This course aims at furnishing the fundamental knowledge about the chemical-physical and toxicological properties, and utilization of the major classes of anticancer and antimicrobial drugs. A particular attention will be devoted to the comprehension of the mechanisms of action of the drugs at the molecular level, and of the relationships between their chemical structure and biological activity. Moreover, the course is addressed to the presentation and discussion of the pharmacokinetic, and pharmacokinetic/pharmacodynamic (PK/PD) characteristics of chemotherapeutic drugs with special regards to their spectrum of activity and clinical use.