In short
Nilotinib (Tasigna) is a targeted cancer drug used to treat chronic myeloid leukaemia (CML), a cancer of the white blood cells. It belongs to a class of medicines called tyrosine kinase inhibitors. One Phase 1 trial in the EU Clinical Trials Information System (CTIS) compared the bioavailability of nilotinib 200 mg hard capsules in 20 healthy subjects, with the study now completed.
Key points
- Nilotinib is a tyrosine kinase inhibitor that blocks the BCR-ABL protein in CML cells.
- The registered trial is a Phase 1 bioavailability study in 20 healthy subjects.
- The trial compared nilotinib 200 mg hard capsules with Tasigna 200 mg hard capsules.
- The study measured pharmacokinetic endpoints including Cmax and AUC.
- The trial status is Completed.
- Nilotinib is authorised as a medicine in the EU and is also known as Tasigna.
What is nilotinib?
Nilotinib hydrochloride monohydrate, also known as nilotinib and sold under the trade name Tasigna, is a targeted cancer drug. It is a chemically synthesised substance classified as an antineoplastic agent (ATC code L01EA03; L01XE08). Nilotinib is authorised as a medicine in the European Union, with authorisation records held by Novartis Europharm Limited and Bluepharma Indústria Farmacêutica S.A.
How does nilotinib work?
Nilotinib is a type of targeted cancer drug called a tyrosine kinase inhibitor (TKI). 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. Most people with CML have the Philadelphia chromosome.
Which conditions is it used or studied for?
- Chronic myeloid leukaemia (CML) — a cancer of the white blood cells. Nilotinib is used to treat certain types of CML, including newly diagnosed Philadelphia chromosome positive CML in chronic phase in adults and children aged 1 year and older.
- Accelerated phase Ph+ CML — nilotinib is also indicated for adults with chronic phase and accelerated phase Ph+ CML resistant to or intolerant to prior therapy.
How is nilotinib given?
Nilotinib is given as hard capsules for oral use. 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. The usual schedule is twice a day, about 12 hours apart. A 200 mg capsule strength is available, including from Teva UK Ltd.
What do the clinical trials show?
One Phase 1 trial is registered in the EU Clinical Trials Information System for nilotinib. The trial compared the bioavailability of nilotinib 200 mg hard capsules with Tasigna 200 mg hard capsules in 20 healthy subjects. The study is completed.
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. The aim was to explore the comparative bioavailability between the test product and the reference product.
What side effects are known?
Nilotinib may cause QT prolongation, an irregular heart rhythm that can lead to fainting, loss of consciousness, seizures, or sudden death. Sudden deaths have been reported in patients receiving nilotinib. Patients with low levels of potassium or magnesium in the blood, or with long QT syndrome, should not take nilotinib. Blood tests are carried out before and during treatment to check blood cell levels and how well the liver and kidneys are working.