Hibiscus rosa-sinensis (H. rosa-sinensis) has been largely used in traditional medicine. This study aims to review the pharmacological and phytochemical properties of Hibiscus rosa-sinensis L and also summarize the pharmacological, photochemical, and toxicological characteristics of H. rosa-sinensis. The current review focuses on the distribution, chemical content, and main uses of H. rosa-sinensis. Various scientific databases, including ScienceDirect, Scopus, PubMed, Google Scholar, etc., were used. Correct plant names were verified from plantlist.org. The results were interpreted, analyzed, and documented based on bibliographic information. This plant has been frequently used in conventional medicine due to its high concentration of phytochemicals. All its parts contain numerous chemical compounds, such as flavonoids, tannins, terpenoids, anthocyanins, saponins, cyclopeptide alkaloids, and vitamins. More interestingly, the roots of this plant contain glycosides, tannins, phytosterols, fixed oils, fats, flavonoids, saponins, gums, and mucilages. The leaves contain alkaloids, glycosides, reducing sugars, fat, resin, and sterols. The stem contains other chemical compounds, such as ß-sitosterol, teraxeryl acetate, cyclic sterculic, and malvalic acids. Finally, the flowers contain riboflavin, thiamine, apigenidine, oxalic acid, citric acid, quercetin, niacin, pelargonidine, and ascorbic acid. This species has a wide variety of pharmacological applications, such as antimicrobial, antioxidant, antidiabetic, anti-inflammatory, antihypertensive, antifertility, antifungal, anticancer, hair growth-promoting, antihyperlipidemic, reproductive, neurobehavioral, antidepressant, and antipyretic activities. Finally, toxicological studies have shown that higher doses of extracts from the plant are safe.