Imatinib

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Imatinib (“Gleevec” or “Glivec”), is a 2-phenyl amino pyrimidine derivative. It can be classified as tyrosine kinase inhibitor (TKI)[1]. This protein has revolutionized the treatment of chronic myeloid leukemia (CML) in 2001.

Clinical Pharmacology

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[2].

Clinical implications

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)[3]. It is a chemotherapy drug that works by slowing or stopping the growth of cancer cells.

References

  1. Cancer Research UK, Imatinib(Glivec) [Available at]:https://www.cancerresearchuk.org/about-cancer/cancer-in-general/treatment/cancer-drugs/drugs/imatinib
  2. Iqbal, N., & 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/
  3. 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/
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