The Leontopodium R.Br. ex Cass. taxa have been extensively phytochemically researched for their beneficial properties by the pharmaceuticals industry. These species have been used as remedies since ancient times, and their usage in traditional medicine has been a source of inspiration for current research. As a result, a comprehensive review study concerning the bioactivities of secondary metabolites belonging to Leontopodium species would be of great interest. Our research shows that the majority of studies addressed the anti-inflammatory activity, and the most studied compound was leoligin, a lignan with cardioprotective properties. The diverse range of bioactivities were intricately linked to the abundance of secondary metabolites, which conferred effective antimicrobial activity, antioxidant properties, the anti-neurodegenerative potential due to improvements in cholinergic transmission, the anti-tumour effects on various cancer cell lines, particularly breast and lung cancer, and the hypoglycaemic and hepatoprotective properties. All these important bioactivities also recommend Leontopodium taxa as a valuable source for the discovery of new drugs.