With the beginning of the 21st century, a new and exciting era for cancer therapy has begun with the appearance of molecular targeted drugs. Numerous drugs for chemotherapy have been discovered following careful screening of natural and synthetic components. After screening, candidate chemotherapy drugs are examined to determine if they have sufficiently cytotoxic to function as an anti-tumor therapeutic. However, the development of molecular targeted drugs is based on more logical methodologies. First, the target is determined then a search is conducted for molecules able to inhibit the target molecule. Some molecular targeting drugs, such as Glivec (Imatinib, STI571), have shown amazing effects when compared to currently used chemotherapy drugs, whereas few others have completely failed to inhibit tumor development in clinical trials. Thus, an efficient method for finding effective molecular targeted drugs is needed. An important question is whether the target molecule is responsible for tumor growth or metastasis. In addition, the clinical administration schedule must be suitable for the component used. The drugs will not be completely successful in clinical trials if any of the key points are overlooked. Translational studies are necessary for a complete evaluation of molecular targeted drugs and, based on the results observed in clinical applications, the testers must return to their basic laboratory if necessary and improve the drugs for more advanced therapy. In this review we discuss on the current and future status of molecular target drugs.