Brand/Development Name: Tasigna
Company(ies): Novartis
Principal Therapy Area: Cancer
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Taken twice daily (bid), nilotinib works by inhibiting the proliferation of cells containing an abnormal chromosome. It does this by targeting the production of the KIT, PDGFR, and Bcr-Abl proteins, the latter of which is only produced by cells containing the abnormal Philadelphia chromosome. This protein is recognised as the key cause and driver of the overproduction of cancer-causing white blood cells in patients with Philadelphia chromosome-positive (Ph+) chronic myeloid leukaemia (CML).
Applying experience gained from the development of Glivec/Gleevec (imatinib), Novartis created the next-generation tyrosine kinase inhibitor, nilotinib, in August 2002, just one year after the launch of imatinib. Nilotinib was developed for patients intolerant of and/or resistant to imatinib. The drug was designed to target the Bcr-Abl protein more preferentially than imatinib without adding new mechanisms of action. In preclinical studies, it was able to overcome resistance resulting from Bcr-Abl kinase mutations in 32 out of 33 cell lines commonly associated with Ph+ CML. Patients with a variety of these mutations also responded to treatment with nilotinib.
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