 The purpose of this paper is to summarise mode of action of cisplatin on the tumour cells, a brief outlook on the metallocene compounds as anti-tumour 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 anti-tumour immune response was evaluated. Furthermore, herein are summarised some metallocenes, titanocene, vanadocene, molybdocene, ferocene and zirconocene, with high anti-tumour activity. This article was authored by Santiago Gomez-Ruiz, Daniella Maximovich Ivanovich, Sandra Majotovic and others.