Products
Nilotinib is commercially available in capsule form (Tasigna). It has been approved in many countries since 2007.
Structure and properties
Nilotinib (C28H22F3N7O, Mr = 529.5 g/mol) is present in the drug product as nilotinib hydrochloride monohydrate, a white to slightly yellowish or greenish-yellow powder. The aminopyrimidine is structurally closely related to its precursor imatinib (Gleevec).
Effects
Nilotinib (ATC L01XE08) has antiproliferative properties. It binds competitively to the ATP-binding site of BCR-ABL kinase, inhibiting cell proliferation. Nilotinib is active against imatinib-resistant and mutant forms of BCR-ABL.
Indications
For the treatment of chronic myeloid leukemia (Ph+CML) in chronic and accelerated phase in the presence of resistance or high toxicity with pretreatment with imatinib.
Dosage
According to the SmPC. Capsules are taken fasting in the morning and evening 12 hours apart. The capsules should not be opened and the powder in the capsules should not come into contact with the skin, mucous membranes, and respiratory tract.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Nilotinib is a substrate of CYP3A4 and P-glycoprotein. Corresponding drug-drug interactions are possible and must be considered.
Adverse effects
The most common potential adverse effects include thrombocytopenia, neutropenia, and anemia, muscle pain, rash, pruritus, headache, lipase elevation, fatigue, nausea, constipation, and diarrhea. Nilotinib may prolong the QT interval and rarely cause sudden cardiac death. Other side effects observed include.
