Severe side effects and poor therapeutic efficacy are the main drawbacks of current anticancer drugs. These problems can be mitigated by targeting, but the targeting efficacy of current drugs is poor and urgently needs improvement. Taking this into consideration, this Review first summarizes the current targeting strategies for cancer therapy in terms of cancer tissue and organelles. Then, we analyse the systematic targeting of anticancer drugs and conclude that a typical journey for a targeted drug administered by intravenous injection is a CTIO cascade of at least four steps. Furthermore, to ensure high overall targeting efficacy, the properties of a targeting drug needed in each step are further analysed, and some guidelines for structure optimization to obtain effective targeting drugs are offered. Finally, some viewpoints highlighting the crucial problems and potential challenges of future research on targeted cancer therapy are presented. This review could actively promote the development of precision medicine against cancer.
Keywords: cancer therapy; drug delivery; medicinal chemistry; molecular engineering; targeting strategies.
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