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imatinib

Structure via PubChem · Public domain (PubChem)

EntityQ177094· pop 35· linked from 790 articles

Also known as STI571, CGP 57148, STI 571, QTI571, alpha-(4-methyl-1-piperazinyl)-3'-{[4-(3-pyridyl)-2-pyrimidinyl]amino}-P-toluidide, 4-(4-methyl-piperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-benzamide

Imatinib, sold under the brand names Gleevec and Glivec (both marketed worldwide by Novartis) among others, is an oral targeted therapy medication used to treat cancer. Imatinib is a small molecule inhibitor targeting multiple tyrosine kinases such as CSF1R, ABL, c-KIT, FLT3, and PDGFR-β. Specifically, it is used for chronic myelogenous leukemia (CML) and acute lymphocytic leukemia (ALL) that are Philadelphia chromosome–positive (Ph+), certain types of gastrointestinal stromal tumors (GIST), hypereosinophilic syndrome (HES), chronic eosinophilic leukemia (CEL), systemic mastocytosis, and myelo

Key facts

Drug.verifiedrevid
459451238
Drug.image
Imatinib2DACS.svg
Drug.image_class
skin-invert-image
Drug.width
250
Drug.image2
File:Imatinib structure.png
Drug.image_class2
bg-transparent
Drug.width2
280
Drug.alt2
Ball-and-stick model of the imatinib molecule
Drug.pronounce
ih-MAT-ih-nib
Drug.tradename
Gleevec, Glivec, others
Drug.MedlinePlus
a606018
Drug.DailyMedID
Imatinib
Drug.pregnancy_AU
D
Drug.routes_of_administration
By mouth
Drug.class
Tyrosine kinase inhibitor
Drug.ATC_prefix
L01
Drug.ATC_suffix
EA01
Drug.legal_AU
S4

via Wikipedia infobox

Chemical data

Formula
C29H31N7O
Molecular weight
493.6 g/mol
IUPAC name
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
SMILES
CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC=CC(=N4)C5=CN=CC=C5
InChIKey
KTUFNOKKBVMGRW-UHFFFAOYSA-N
XLogP
3.5
Polar surface area
86.3 Ų
H-bond donors
2
H-bond acceptors
7
Formal charge
0

via PubChem

Wikidata facts

Mass
493.259
Show 4 more facts
chemical formula
C₂₉H₃₁N₇O
World Health Organisation international non-proprietary name
imatinib
canonical SMILES
CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC=CC(=N4)C5=CN=CC=C5
Commons category
Imatinib
Sources (7)

via Wikidata · CC0

~28 min read

Article

28 sections
Contents
  • Medical uses
  • Chronic myelogenous leukemia
  • Gastrointestinal stromal tumors
  • Dermatofibrosarcoma protuberans (DFSP)
  • Other
  • Contraindications and cautions
  • Side effects
  • Cardiotoxicity
  • Childhood growth inhibition
  • Pigmentation changes
  • Hepatotoxicity
  • Overdose
  • Interactions
  • Pharmacology
  • Mechanism of action
  • Other pathways affected
  • Pharmacokinetics
  • Chemistry
  • Synthesis
  • History
  • Society and culture
  • Economics
  • Controversies
  • Patent litigation in India
  • Research
  • Etymology
  • References
  • External links

{{infobox drug | verifiedrevid = 459451238 | image = Imatinib2DACS.svg | image_class = skin-invert-image | width = 250 | alt = | image2 = File:Imatinib structure.png | image_class2 = bg-transparent | width2 = 280 | alt2 = Ball-and-stick model of the imatinib molecule | caption = | pronounce = ih-MAT-ih-nib | tradename = Gleevec, Glivec, others | Drugs.com = | MedlinePlus = a606018 | DailyMedID = Imatinib | pregnancy_AU = D | pregnancy_AU_comment = | pregnancy_category = | routes_of_administration = By mouth | class = Tyrosine kinase inhibitor | ATC_prefix = L01 | ATC_suffix = EA01 | ATC_supplemental = | legal_AU = S4 | legal_AU_comment = | legal_BR = | legal_BR_comment = | legal_CA = Rx-only | legal_CA_comment = | legal_DE = | legal_DE_comment = | legal_NZ = | legal_NZ_comment = | legal_UK = POM | legal_UK_comment = | legal_US = Rx-only | legal_US_comment = | legal_EU = Rx-only | legal_EU_comment = | legal_UN = | legal_UN_comment = | legal_status =

| bioavailability = 98% | protein_bound = 95% | metabolism = Liver (mainly CYP3A4-mediated) | metabolites = | onset = | elimination_half-life = 18 h (imatinib)40 h (active metabolite) | duration_of_action = | excretion = Fecal (68%) and kidney (13%)

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