Humanity has a longstanding reliance on natural plants for medicinal purposes, and Gymnema lactiferum (G. lactiferum) has emerged as a medicinal plant with deep‐rooted traditional usage. Throughout history, this plant has been an integral part of traditional medical systems, demonstrating diverse therapeutic effects. Notably, among these effects is its ability to decrease blood glucose concentration in diabetic patients, impart cooling effects, serve as an anabolic and rehydrating agent, stimulate spermiogenesis, and exhibit wormicidal properties. Furthermore, G. lactiferum has been used in treating conditions such as hemorrhoids cancers, anorexia, and as a cardiac stimulant. The primary objective of this review is to comprehensively gather and critically assess research findings regarding the medicinal properties of G. lactiferum, specifically emphasizing the bioactive compounds responsible for these properties. Previous studies have documented the presence of various phytochemicals in G. lactiferum, which are associated with some biological activities, including antioxidative, anti‐hyperglycemic, cholesterol‐regulating, and anti‐inflammatory properties. Additionally, this review explores potential future applications for this plant. Beyond its medicinal significance, extracts derived from G. lactiferum demonstrate promise for future nutritional applications. This review highlights the potential use of G. lactiferum as an herbal medicine by critically assessing research on its medicinal value.