Arsenic is a well-known carcinogen that contributes to the progression of multiple cancers and has recently been reported to be one of the most effective new anticancer agents in the treatment of various cancer types, together with acute promyelocytic leukemia (APL) as well as other solid tumors. However, the effect of arsenic and its compoundson different metabolic processes are still unknown. In cancer therapy, the advancement of arsenic trioxide in the treatment of different cancers has a unique history. The glorious past of arsenic and its different forms with a significant focus on arsenic trioxide as a therapeutic approach along with the mode of action, pathogenicity, pharmacokinetics, health hazards, current clinical studies of arsenic trioxide is illustrated in this study.Besides, how arsenic strengthens its deleterious effects and how it can effectively contribute to new therapeutic developments must also be understood.Therefore an urgent need for a deeper understanding of arsenic's contradictory effect, which could have the potential to be an effective medication for different kinds of cancers. In this review, we emphasized its selective channels that would have been beneficial in focusing attention over its real role in terms of toxicity as well as potential medications for the treatment of various forms of cancer.