Nilotinib

Definition

An orally bioavailable aminopyrimidine-derivative Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. Designed to overcome imatinib resistance, nilotinib binds to and stabilizes the inactive conformation of the kinase domain of the Abl protein of the Bcr-Abl fusion protein, resulting in the inhibition of the Bcr-Abl-mediated proliferation of Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) cells. This agent also inhibits the receptor tyrosine kinases platelet-derived growth factor receptor (PDGF-R) and c-kit, a receptor tyrosine kinase mutated and constitutively activated in most gastrointestinal stromal tumors (GISTs). With a binding mode that is energetically more favorable than that of imatinib, nilotinib has been shown to have an approximately 20-fold increased potency in kinase and proliferation assays compared to imatinib.

Also known as 4-Methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)-N-(5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl)benzamide, AMN 107 Base Form, NILOTINIB — per NCIT

Also identified as

• ATC L01EA03 per RXNORM
• NCIT NCIT:C48375 per NCIT
• SCTID 427941004 per RXNORM
• SCTID 428468009 per RXNORM
• UNII F41401512X per RXNORM

Indications

Organ Effects

1 entry above is marked DERIVED: Atlas Médico inferred it by combining two sourced claims, and no source asserts this link directly. Treat it as a navigation aid, not as a clinical statement.