Background: Piperine, an active constituent isolated from Piper nigrum, Piper chaba, Piper sarmentosum, Piper guineense and Piper longum which is used to cure a variety of ailments related to lung, stomach, colon, skin etc. like Alzheimer’s, Parkinson’s disease, ulcerative colitis, cancer, arthritis, inflammatory bowel diseases, diabetes etc. Objective: The objective of the review is to study the synergistic effect of piperine specially in cancer. Methods: Patents and current literature mainly emphasizing the synergistic effect of piperine along with other drugs, especially anticancer drugs was reviewed keeping in mind the scientific novelty and impact. Results: Several synergistic combinations of piperine were explored which can be beneficial for the pharmaceutical industry. Conclusion: This review will assist the researchers in the preparation of novel formulations with improved efficacy cutting the cost of developing new drug molecules.