Nilotinib

Information about Nilotinib

Nilotinib is a selective tyrosine kinase receptor inhibitor used in the therapy of chronic myelogenous leukemia.

Liver safety of Nilotinib

Nilotinib therapy is associated with transient elevations in serum aminotransferase levels and rare instances of clinically apparent acute liver injury. 

Mechanism of action of Nilotinib

Nilotinib (nye loe' ti nib) is a selective inhibitor of the abnormal tyrosine kinase receptor known as bcr-abl, formed by the reciprocal translocation between chromosome 9 and 22, which creates the Philadelphia chromosome that is associated with chronic myelogenous leukemia (CML).  The bcr-abl tyrosine kinase receptor is constitutively expressed in leukemic cells and causes unregulated cell growth and proliferation.  Nilotinib is a specific inhibitor of bcr-abl and structurally related to imatinib.  Like imatinib, nilotinib also blocks the tyrosine kinase activity of the abnormal tyrosine kinase (cKit) that is found in gastrointestinal stromal tumors (GIST) and platelet derived growth factor (PDGF), which is commonly mutated in renal cell carcinoma. 

FDA approval information for Nilotinib

Nilotinib received approval for use in the United States in 2007 for treatment of Philadelphia chromosome-positive CML resistant to or intolerant of prior treatment that included imatinib.  Indications were subsequently expanded to include newly diagnosed cases of CML in the chronic phase. 

Dosage and administration for Nilotinib

Nilotinib is available in capsules of 150 and 200 mg under the brand name Tasigna.  The recommended initial dose is 400 mg by mouth twice daily, with dose modification based upon tolerance. 

Side effects of Nilotinib

Side effects are common and include fatigue, diarrhea, anorexia, skin discoloration, rash, hand-foot syndrome, edema, muscle cramps, arthralgias, headache, abdominal discomfort, anemia, cough, and pruritus.  Uncommon side effects include QT interval prolongation, heart failure, pancreatitis, tumor lysis syndrome and renal failure.

 

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