Clerodendrum volubile is an underutilized leafy vegetable consumed in some parts of Nigeria. The interest in C. volubile has continued to increase due to its multipurpose values, including traditional uses, nutritional properties, and some therapeutic potentials; however, the pharmacological prospects of the plant are yet to be fully explored. Therefore, in the present review, different databases such as PubMed, Scopus, Web of Science, Google Scholar, etc. were explored to retrieve publications used to write this review. The pharmacological potentials of C. volubile, such as anticancer, antioxidant, antiviral, antimicrobial, anti-inflammatory, hepatoprotective, antidiabetic, and anti-hypertensive properties, were highlighted. The toxicological potential of the plant is also discussed. Proposed mechanisms that underline its biological activities include modulation of redox homeostasis, leading to decreased oxidative stress; down-regulation of matrix metalloproteinase-9 (MMP-9) expression; inhibition of key enzymes implicated in diabetes mellitus, hypertension, and neurological diseases; and inhibition of oxidative burst and inflammatory cytokines. Furthermore, the prospect of endophytes from C. volubile as a bioresource to produce novel therapeutic agents, as well as the development of nanotherapeutics from the plant extracts and its phytoconstituents, are discussed. In conclusion, C. volubile possesses an enormous number of possible pharmacological properties and therapeutic potentials waiting to be explored.