By controlling mitochondrial membrane permeability, the Bcl-2 family of proteins plays a crucial role in the regulation of cell death. Members of this family are functionally categorized as either pro- or anti-apoptotic based on their ability to promote or inhibit mitochondrial-dependent cell death signals. The critical role of Bcl-2 family proteins in human diseases has made them the focus of intense research by the pharmaceutical industry and academia. Anti-apoptotic Bcl-2 homologues have been widely explored as potential therapeutic targets for anticancer therapy through the development of nucleic-acid and peptide-based inhibitory molecules. Recently, strategies for the development of peptides or polypeptides derived from specific Bcl-2 family members have also been devised. This paper provides a brief review of the most recent patents that have been published relating to this area.