Nilotinib
Mechanism :
Nilotinib is a selective tyrosine kinase inhibitor that targets BCR-ABL kinase, c-KIT and platelet derived growth factor receptor (PDGFR).
Indication :
- Chronic myelogenous leukemia
- Off-label:
- Acute lymphoblastic leukemia (ALL)
- Philadelphia chromosome-positive (Ph+)
- Gastrointestinal stromal tumor (GIST) (refractory)
Contraindications :
Hypersensitivity to nilotinib or any component of the formulation; persistent QTc >48 msec, Hypokalemia, hypomagnesemia, or long QT syndrome.
Dosing :
Oral:
≥1 year
230 mg/m² twice daily (rounded to the nearest 50 mg dose); Maximum: 400 mg (as a single dose) twice daily.
Adverse Effect :
Rash, headache, nausea, pruritus, fatigue, fever, diarrhea, constipation, vomiting, arthralgia, cough, extremity pain, asthenia, muscle spasms, myalgia, abdominal pain, bone pain, back pain, dyspnea, nasopharyngitis, peripheral edema, dizziness, QTc prolongation, hyperglycemia, hyperkalemia, hypomagnesemia, neutropenia, pancytopenia, Hepatitis B virus reactivation, Thrombotic microangiopathy.
Interaction :
Antacids: May decrease the serum concentration of Nilotinib.
Antidiabetic Agents: Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents.
CYP3A4 Inducers: May decrease the serum concentration of Nilotinib.
CYP3A4 Inhibitors: May increase the serum concentration of Nilotinib.
QT-prolonging Agents: May enhance the QTc-prolonging effect of Nilotinib.
Vaccines (Live): Immunosuppressants may enhance the adverse/toxic effect of live vaccines.
Hepatic Dose :
Hepatotoxicity occurring during treatment:
If elevated ALT or AST = 5 times upper limit of normal (ULN) or bilirubin elevation is = 1.5 times ULN: Withhold treatment and monitor transaminases or bilirubin. When ALT or AST returns to < 2.5 times ULN or bilirubin returns to = 1.5 times ULN, resume treatment at 230 mg/m2 once daily (if previous dose was 230 mg/m2 twice daily). If previous dose was already 230 mg/m2 once daily and recovery to = grade 1 was longer than 28 days, discontinue treatment.
If elevated bilirubin