The study investigated the toxic effects of ethanol, aqueous, and hexane extracts of Calotropis procera Ait on Aedes aegypti (L) larvae. Leaf samples were collected in Riyadh, and then transported to the Department of Biology at the College of Science, Imam Mohammad Ibn Saud Islamic University, where they were manually cleaned and dried at room temperature in the shade. A phytochemical screening was performed to identify the chemical components of the plant according to the AOAC (1990) guidelines. Bioassay tests were conducted in a controlled environment with a temperature of 27 ± 2 °C, relative humidity of 75–85%, and a 12-hour light/dark cycle. The larvicidal activity of the plant extracts was evaluated using the methodology recommended by WHO (1996). Lethal concentrations (LC50 and LC95) were determined through regression analysis to assess larval mortality within 24 hours. The phytochemical analysis revealed the presence of tannins, cardiac glycosides, flavonoids, phenols, alkaloids, and terpenoids, while steroids and saponins were absent. Based on LC50 and LC95 values, the hexane extract showed the highest larvicidal potential (0.00250 ppm), followed by the ethanol extract (0.00251 ppm) and the aqueous extract (0.0028 ppm). These results indicate that Calotropis procera possesses strong larvicidal properties and can be used as an eco-friendly alternative for the control of Aedes aegypti larvae.