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