Wattakaka volubilis (L.f.) Stapf, a substantial woody climber of the family Apocynaceae, is widely employed in numerous Ayurvedic formulations to treat leucoderma, asthma, tumors, urinary tract infections, piles, and inflammations. Traditionally, its leaves and entire plant are utilized to alleviate cough, severe cold, fever, rheumatic pain, rabies, snakebites, boils, abscesses, and ocular afflictions. Diverse chemical constituents, encompassing alkaloids, terpenes, amino acids, tannins, pregnane glycosides, flavonoids, and polyphenols, are present in the extracts from different plant parts such as bark, leaves, flowers, and fruits. These extracts exhibit a wide array of pharmacological properties, including anticancer, larvicidal, anti-leishmanial, chondroprotective, and anthelmintic activities. However, for thorough validation, well-designed in vivo and clinical trials are imperative to substantiate its immense medicinal potential. The current investigation aims to deliver a comprehensive review of the bioactive compounds and pharmacological attributes of this plant.