Imatinib (“Gleevec” or “Glivec”), is a 2-phenyl amino pyrimidine derivative. It can be classified as tyrosine kinase inhibitor (TKI). This protein has revolutionized the treatment of chronic myeloid leukemia (CML) in 2001.
The active sites of tyrosine kinases each have a binding site for ATP. The catalysed enzymatic activity, known as protein tyrosine phosphorylation is the transfer of a terminal phosphate from ATP to tyrosine residues on its substrates. Deregulation of tyrosine kinase activity has been shown to play a central role in the pathogenesis of human cancers.
Imatinib works by binding close to the ATP binding site, locking it in a closed conformation, therefore inhibiting the enzyme activity of the protein semi-competitively. This process ultimately prevents the occurrence of downstream signaling pathways which promote leukemogenesis.
This medication is used to treat certain types of cancer such as chronic myeloid leukaemia (CML) by Inhibiting at BCR-ABL gene on chromosome 22 (Philadelphia chromosome). It is a chemotherapy drug that works by slowing or stopping the growth of cancer cells.
- ↑ Cancer Research UK, Imatinib(Glivec) [Available at]:https://www.cancerresearchuk.org/about-cancer/cancer-in-general/treatment/cancer-drugs/drugs/imatinib
- ↑ Iqbal, N., &amp;amp;amp; Iqbal, N. (2014). Imatinib: a breakthrough of targeted therapy in cancer. Chemotherapy research and practice, 2014.[Available at]: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4055302/
- ↑ Kang, Z. J., Liu, Y. F., Xu, L. Z., Long, Z. J., Huang, D., Yang, Y., Liu, B., Feng, J. X., Pan, Y. J., Yan, J. S., … Liu, Q. (2016). The Philadelphia chromosome in leukemogenesis. Chinese journal of cancer, 35, 48. doi:10.1186/s40880-016-0108-0. [Available at]:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4896164/