NKP1339 and TLD1433 are still under investigation at this point...."
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"...In this review, we present a brief description of Ru-based anticancer complexes. With all the studies on these interesting entities, it is evident that new metalloanticancer drugs with improved efficacy and selectivity, and less toxicity compared to existing Pt-based anticancers should be seen in clinical use to provide new hope for cancer patients..."