Purpose of Review <p><i>Boenninghausenia albiflora</i> (Hook.) Rchb. ex Meisn., a unique species within the Rutaceae family, has been acknowledged in Asian traditional medicine for its efficacy in treating infections, wounds, bleeding disorders, and vector-borne diseases. This review aims to compile existing knowledge regarding its ethnomedicinal applications, phytochemistry, and pharmacological characteristics to evaluate its therapeutic potential and significance for contemporary drug discovery.</p> Recent Findings <p>Phytochemical investigations indicate that <i>B. albiflora</i> is abundant in essential oils, alkaloids, flavonoids, phenolics, terpenoids, and coumarins, including suberosin, dehydrogeijerin, and murralongin. These compounds exhibit a variety of pharmacological effects. Experimental research has shown the plant to possess significant antioxidant activity (associated with phenolic acids and flavonoids), anti-inflammatory and anticancer properties (attributed to coumarins), as well as antibacterial effectiveness against both Gram-positive and Gram-negative bacteria. The plant also demonstrates antimalarial properties against both chloroquine-sensitive and resistant strains, hepatoprotective effects in vivo, and antidiabetic activity in alloxan-induced models. Furthermore, essential oils exhibit strong insecticidal and repellent characteristics, reinforcing its ethnoveterinary and pesticidal uses.</p> Summary <p><i>B. albiflora</i> is a valuable medicinal resource due to its extensive array of bioactive metabolites and confirmed pharmacological activities. Though classical uses are increasingly supported by experimental evidence, more pharmacological and clinical work must be done to establish safety, efficacy, and mechanism of action. Its potential applications include medicine, nutraceutical design, and eco-friendly pest control.</p>