Meldonium has attracted considerable attention in sports due to its suggested effects on energy metabolism and high-profile doping cases. This narrative review evaluates Meldonium's biochemical mechanisms, pharmacokinetics, safety profile, and the quality of evidence surrounding its use in athletes. While Western literature categorizes Meldonium as a metabolic modulator, Eastern literature often classifies it as an antihypoxic agent. By inhibiting carnitine biosynthesis, Meldonium shifts substrate utilization from fatty acid oxidation toward more oxygen-efficient glucose metabolism. However, despite its widespread use and inclusion on the World Anti-Doping Agency (WADA) prohibited list, there remains a profound lack of high-quality, randomized placebo-controlled trials demonstrating consistent ergogenic benefits in healthy athletes. Existing human performance studies exhibit a high risk of bias and methodological flaws. This review provides a critical appraisal of the current literature, highlighting the physiological trade-offs of Meldonium use and emphasizing the need for rigorous clinical trials to determine its genuine impact on athletic performance and long-term safety. This comprehensive review aims to clarify Meldonium's pharmacological profile, inform athlete health considerations, and guide future research into its legitimate clinical and sports applications.