Imatinib Mesylate is a tyrosine kinase inhibitor used primarily in cancer research studies focused on leukemia. Chronic Myeloid Leukemia (CML) cells contain a hybrid tyrosine kinase BCR/ABL that works to provide the cancer cell with ATP at an uncontrolled rate. Imatinib Mesylate inhibits this protein to slow cell growth and promote apoptosis.
Imatinib was invented in the early 1990s by scientists at Ciba-Geigy (which later merged with Sandoz to become Novartis in 1996).
Imatinib Mesylate is freely soluble in water.
| Mechanism of Action |
Imatinib Mesylate binds to the ATP binding site of the BCR/ABL tyrosine kinase. This enzyme is the constitutive abnormal tyrosine kinase created by the Philadelphia chromosome abnormality in chronic myeloid leukemia (CML). Imatinib is a small molecule inhibitor targeting multiple tyrosine kinases. Imatinib is a Bcr-Abl Tyrosine Kinase Inhibitor, Cytochrome P450 3A4 Inhibitor, and Cytochrome P450 2D6 Inhibitor. |
| Molecular Formula | C29H31N7O•CH3SO3H |
| References |
Goldman JM and Melo JV (2003) Chronic myeloid leukemia — Advances in biology and new approaches to treatment. New England J. of Med. 349(15):1451-1464 Mohamed AN, Pemberton P, Zonder J, Schiffer CA. The effect of imatinib mesylate on patients with Philadelphia chromosome-positive chronic myeloid leukemia with secondary chromosomal aberrations. Clin Cancer Res. 2003 Apr;9(4):1333-7 PMID 12684401 |
