Cancer is a multifaceted disease that occurs when cells proliferate and migrate in an uncontrolled and unregulated manner. The development of cancer is the result of the interaction of a number of factors, including genetic mutations, environmental factors and lifestyle habits. There are many pharmacological and natural compounds that can be used to prevent and/or treat cancer. Piperine, a naturally occurring compound with multiple therapeutic properties, is the primary bioactive component of black pepper ( Piper nigrum L.), a member of the Piperaceae plant family. In recent years, it has attracted much interest as a potentially useful agent for the preventive and curative management of cancer. Results from studies of human cancer cell lines and advanced animal tumour models suggest that there are multiple pathways by which piperine may affect cancer development and metastasis. This review examines the molecular and cellular mechanisms through which piperine exerts its effects on cancer formation and progression, as well as its potential effects on various types of cancer.