Caspases are a proteases with a conserved cysteine residue at their active site. There enzymes cleave their substrates after an aspartate residue. They have role in various cellular processes, including apoptosis, differentiation and inflammatory responses. Twelve caspases have been identified in humans and are divided into two groups, caspases involved in the process of apoptosis and caspases involved in inflammatory response. Caspases participating in apoptosis are divided into caspases initiators and caspases effectors. Even though, caspases have an effect on many cellular processes, when it comes to tumors, caspases are most commonly associated with apoptosis, having the crucial role inthe execution of cell death. Tumors are caused by uncontrollable cell proliferation, which is usually a result of the loss of cell death control. This results in the survival of tumor cells and, ultimately, tumor metastasis. Current research is directed to caspases as target molecules in cancer treatment or to the regulation of their activity in order to increase apoptosis in tumor cells. Caspase inhibitor or activator can affect the cell fate, survival or its death. The goal is to find a drug with as little side effects as possible and without affecting the healthy cells.