imatinib

Imatinib is a small molecule tyrosine kinase inhibitor used as an oral targeted therapy for various cancers and bone marrow disorders. It works by selectively inhibiting several tyrosine kinases including BCR-ABL (the fusion protein in Philadelphia chromosome-positive leukemias), c-KIT (CD117), and platelet-derived growth factor receptor (PDGF-R). By blocking these kinases' activity at their ATP-binding sites, imatinib prevents the proliferation of cancer cells that depend on these signaling pathways. Developed originally by Novartis and first approved in 2001 under the brand name Gleevec/Glivec, it revolutionized treatment for chronic myeloid leukemia (CML) and is also indicated for gastrointestinal stromal tumors (GIST), acute lymphoblastic leukemia with Philadelphia chromosome positivity (Ph+ ALL), dermatofibrosarcoma protuberans (DFSP), systemic mastocytosis (ASM), hypereosinophilic syndrome/chronic eosinophilic leukemia (HES/CEL), myelodysplastic/myeloproliferative diseases (MDS/MPD)[1][2][3][4][5].

Brand names

GleevecGlivecImkeldiCelonibEnlivenImatibMesylonibMitinabPlivatinibShantinib

Other names

imatinib mesylate