Introduction and objective: Neoplastic diseases are a common cause of death, especially in developed countries. Various methods are used in cancer therapy including natural substances. Terpenes and terpenoids play a special role, including betulin and betulinic acid with the pentacyclic structure of lupane. They have a wide range of pharmacological activity, among which anti-cancer activity attracts the greatest attention. Abbreviated description of the state of knowledge: he review discusses the pharmacological effects of betulin and its derivatives on tumours, and focuses on the potential of its application in the treatment of melanoma. The review study also presents future prospects for the use of this natural substance. Betulin and its derivatives have the ability to influence the processes of apoptosis, angiogenesis and autophagy. Additionally, they have the ability to sensitize, increasing the sensitivity to commonly used methods of cancer treatment. To-date, numerous studies have been carried out on the synthesis of betulinic acid derivatives, which would show greater polarity and activity compared to the starting compound. Due to their greater bioavailability, the modified compounds showed a stronger anti-tumour effect. Conclusion: The results of the above-mentioned studies confirm the anti-cancer properties of betulin. Regarding melanoma, betulin shows significant therapeutic efficacy. This gives new perspectives for the treatment of the most dangerous skin cancer.