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Drug for the treatment of lung carninoma
Dacomitinib
Pronunciation dak" oh mi' ti nib
Trade names Vizimpro Other names PF-00299804
AHFS /
Drugs.com
Monograph
MedlinePlus
a618055
License data
Routes of administration
By mouth
ATC code
Legal status
Bioavailability 80%
Protein binding 98%
Metabolism
CYP2D6 ,
CYP3A4
Metabolites O-desmethyl-dacomitinib
Elimination half-life 70 hrs
Excretion 79% faeces, 3% urine
(2E )-N -{4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl}-4-(1-piperidinyl)-2-butenamide
CAS Number
PubChem
CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard (
EPA )
Formula C 24 H 25 Cl F N 5 O 2
Molar mass 469.95 g·mol−1 3D model (
JSmol )
COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)NC(=O)/C=C/CN4CCCCC4
InChI=1S/C24H25ClFN5O2/c1-33-22-14-20-17(24(28-15-27-20)29-16-7-8-19(26)18(25)12-16)13-21(22)30-23(32)6-5-11-31-9-3-2-4-10-31/h5-8,12-15H,2-4,9-11H2,1H3,(H,30,32)(H,27,28,29)/b6-5+
Key:LVXJQMNHJWSHET-AATRIKPKSA-N
Dacomitinib , sold under the brand name Vizimpro , is a
medication for the treatment of
non-small-cell lung carcinoma (NSCLC). It is a selective and
irreversible inhibitor of
EGFR .
[3]
Dacomitinib has advanced to several
Phase III clinical trials .[
when? ] The January 2014 results of the first trials were disappointing, with a failure to meet the study goals.
[4]
[5]
[6] Additional Phase III trials are ongoing[
when? ] .
[4]
In 2017, results of a trial comparing dacomitinib to
gefitinib for NSCLC (driven by mutated EGFR) were announced.
[7]
Dacomitinib was approved for medical use in the United States in September 2018,
[8] in Japan in 2019, and in the European Union in 2019,
[9] for the treatment of
non-small cell lung cancer with
epidermal growth factor receptor (EGFR) gene mutation.
References
External links
"Dacomitinib" . Drug Information Portal . U.S. National Library of Medicine.
CI
monoclonal antibodies ("-mab")
Tyrosine kinase inhibitors ("-nib")
Receptor tyrosine kinase
RET inhibitors:
Entrectinib (ALK, ROS1, NTRK),
Futibatinib (FGFR2),
Infigratinib ,
Larotrectinib (NTRK),
Pemigatinib (FGFR),
Pralsetinib ,
Repotrectinib (ROS1, TRK, ALK),
Selpercatinib (VEGFR, FGFR),
Vandetanib (VEGFR, EGFR).
Non-receptor
Other
Angiopoietin
CNTF
EGF (ErbB)
FGF
FGFR1
FGFR2
Agonists:
Ersofermin
FGF (
1 ,
2 (bFGF) ,
3 ,
4 ,
5 ,
6 ,
7 (
KGF ),
8 ,
9 ,
10 (KGF2) ,
17 ,
18 ,
22 )
Palifermin
Repifermin
Selpercatinib
Sprifermin
Trafermin
FGFR3
FGFR4 Unsorted
HGF (c-Met)
IGF
LNGF (p75NTR )
PDGF
RET (GFL)
SCF (c-Kit)
TGFβ
Trk
TrkA
Negative allosteric modulators:
VM-902A
TrkB
Agonists:
3,7-DHF
3,7,8,2'-THF
4'-DMA-7,8-DHF
7,3'-DHF
7,8-DHF
7,8,2'-THF
7,8,3'-THF
Amitriptyline
BDNF
BNN-20
Deoxygedunin
Deprenyl
Diosmetin
DMAQ-B1
HIOC
LM22A-4
N-Acetylserotonin
NT-3
NT-4
Norwogonin (5,7,8-THF)
R7
R13
TDP6
TrkC
VEGF Others
Additional growth factors:
Adrenomedullin
Colony-stimulating factors (see
here instead)
Connective tissue growth factor (CTGF)
Ephrins (
A1 ,
A2 ,
A3 ,
A4 ,
A5 ,
B1 ,
B2 ,
B3 )
Erythropoietin (see
here instead)
Glucose-6-phosphate isomerase (GPI; PGI, PHI, AMF)
Glia maturation factor (GMF)
Hepatoma-derived growth factor (HDGF)
Interleukins /
T-cell growth factors (see
here instead)
Leukemia inhibitory factor (LIF)
Macrophage-stimulating protein (MSP; HLP, HGFLP)
Midkine (NEGF2)
Migration-stimulating factor (MSF; PRG4)
Oncomodulin
Pituitary adenylate cyclase-activating peptide (PACAP)
Pleiotrophin
Renalase
Thrombopoietin (see
here instead)
Wnt signaling proteins
Additional growth factor receptor modulators:
Cerebrolysin (neurotrophin mixture)