This review article aims to present an overview regarding the volatile compounds in different scented species of Pelargonium and their biological activities, immunomodulatory activity, cytotoxic activity, high larvicidal activity and ethnopharmacological uses. Although the Pelargonium genus includes many species, we focused only on the scented ones, with the potential to be used in different domains. Pelargonium essential oil showed great properties as antioxidant activity, antibacterial activity (against K. pneumonie, S. aureus or E. coli strains) and antifungal activity (against many fungi including Candida sp.), the responsible compounds for these properties being tannins, flavones, flavonols, flavonoids, phenolic acids and coumarins. Due to the existence of bioactive constituents in the chemical composition of fresh leaves, roots, or flowers of Pelargonium sp. (such as monoterpenoid compounds–citronellol, geraniol, linalool, and flavonoids–myricetin, quercetin and kaempferol), this species is still valuable, the bio-compounds representing the base of innovative substitutes in food processing industry, nutraceuticals, or preventive human or veterinary medicine (substitute of antibiotics). Highlighting the volatile chemical composition and properties of this scented plant aims to rediscover it and to emphasize the vast spectrum of health-promoting constituents for a sustainable approach. Future research directions should point to the application of plant biotechnology with a significant role in conservation strategy and to stimulate commercial interest.