S u m m a r yThis article presents multidirectional effects of capsaicin and its natural derivatives as well as natural and synthetic analogs in term of their therapeutic properties. Active agents present in various Capsicum genus plants exert analgesic, anti-inflammatory, antibacterial, antioxidant and gastroprotective effects. Furthermore, capsaicin positively influences the metabolism of lipids. Numerous research show that capsaicinoids inhibit proliferation and migration process of cancer cells, what makes them molecules of high interest in oncology. Among broad range of positive activities, we have focused only on those properties that have already found application in medicine or seemed to be the most probably used in the near future. Even if in low or single doses this compound has been reported successful in numerous therapies, the negative consequences of high doses or prolonged administration is also discussed in the review.