Cancer is still considered one of the most serious diseases threatening human life. In the past three decades, there enormous efforts have been undertaken to confront cancer diseases. Within such efforts, many therapeutic agents have been developed to treat cancer patients in their early, as well as late cancer-developing stages. These agents vary from antibiotics, chemically synthesized compounds, and natural products-based drugs. Proteins, peptides, and amino acids have been implicated in preventing the development of different types of cancer. For this, this review focuses on the reports regarding peptide compounds showing their biological activity especially as anti-cancer agents.For example: Bleomycin, Cryptophycin and its analogues, Bombesin, Bradykinin and prophyrin family.