Citronellal, known as rhodinal, is a naturally occurring monoterpenoid aldehyde distinctly found in the distilled oils of Cymbopogon species including C. marginatus, C. citratus, C. validus and C. winterianus family Gramineae. It is also obtained from eucalyptus, mentha, melissa, cinnamomum and allium. It is traditionally used in air freshener, cleaner, floor polishing, deodorants, moisturizing hand/body lotion, perfumes, and adhesives due to its lemon characteristic fragrance and therapeutic benefits. This study aimed to summarize the pharmacological activities and underlying mechanisms of citronellal against different diseases, as well as its toxicological profile. The data was collected from various reliable and authentic literatures by searching different academic search engines, including PubMed, Springer Link, Scopus, Wiley Online, Web of Science, ScienceDirect, and Google Scholar. The findings imply that citronellal demonstrated several pharmacological effects in various preclinical and pharmacological experimental systems. The results indicated that citronellal demonstrated antioxidant, anti‐inflammatory, antibacterial, antifungal, anthelminthic, and anticancer effects with beneficial effects in neurological and cardiovascular diseases. Our findings also indicated the toxic level of the phytochemical. In conclusion, it has been proposed that citronellal has the capability to serve as a hopeful therapeutic agent, so further extensive clinical research is necessary to develop it as a reliable drug.