Apoptosis has revealed an essential function in the development or prevention of oncogenic transformation in the body; however, programmed cell death (PCD) must be tightly controlled since deregulated cell death is involved in the development of a large number of different pathologies. Apoptosis can be decreased in pathological states such as in cancer and autoimmunity or elevated such as in stroke, neurodegeneration, retinal cell death, myocardial and liver ischemia, inflammatory diseases such as sepsis, osteoarthritis (OA), rheumatoid arthritis (RA), and asthma. Different types of apoptotic inhibitors will be discussed in this chapter displaying their mechanism of action, which have been reported to be therapeutic targets for cell survival or at least limiting cell death. These inhibitors are classified according to their nature into natural antiapoptotic proteins that present mainly in the cell and synthetic small molecule inhibitors that are widely used to protect against overexpression of apoptosis mediators and, in turn, to prevent corresponding diseases.