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Nilotinib hydrochloride monohydrate, also known as nilotinib and sold under the trade name Tasigna, is a targeted cancer drug.[2] It is a chemically synthesised substance classified as an antineoplastic agent (ATC code L01EA03; L01XE08).[1] Nilotinib is authorised as a medicine in the European Union, with authorisation records held by Novartis Europharm Limited and Bluepharma Indústria Farmacêutica S.A.[1]
Nilotinib is a type of targeted cancer drug called a tyrosine kinase inhibitor (TKI).[2] Tyrosine kinases are proteins that act as chemical messengers and can stimulate cancer cells to grow. Nilotinib blocks a tyrosine kinase protein called BCR-ABL, which is made by CML cells that have an abnormal chromosome called the Philadelphia chromosome. Blocking this protein stops the leukaemia cells that have the Philadelphia chromosome from growing.[2] Most people with CML have the Philadelphia chromosome.[2]
Nilotinib is given as hard capsules for oral use.[1] The capsules are swallowed whole with water, taken on an empty stomach at least 2 hours before a meal and with no food for 1 hour after.[2] The usual schedule is twice a day, about 12 hours apart.[2] A 200 mg capsule strength is available, including from Teva UK Ltd.[4]
One Phase 1 trial is registered in the EU Clinical Trials Information System for nilotinib.[1] The trial compared the bioavailability of nilotinib 200 mg hard capsules with Tasigna 200 mg hard capsules in 20 healthy subjects.[1] The study is completed.[1]
The primary outcome measured pharmacokinetic endpoints: Cmax (the maximum concentration of the drug in the blood), tmax (the time to reach that maximum), AUC0-t and AUC0-∞ (the total exposure to the drug over time), the percentage of extrapolated AUC, the elimination rate constant λz, and the half-life t1/2.[1] The aim was to explore the comparative bioavailability between the test product and the reference product.[1]
Nilotinib may cause QT prolongation, an irregular heart rhythm that can lead to fainting, loss of consciousness, seizures, or sudden death.[5] Sudden deaths have been reported in patients receiving nilotinib.[3] Patients with low levels of potassium or magnesium in the blood, or with long QT syndrome, should not take nilotinib.[3] Blood tests are carried out before and during treatment to check blood cell levels and how well the liver and kidneys are working.[2]
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