| Summary: | Abstract How to efficiently deliver therapeutic agents into cancer cells is a knotty problem for researchers. Over the past 30 years, the use of cell‐penetrating peptides (CPPs) to facilitate intracellular cargo delivery has received extensive attention. Encouraged by their robust membrane permeability and satisfactory biocompatibility, various CPPs have been applied to construct anticancer drugs. However, owing to some unsolved problems, such as lack of cell selectively, short circulation time, and poor in vivo stability, no CPP has been approved by the Food and Drug Administration so far. Thus, further efforts are urgently needed to solve these problems. In this commentary, we discuss the current state and future directions of CPPs in the field of cancer therapy.
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