Dasatinib/Startacel is the first generation of targeted drugs

In the development of targeted therapy for leukemia, dasatinib is generally classified as a second-generation tyrosine kinase inhibitor. To understand this positioning, we need to start with the evolutionary background of targeted therapy for chronic myelogenous leukemia (CML). The first generation of targeted drugs, represented by imatinib, achieved precise inhibition of BCR-ABL fusion protein for the first time, completely changing the treatment model of CML.

With the extension of clinical application time, some patients have developed resistance or insufficient efficacy to the first-generation drugs, which directly promotes the development of second-generation targeted drugs. It was against this background that dasatinib came out. It is characterized by its stronger and broader inhibitory ability against BCR-ABL kinase and its ability to cover a variety of imatinib resistance-related mutation sites. This is also an important reason why it is positioned as a second-generation targeted drug.

Judging from the consensus of guidelines and academic literature, second-generation targeted drugs are not just “more effective”, but play a key role in drug resistance management and personalized treatment. Dasatinib is considered an important treatment option in chronic-phase and accelerated-phase CML, as well as in some acute lymphoblastic leukemias. Its intergenerational positioning also means that in terms of treatment strategies, it is often used in first-line or sequential treatment after imatinib failure.

It should be pointed out that the "generation" of targeted drugs is not a simple ranking of advantages and disadvantages, but reflects its research and development background and applicable population. With the emergence of third-generation targeted drugs, treatment options have become more diverse, but dasatinib, as a classic second-generation targeted drug, still occupies an important position in the global hematological cancer treatment system. Its intergenerational nature also provides a clear logical framework for doctors to formulate long-term treatment plans.

Reference materials:https://www.ema.europa.eu/en/medicines/human/EPAR/sprycel