Approved October 2007
chronic myelogenous leukemia
Cancer & Oncology
Tasigna (nilotinib hydrochloride monohydrate) is an orally available signal transduction inhibitor of the Bcr-Abl kinase, c-kit and Platelet Derived Growth Factor (PDGF), all of which play a role in cell proliferation, cell migration, and angiogenesis.
Tasigna is specifically indicated for the treatment of chronic phase and accelerated phase Philadelphia chromosome positive chronic myelogenous leukemia (CML) in adult patients resistant or intolerant to prior therapy that included imatinib.
Tasigna is supplied as a 400 mg tablet designed for oral administration. The recommended initial dose of the drug is 400 mg orally twice daily, at approximately 12 hour intervals. No food should be consumed at least two hours before and one hour after administration of Tasigna. Dose adjustments or modifications should be followed according to the label for subjects with ECGs with a QTc > 480 msec, for subjects with neutropenia and/or thrombocytopenia and for subjects with selected non-hematologic laboratory abnormalities. The concomitant use of strong CYP3A4 inhibitors and strong CYP3A4 inducers should be avoided.
FDA approval of Tasigna was based on the results of a clinical trial. This open-label, multi-center trial enrolled subjects with imatinib-resistant or -intolerant CML with separate cohorts for chronic phase (CML-CP) and accelerated phase (CML-AP) disease. Overall 280 CML-CP subjects with a minimum follow-up of 6 months and 105 CML-AP subjects with a minimum follow-up of 4 months were enrolled. The efficacy endpoint in the CML-CP arm was unconfirmed major cytogenetic response (MCyR) which included complete and partial cytogenetic responses. A major cytogenetic response was observed in 40% of the subjects. Complete response was observed in 28% and partial response was observed in 12% of this group. The efficacy endpoint in the CML-AP arm confirmed hematologic response (HR), defined as either a complete hematologic response (CHR) or no evidence of leukemia (NEL). A confirmed hematologic response was observed in 26%, with 18% showing a complete hematologic response and 8% showing no evidence of leukemia. Median duration of response had not been reached at this time for either group. However, based on current data, 59% of the CML-CP subjects with a major cytogenetic response had a duration of response of at least 6 months and 63% of CML-AP subjects with a confirmed hematologic response had a duration of response of at least 6 months.
Ongoing Study Commitments
Adverse events associated with the use of Tasigna in CML-CP patients may include, but are not limited to, the following:
Adverse events associated with the use of Tasigna in CML-AP patients may include, but are not limited to, the following:
Tasigna (nilotinib hydrochloride monohydrate) is an orally available signal transduction inhibitor of the Bcr-Abl kinase, c-kit and Platelet Derived Growth Factor (PDGF). Nilotinib binds to and stabilizes the inactive conformation of the kinase domain of Abl protein. In vitro, nilotinib inhibited Bcr-Abl mediated proliferation of murine leukemic cell lines and human cell lines derived from Ph+ CML patients. In vivo, nilotinib reduced the tumor size in a murine Bcr-Abl xenograft model.
For addiitonal information regarding tasigna or chronic myelogenous leukemia, please visit the Tasigna web page.
The Tasigna (nilotinib hydrochloride monohydrate) drug information shown above is licensed from Thomson CenterWatch. The information provided here is for general educational purposes only and does not constitute medical or pharmaceutical advice which should be sought from qualified medical and pharmaceutical advisers.