Garcinia cambogia (Family: guttiferae), commonly referred to as Malabar tamarind, is a tropical species widely distributed across South and Southeast Asia and traditionally valued for its culinary and therapeutic properties. The fruit rind of this plant is a rich source of diverse bioactive metabolites, predominantly hydroxycitric acid (HCA), along with garcinol, xanthones, benzophenones, flavonoids, and phenolic compounds. HCA, the principal phytoconstituent, acts as a competitive inhibitor of adenosine triphosphate-citrate lyase, thereby regulating lipid biosynthesis, suppressing appetite, and enhancing energy metabolism. Comprehensive phytochemical analyses have revealed the presence of alkaloids, saponins, tannins, flavonoids, terpenoids, and glycosides, conferring potent antioxidant, anti-inflammatory, antidiabetic, and antimicrobial activities. Pharmacological investigations have established the plant’s potential in weight management, metabolic regulation, hepatoprotection, and mood modulation through serotonergic pathways. Toxicological assessments affirm its safety at therapeutic concentrations, although excessive or prolonged consumption may result in hepatic alterations. Advanced analytical approaches such as High-Performance Liquid Chromatography (HPLC), Gas Chromatography–Mass Spectrometry (GC–MS), and Thin Layer Chromatography (TLC) are employed for qualitative and quantitative standardization of its active constituents. Collectively, Garcinia cambogia stands as a phytopharmaceutical of significant scientific interest, embodying a broad spectrum of pharmacological benefits and offering valuable prospects for further exploration in modern evidence-based medicine.