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Dacomitinib
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Dacomitinib

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Dacomitinib
Dacomitinib.svg
Clinical data
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
Legal status
Pharmacokinetic data
Bioavailability 80%
Protein binding 98%
Metabolism CYP2D6, CYP3A4
Metabolites O-desmethyl-dacomitinib
Elimination half-life 70 hrs
Excretion 79% faeces, 3% urine
Identifiers
  • (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)
Chemical and physical data
Formula C24H25ClFN5O2
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.

Dacomitinib has advanced to several Phase III clinical trials. The January 2014 results of the first trials were disappointing, with a failure to meet the study goals. Additional Phase III trials are ongoing.

In 2017, results of a trial comparing dacomitinib to gefitinib for NSCLC (driven by mutated EGFR) were announced.

Dacomitinib was approved for medical use in the United States in September 2018, in Japan in 2019, and in the European Union in 2019, for the treatment of non-small cell lung cancer with epidermal growth factor receptor (EGFR) gene mutation.

External links

  • "Dacomitinib". Drug Information Portal. U.S. National Library of Medicine.



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