Nilotinib (Tasigna)
Nilotinib is a second generation tyrosine kinase inhibitor, 30-
fold more potent than Imatinib and more selective for the
BCR-ABL moeity than Imatinib.
fold more potent than Imatinib and more selective for the
BCR-ABL moeity than Imatinib.
- Nilotinib was approved for use by the FDA in Gleevec-
resistant patients in 2007 in the US. It is manufactured
by Novartis. - The Phase II Nilotinib data for Gleevec-resistant
patients has been impressive. Out of 321 patients who
were Gleevec-resistant or intolerant, 206 patients did
not have complete hematologic remission at the start of
Nilotinib therapy. However, after start of therapy, 77%
of these patients had a complete hematologic remission
on Nilotinib. - The incidence of major cytogenetic remission was 57%
with 41% of patients reaching complete cytogenetic
remission (CCR). - 84% of patients maintained MCR at 18 months and the
survival at this time point was 91%. - Nilotinib 400mg twice a day was well tolerated. Rash,
diarrhea and headache were frequent side-effects. Low
neutrophil counts, low platelet counts and elevated
serum lipase levels were some of the other side-effects. - In a newly diagnosed trial of 35 patients on 400mg
twice a day Nilotinib, 100% of patients achieved CCR
in 12 months and 45% of patients achieved a major
molecular response (MMR) at 12 months. - In another study of PK levels of Nilotinib, Chinese
patients were found to have similar levels of Nilotinib
concentrations as Caucasian patients.
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