Systematic (IUPAC) name | |
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4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)- 5-(trifluoromethyl)phenyl]-3- [(4-pyridin-3-ylpyrimidin-2-yl) amino]benzamide | |
Clinical data | |
Trade names | Tasigna |
AHFS/Drugs.com | monograph |
MedlinePlus | a608002 |
Licence data | EMA:Link, US FDA:link |
Pregnancy cat. | D(US) |
Legal status | POM (UK) ℞-only (US) |
Routes | Oral |
Pharmacokinetic data | |
Bioavailability | 30% |
Protein binding | 98% |
Metabolism | hepatic |
Half-life | 17 h |
Excretion | biliary |
Identifiers | |
CAS number | 641571-10-0(base) |
ATC code | L01XE08 |
PubChem | CID 644241 |
DrugBank | DB04868 |
ChemSpider | 559260 |
UNII | F41401512X |
KEGG | D08953 |
ChEBI | CHEBI:52172 |
ChEMBL | CHEMBL255863 |
Chemical data | |
Formula | C28H22F3N7O |
Mol. mass | 529.5245 g/mol |
SMILES | eMolecules & PubChem |
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Nilotinib (AMN107, trade name Tasigna), in the form of the hydrochloride monohydrate salt, is a tyrosine kinase inhibitor approved for the treatment of chronic myelogenous leukemia[1].
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It was approved as Tasigna in the USA and the EU for drug-resistant chronic myelogenous leukemia (CML).[2] In June 2006, a Phase I clinical trial found nilotinib has a relatively favorable safety profile and shows activity in cases of CML resistant to treatment with imatinib (Gleevec), another tyrosine kinase inhibitor currently used as a first-line treatment.[3] In that study 92% of patients (already resistant or unresponsive to imatinib) achieved a normal white blood cell counts after five months of treatment.[4] The drug carries a black box warning for possible heart complications.[5][6]
Nilotinib inhibits the kinases BCR-ABL,[7] KIT, LCK, EPHA3, EPHA8, DDR1, DDR2, PDGFRB, MAPK11 and ZAK.[8]
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