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Review
. 2022 Jan 2;10(1):1965418.
doi: 10.1080/21688370.2021.1965418. Epub 2021 Aug 17.

Cell-penetrating peptides improve pharmacokinetics and pharmacodynamics of anticancer drugs

Izabela Rusiecka  1 , Iwona Gągało  1 , Ivan Kocić  1
Affiliations
Review

Cell-penetrating peptides improve pharmacokinetics and pharmacodynamics of anticancer drugs

Izabela Rusiecka et al. Tissue Barriers. .

Abstract

This review concentrates on the research concerning conjugates of anticancer drugs with versatile cell-penetrating peptides (CPPs). For a better insight into the relationship between the components of the constructs, it starts with the characteristic of the peptides and considers its following aspects: mechanisms of cellular internalization, interaction with cancer-modified membranes, selectivity against tumor tissue. Also, CPPs with anticancer activity have been distinguished and summarized with their mechanisms of action. With respect to the conjugates, the preclinical studies (in vitro, in vivo) indicated that they possess several merits in comparison to the parent drugs. They concerned not only better cellular internalization but also other improvements in pharmacokinetics (e.g. access to the brain tissue) and pharmacodynamics (e.g. overcoming drug resistance). The anticancer activity of the conjugates was usually superior to that of the unconjugated drug. Certain anticancer CPPs and conjugates entered clinical trials.

Keywords: CPP; anticancer CPPS; anticancer drugs; cell-penetrating peptides; clinical trials; conjugates; internalization; preclinical studies.

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Conflict of interest statement

No potential conflict of interest was reported by the author(s).

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