Nilotinib — Drug Monograph
Brand names: Tasigna
Drug class: Tyrosine Kinase Inhibitor
Mechanism of Action
Nilotinib is a potent and selective inhibitor of the BCR-ABL tyrosine kinase. It binds to the ATP-binding site of the BCR-ABL protein in its inactive conformation, preventing autophosphorylation and subsequent downstream signaling. This leads to the inhibition of proliferation and induction of apoptosis in cell lines and primary human gene-positive leukemic cells. Nilotinib also inhibits the receptor tyrosine kinases KIT and PDGFR.
FDA Indications
- Adult and pediatric patients greater than or equal to 1 year of age with newly diagnosed Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in chronic phase (CP)
- Adult patients with chronic phase (CP) and accelerated phase (AP) Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) resistant to or intolerant to prior therapy that included imatinib
- Pediatric patients greater than or equal to 1 year of age with Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in chronic phase (CP) with resistance or intolerance to prior tyrosine-kinase inhibitor (TKI) therapy
Common Side Effects
- Nausea
- Rash
- Headache
- Fatigue
- Pruritus
- Vomiting
- Diarrhea
- Cough
- Constipation
- Arthralgia
- Nasopharyngitis
- Pyrexia
- Night sweats
Clinical Pearl
Nilotinib requires strict adherence to fasting requirements as food significantly increases bioavailability and the risk of QT prolongation. It is a second-generation TKI with higher potency than imatinib and is effective against many imatinib-resistant BCR-ABL mutations, except T315I. Monitoring for cardiovascular events is critical, as nilotinib is associated with accelerated atherosclerosis. Patients may be eligible for Treatment-Free Remission (TFR) monitoring after achieving a sustained…
Related Therapies & Mechanisms
- Asciminib (Scemblix) — Tyrosine Kinase Inhibitor · Leukemia
- Dasatinib (Sprycel) — Tyrosine Kinase Inhibitor · Leukemia
- Ibrutinib (Imbruvica) — Tyrosine Kinase Inhibitor · Leukemia
- Idelalisib (Zydelig) — Tyrosine Kinase Inhibitor · Leukemia