Imatinib

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Imatinib
Systematic (IUPAC) name
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3- [(4-pyridin-3-ylpyrimidin-2-yl)amino]-phenyl]- benzamide
Identifiers
CAS number	152459-95-5 220127-57-1 (mesilate)
ATC code	L01XE01
PubChem	5291
DrugBank	APRD01028
Chemical data
Formula	C₂₉H₃₁N₇O
Mol. mass	493.603 g/mol 589.7 g/mol (mesilate)
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	98%
Protein binding	95%
Metabolism	Hepatic (mainly CYP3A4-mediated)
Half life	18 hours (imatinib) 40 hours (active metabolite)
Excretion	Fecal (68%) and renal (13%)
Therapeutic considerations
Pregnancy cat.	D(AU) D(US)
Legal status	POM(UK) ℞-only(US)
Routes	Oral

Imatinib is a drug used to treat certain types of cancer. It is currently marketed by Novartis as Gleevec (USA) or Glivec (Europe/Australia) as its mesylate salt, imatinib mesilate (INN). It was originally coded during development as CGP57148B or STI-571 (these terms are used in early preclinical publications). It is used in treating chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and a number of other malignancies.

It is the first member of a new class of agents that act by inhibiting particular tyrosine kinase enzymes, instead of non-specifically inhibiting rapidly dividing cells.

Summary Provided Under GNU Free Documentation License

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