What type of targeted drug does Imatinib (Gleevec) belong to?

Imatinib, trade name Gleevec, is a tyrosine kinase inhibitor (TKI) and belongs to the first generation of targeted drugs. Its main mechanism of action is to inhibit the tyrosine kinase activity of BCR-ABL fusion protein, thereby blocking abnormal signaling of malignant cells and inhibiting the proliferation and survival of tumor cells. This drug was originally used to treat chronic myelogenous leukemia (CML). It was the first targeted therapy drug successfully launched in human history, ushering in a new era of "precision treatment".

The most classic indication for imatinib is patients with Philadelphia chromosome-positive CML. The BCR-ABL fusion gene plays a driving role in this leukemia, and imatinib, by precisely targeting the tyrosine kinase encoded by this disease-causing gene, significantly extends the survival of patients and transforms CML from a "terminal disease" in the past into a chronic disease that can be controlled in the long term. In addition, imatinib is approved for the treatment of gastrointestinal stromal tumors (GIST) and other tumors expressing c-KIT or PDGFRA mutations.

In gastrointestinal stromal tumors, imatinib effectively blocks the signaling pathways of tumor cells by inhibiting the activity of oncogenic mutated tyrosine kinases such as c-KIT or PDGFRA, thereby controlling tumor progression. It is suitable for adjuvant treatment after GIST surgery and also for advanced cases that are inoperable or have metastasized. Imatinib's broad-spectrum targeting mechanism has shown potential in multiple cancer types and has been widely studied for use in other rare tumor types.
Overall, imatinib is a milestone in the history of targeted drug development. Its precise mechanism, good oral tolerance and long-term efficacy make it a core drug in the standard treatment plan for multiple cancer types. With the advent of second- and third-generation TKIs, imatinib has been gradually replaced in some drug-resistant or mutated populations, but it is still one of the first-choice drugs in the vast majority of newly treated patients.
Reference: https://www.gleevec.com/