 The purpose of this paper is to summarize mode of action of susplating on the tumor cells, a brief outlook on the metallocene compounds as anti-tumor drugs as well as the future tendencies for the use of the latter in anti-cancer chemotherapy. Molecular mechanisms of susplating interaction with DNA, DNA repair mechanisms and cellular proteins are discussed. Molecular background of the sensitivity and resistance to susplating, as well as its influence on the efficacy of the anti-tumor immune response was evaluated. Furthermore, herein are summarized some metallocenes, titanocene, vanadocene, molybdocene, ferocene, and zirconocene with high anti-tumor activity. This article was offered by Santiago Gomez Ruiz, Daniela Maximovich Ivanovich, Sanjim Mijitovic, and others.