Desmodium gangeticum (L.) DC., commonly known as "Salparni," is a prominent medicinal plant in the Fabaceae family, extensively utilized in traditional Ayurvedic and folk medicine systems across South and Southeast Asia. As a key ingredient of the classical Ayurvedic formulation Dashamoola, D. gangeticum is traditionally prescribed for fever, inflammation, respiratory, and nervous system disorders. The plant is characterized by a diverse phytochemical profile, including alkaloids, flavonoids, triterpenoids, sterols, and glycosides, which underpin its broad-spectrum pharmacological effects such as anti-inflammatory, antioxidant, hepatoprotective, antimicrobial, and anticancer activities. Despite its rich ethnomedical heritage, modern pharmaceutical research on D. gangeticum remains in early stages, with limited clinical validation and challenges related to poor aqueous solubility and bioavailability of its bioactive. Recent advances in extraction, standardization, and drug delivery—such as nano formulations, phytosomes, and targeted delivery systems—hold promise for enhancing its therapeutic efficacy and overcoming biopharmaceutical limitations. This review provides a comprehensive overview of the plant’s phytochemistry, extraction methods, pharmacological activities, and formulation strategies, while highlighting regulatory and safety considerations. It also identifies key research gaps and future directions, including the need for rigorous clinical trials, advanced drug delivery platforms, and integration of omics technologies to fully harness the therapeutic potential of D. gangeticum as a modern phytopharmaceutical.