What is the mechanism of action of Imatinib?

ImatinibIs a kinase inhibitor used alone or with other drugs to treat different types of cancer or bone marrow diseases. It prevents or stops the growth of cancer cells and is called an anti-tumor (cancer) agent. What is the mechanism of action of Imatinib(Imatinib)?

Imatinib mesylate is a protein tyrosine kinase inhibitor that inhibits BCR-ABLtyrosine kinase, a constitutively abnormal tyrosine kinase produced by CMLPhiladelphia chromosome abnormalities. Imatinib inhibits proliferation and induces apoptosis in BCR-ABL-positive cell lines as well as fresh leukemia cells from Philadelphia chromosome-positive chronic myelogenous leukemia. Imatinib inhibits colony formation ex vivo in peripheral blood and bone marrow samples of chronic myeloid patients. Imatinib inhibits tumor growth in vivo in BCR-ABL-transfected murine bone marrow cells and BCR-ABL-positive leukemia cell lines from blastic CML patients. Imatinib is also an inhibitor of platelet-derived growth factor (PDGF) and stem cell factor (SCF) c-kit receptor tyrosine kinases and inhibits PDGF- and SCF-mediated cellular events.

Imatinib is well absorbed after oral administration and reaches Cmax within 2-4 hours after administration. The average absolute bioavailability is 98%. The mean AUC of imatinib increased proportionally with increasing doses from 25 mg to 1000 mg. There is no significant change in the pharmacokinetics of imatinib after repeated administration. When imatinib mesylate tablets are administered once daily, the accumulation at steady state is 1.5-2.5 times. At clinically relevant concentrations of imatinib, the binding rate to plasma proteins in in vitro experiments is approximately 95%, mainly binding to albumin and α1-acid glycoprotein. IndiaThe retail price of NATCOpharmaceuticals100mg120 tablets is about 400. IndiaCiplaPharmaceutical retail price per box100mg10 capsules40yuan. If you want to get more high-quality information, you can contact Yaode, and Yaode will do its best to learn more about high-quality overseas drugs for you.

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