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Fumitremorgin C (FTC) is a naturally occurring indolyldiketopiperazinyl mycotoxin isolated from the fungus *Aspergillus fumigatus*. It is a potent and highly selective inhibitor of the ATP-binding cassette superfamily G member 2 (ABCG2), also known as the breast cancer resistance protein (BCRP). By inhibiting this efflux transporter, fumitremorgin C can reverse multidrug resistance in various cancer cell lines, including breast and colon cancers, by preventing the extrusion of chemotherapeutic agents. Despite its efficacy in vitro, fumitremorgin C is not suitable for clinical use due to significant neurotoxic side effects, specifically the induction of tremors at low doses. It remains a critical research tool for studying BCRP-mediated resistance mechanisms and has served as a structural template for the development of more potent and less toxic synthetic analogs such as Ko143.
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