Drug intelligence / Profile preview

rotenone

Development stage
Unknown
Lead developer
Central Life Sciences
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Inhalation, Topical
01

Overview

Rotenone is a naturally occurring isoflavone compound extracted from the roots and stems of several tropical and subtropical plants in the Fabaceae family, such as Derris elliptica and Lonchocarpus species. It has been used since the 19th century as a botanical insecticide and piscicide for pest control in agriculture, home gardens, pet care (lice/tick control), and water body management to eradicate fish. Rotenone acts by inhibiting mitochondrial complex I (NADH: ubiquinone oxidoreductase) in the electron transport chain. This blocks electron transfer from iron-sulfur centers to ubiquinone (CoQ), disrupting ATP production and increasing reactive oxygen species that can damage cellular components[2][6][8]. Rotenone also inhibits microtubule assembly. In biomedical research, it is widely used to model Parkinson’s disease due to its neurotoxic effects on dopaminergic neurons[5][6][8]. Rotenone is highly toxic via oral or inhalation exposure; its use as a pesticide is restricted in many countries due to health concerns.

Other names
derrisderris rootcubé resinbarbascotuba root extract
02

Targets

ND1 (Mitochondrial electron transport chain complex I)

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