Imatinib mesylate, marketed under the brand name Gleevec, is a tyrosine kinase inhibitor (TKI) and represents a landmark breakthrough in the treatment of CML. Its development revolutionized cancer therapy by introducing the concept of targeted therapy, specifically addressing the molecular abnormalities driving the disease.
Imatinib binds to the ATP-binding site of the BCR::ABL1 tyrosine kinase. By occupying the ATP-binding site, imatinib competitively inhibits the kinase activity of the mutated protein, preventing the phosphorylation of downstream substrates. This inhibition disrupts the signaling pathways that promote cell division and survival, leading to the reduction of leukemic cell proliferation and promoting apoptosis.
3. “Mechanism Imatinib.svg.” Wikimedia Commons, https://commons.wikimedia.org/wiki/File:Mechanism_imatinib.svg.
