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RESEARCH PRODUCT

Identification of chemosensitizers by drug repurposing to enhance the efficacy of cancer therapy

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Abstract The progressively rising drug resistance has driven the development of chemosensitizers, which aim to enhance the current chemotherapeutic efficacy through either quantitatively increasing intracellular drug concentration by inhibiting drug efflux, vesicle sequestration, and metabolic inactivation or qualitatively exerting concomitant effects on cellular regulation to promote apoptosis. Given the high failure rates and costs during standard drug development, drug repurposing represents an effective and economic approach for chemosensitizer identification. By applying drug repurposing, a wide range of existing clinic drugs including anticardiovascular agents, immunosuppressants, antiinfectious agents, antipsychotic agents, antiinflammation agents, and anti-HIV agents, have been investigated for their property to enhance the efficacy of standard cytotoxic regimens. In this chapter, chemosensitizers inspired by drug repurposing and their functional mechanisms will be discussed in depth.