Theranostics 2022; 12(5):2115-2132. doi:10.7150/thno.69424 This issue


Platinum-based drugs for cancer therapy and anti-tumor strategies

Chunyu Zhang1,2#, Chao Xu3#, Xueyun Gao2✉, Qingqiang Yao1✉

1. Institute of Materia Medica, Shandong First Medical University & Shandong Academy of Medical Sciences, Jinan 250000, Shandong, China.
2. Department of Life Science and Chemistry, Faculty of Environment and Life Science, Beijing University of Technology, Beijing 100124, China.
3. College of Chemistry and Material Science, Shandong Agricultural University, Tai'an 271018, Shandong, China.
#These authors contributed equally to this work.

This is an open access article distributed under the terms of the Creative Commons Attribution License ( See for full terms and conditions.
Zhang C, Xu C, Gao X, Yao Q. Platinum-based drugs for cancer therapy and anti-tumor strategies. Theranostics 2022; 12(5):2115-2132. doi:10.7150/thno.69424. Available from

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Graphic abstract

Platinum-based drugs cisplatin, carboplatin, and oxaliplatin are widely used for chemotherapeutic eradication of cancer. However, the side effects of platinum drugs, such as lack of selectivity, high systemic toxicity, and drug resistance, seriously limit their clinical application. With advancements in nanotechnology and chemical synthesis, Pt-based anti-cancer drugs have made great progress in cancer therapy in recent years. Many strategies relied on the anti-cancer mechanism similar to cisplatin and achieved some success by modifying existing platinum drugs. Pt-based nanodrugs, such as platinum nanoclusters, have novel anti-cancer mechanisms and great potential in tumor-targeted therapy and have shown promising results in clinical application. In this review, we systematically explored the development of first-line platinum chemotherapy drugs in the clinic and their anti-cancer mechanisms. We also summarize the progress of Pt-based anti-cancer drug application in cancer therapy, emphasizing their modification to enhance the anti-tumor effect. Finally, we address challenges faced by platinum chemotherapy drugs, especially Pt nanocluster-based nanodrugs, in cancer treatment. The new platinum drugs and their targeted modifications undoubtedly provide a promising prospect for improving the current anti-cancer treatments.

Keywords: Platinum-based drugs, Cancer therapy, Anti-cancer mechanism, Systemic toxicity, Platinum nanoclusters