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The ORCID identification number(s) for the author(s) of this article can be found under https://doi.org/10.1002/smll.202000363. Iridium(III) complexes are potent candidates for photodynamic therapy. However, their clinical usage is impeded by their poor water solubility, high dark toxicity, and negligible absorption in near-infrared region (NIR region). Here, it is proposed to solve these challenges by developing an iridium(III) complexe-based polymeric micelle system. This system is self-assembled using an iridium(III) complex-containing amphiphilic block polymer. The upconversion nanoparticles are included in the polymeric micelles to permit NIR excitation. Compared with the nonformulated iridium(III) complexes, under NIR stimulation, this polymeric micelle system exhibits higher 1 O 2 generation efficiency, negligible dark toxicity, excellent tumor-targeting ability, and synergistic phototherapy-chemotherapy effect both in vitro and in vivo. www.advancedsciencenews.com

Although classical platinum drugs such as cisplatin, carboplatin and oxaliplatin play a vitally important role in cancer treatment, nonselective distribution of platinum drugs in normal and tumor cells can induce serious gastrointestinal reaction, nephrotoxicity, ototoxicity, neurotoxicity and cross resistance, limiting their applications. Over the past few years, a great number of platinum complexes of non-classical structures have been extensively investigated and evaluated in vitro and in vivo, some of them exhibiting considerable activity. In this review, platinum-based complexes with non-classical structures which have anticancer potential are described and several representative examples are discussed with their mechanism of action.

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