Anticancer drug development is growing complexity and multi-factorials, which demands robust drug evaluative architecture in experimental and preclinical studies. To increase the number of drug licensing, biochemical, pharmacological, technical and economic changes (balance and integration) in evaluative systems should be focused in world labs. Despite a great progress, treatment breakthroughs and drug industry need new minds and more competitive technology (new generation of in vitro test systems) were emerging in the past. Overall, drug evaluative systems consisted half of anticancer drug development and licensing (medicinal chemistry and pharmacology in total) from initial screening to clinical validity. Its advances greatly impact the outcomes of drug production (rates of final drug licensing and efficacy of therapeutics in the clinic). In this regards, creative ideas and new techniques will change the norm and convention of drug screening and mechanic exploration in the future. This article provides multi-disciplinary approaches for experimental and preclinical anticancer drug evaluations, selections and combinations (chemistry and biomedicine). Future trends for drug evaluative systems are especially highlighted in depth, multilateral and multidisciplinary.