Indications
Nilotinib is used to treat newly diagnosed adult patients with Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in the chronic phase. The study is still ongoing, and more data will be needed to know the long-term outcome. Nilotinib is also used for chronic phase (CP) and accelerated phase (AP) Ph+ CML in adult patients who are resistant to, or can't tolerate, earlier treatment that included imatinib. In this group, clinical benefit, such as improvement in disease-related symptoms or increased survival, has not been demonstrated.
⚠️ Always consult a registered physician before taking any medicine.
Pharmacology
Chronic myelogenous leukaemia (CML) is caused by the BCR-ABL oncogene, and Nilotinib works by blocking the tyrosine kinase activity of the BCR-ABL protein. It fits into the ATP-binding site of that protein with higher affinity than imatinib does, so it can over-ride the resistance that mutations cause.
AMN107 can also inhibit TEL-platelet-derived growth factor receptor-beta (TEL-PDGFRbeta), which causes chronic myelomonocytic leukaemia, and FIP1-like-1-PDGFRalpha, which causes hypereosinophilic syndrome. This suggests it may have a use in myeloproliferative diseases that are marked by these kinase fusions.
AMN107 also inhibits the c-Kit receptor kinase, including the D816V-mutated variant of KIT, at concentrations that can be reached in the body with the medicine. This supports its potential use in treating mastocytosis and gastrointestinal stromal tumours.
Pregnancy & Breastfeeding
Nilotinib is Pregnancy Category D. This means there is positive evidence of human foetal risk, but the benefits in pregnant women may still be acceptable despite that risk, for example when the medicine is needed in a life-threatening situation or for a serious disease where safer drugs can't be used or don't work.
Women who are sexually active should use effective contraception while on treatment. Nilotinib should not be used while breast-feeding.
There is no data to support its use in children. In patients with hepatic impairment, a lower starting dose is recommended.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Dosage Reference
⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.
Side Effects & Interactions
Side Effects
No side-effect data recorded yet.