What is the target of Imatinib?

Imatinib is a tyrosine kinase inhibitor used to treat various leukemias, myelodysplastic, myeloproliferative diseases, systemic mastocytosis, eosinophilic syndrome, dermatofibrosarcoma protuberans and gastrointestinal stromal tumor. Imatinib is a small molecule inhibitor of tyrosine kinases such as CSF1R, CSF1R, ABL, c-KIT, FLT3, and PDGFR-β.

Imatinib binds to theBCR-ABLkinase domain by preventing the transfer of phosphate groups on protein substrates to tyrosine and subsequently activating the phosphorylated protein. As a result, the transmission of proliferative signals to the nucleus is blocked and leukemia cell apoptosis is induced. Imatinib is rapidly absorbed when administered orally and has very high bioavailability (98% of an oral dose reaches the bloodstream). The metabolism of imatinib occurs in the liver and is regulated by the cytochrome P450 system of several isoenzymes, including to a lesser extent CYP3A4, CY P1A2, CYP2D6, CYP2C9, CYP2C19. Its main metabolite"Ndesmethylpiperazine derivative" is also very active. The main routes of elimination are in bile and feces, only a small portion of the drug is excreted in urine. Most imatinib is eliminated as a metabolite, only 25% is eliminated in an unchanged form. The respective half-lives of imatinib and its major metabolite are 18 to 40 hours. 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.