Rationale. Piper betle of the family of Piperaceae, (P. betle) is a liana growing in the tropics of the Indonesian-Asian region, has long been actively used in folk medicine as a source of remedies for a variety of health problems. At the same time, the methods and purposes of using P. betle in folk medicine vary from region to region, and the effectiveness of its impact on human remains fully underestimated. The aim of the study. To systematize and analyze modern literature data on the pharmacological potential of the medicinal plant Piper betle, growing in the countries of Madagascar, India, Bali and China of the Indonesian-Asian region. Materials and methods. The search and analysis of data were carried out in international and regional databases (PubMed, Scopus, Web of Science, Science Direct, and Google Scholar) for the period from 1996 to 2025. Results. The analysis of scientific literature data showed that the target fragment of metabolome (TFM) of Peper betle is characterized by a complex composition of biologically active compounds (BAS), which varies significantly from region to region. BAS of the TFM of this plant are responsible for various types of pharmacological activity, which justifies its use in traditional medicine and growing interest to the medical scientific community. It was found that within the range of P. betle growth, the chemical composition of TFM varies in terms of the content of alkaloids, terpenes, phenolic compounds, including flavonoids and volatile components. Conclusion. P. betle is a promising object for further research in the field of phytopharmacology and reproductive medicine. Obviously, in-depth preclinical and clinical studies are needed to confirm the identified effects based on literature sources. At the same time, the collected literature data can contribute to future research in the field of pharmacology in order to create new promising drugs. © 2025, Scientific Centre for Family Health and Human Reproduction Problems. All rights reserved.