Knowra Imatinib Imatinib Imatinib is an oral targeted anticancer drug that inhibits several tyrosine kinases, especially BCR::ABL1 and KIT. It transformed treatment of chronic myeloid leukemia and is also used for gastrointestinal stromal tumors.
BCR::ABL1 : A fusion tyrosine kinase produced by the Philadelphia chromosome, which drives most chronic myeloid leukemia. Imatinib suppresses this kinase, the principal molecular target behind its use in chronic myeloid leukemia.
Chronic myeloid leukemia : A blood cancer in which abnormal hematopoietic stem cells produce excessive myeloid cells, usually driven by BCR::ABL1. Imatinib became a standard treatment by suppressing the kinase that drives this leukemia.
Brian Druker : An American physician-scientist whose research helped establish imatinib as a treatment for chronic myeloid leukemia. Druker connected BCR::ABL1 inhibition to clinical benefit and led pivotal studies of imatinib.
Interferon alfa : A cytokine-based therapy formerly used to treat chronic myeloid leukemia and other diseases. Before imatinib, interferon alfa was a major nonsurgical treatment for chronic-phase disease.
KIT : A receptor tyrosine kinase that regulates cell survival and growth and is often mutated in gastrointestinal stromal tumors. Imatinib inhibits KIT, including mutant forms that drive many gastrointestinal stromal tumors.
Gastrointestinal stromal tumor : A mesenchymal tumor of the digestive tract, commonly driven by mutations in KIT or PDGFRA. Imatinib treats many advanced and resected tumors by inhibiting their activating kinase mutations.
Nicholas Lydon : A medicinal chemist who contributed to the development of imatinib and other kinase inhibitors. Lydon’s work at Ciba-Geigy helped identify and optimize the compound that became imatinib.
Dasatinib : A BCR::ABL1 and SRC-family kinase inhibitor used to treat chronic myeloid leukemia and some acute lymphoblastic leukemias. This later-generation inhibitor can act against several imatinib-resistant BCR::ABL1 variants.
Platelet-derived growth factor receptor : A family of receptor tyrosine kinases involved in cell growth, development, and tissue repair. Imatinib also blocks PDGF receptors, accounting for activity in several less common tumors.
Philadelphia chromosome : An abnormal chromosome formed by a translocation between chromosomes 9 and 22, creating the BCR::ABL1 fusion gene. This chromosome identifies the molecular lesion that made imatinib a targeted treatment for chronic myeloid leukemia.
Show all 22