C ancer therapy is a complex process. It can be physical (radiotherapy) or chemical (chemotherapy), as well as psychological. Chemotherapy has only been partially successful due to its highly toxic nature, although .many lives have been able to be saved using these drugs, but not without severe side effects. For several years scientists have been performing a considerable amount of studies in order to try to understand the roles of the endocannabinoid system (ECS) and its concern in physiological and pathophysiological processes. [1] On the other hand, there are many research groups in the world working on the new pharmacological tools for cancer treatment. Cannabinoids and endocannabinoids constitute one of the newest subject of interest on this topic, since ∆ 9-THC was shown to present an interesting antineoplastic action [2] and the following finding of the same activity of endocannabinoids. [3] One Cancer is a complex pathophysiological condition that produces an important number of death around the world. At present, there are different ways to treat cancer: chemotherapy, radiotherapy and surgery. Cancer chemotherapy used today in many cases is effective, but it is very toxic too. The endocannabinoid system is implicated in a variety of physiological and pathological processes, including cancer. Many studies have shown, since 1975, that both phytocannabinoids Δ9-tetrahydrocannabinol (THC) and cannabidiol (CBD) offer an antioneoplastic activity. Latter, other researchers have displayed that endocannabinoids as anandamide (ANA) and 2-arachidonoylglycerol (2-AG) also present the same potential activity. Phytocannabinoids and endocannabinoids act through CB1 and CB2 receptors to produce that effect. However, THC-the main phytocannabinoid presenting anticancer action-as well as anandamide employed in pharmacological doses, produce important phycotropic effects, but these cannabinoid compounds do not produce major adverse reactions like conventional antineoplastic drugs. On this basis, scientists have to develop analogs or derivatives of cannabinoids/endocannabinoids that cannot induce psychotropic effects. It is important to study more deeply chronopharmacological aspects of cannabinoids/endocannabinoids in cancer therapy, although some is known today.