Dacomitinib Explained

Pronounce:dak" oh mi' ti nib
Tradename:Vizimpro
Dailymedid:Dacomitinib
Routes Of Administration:By mouth
Atc Prefix:L01
Atc Suffix:EB07
Legal Ca:Rx-only
Legal Ca Comment:[1] [2]
Legal Us:Rx-only
Legal Eu:Rx-only
Legal Status:Rx-only
Bioavailability:80%
Protein Bound:98%
Metabolism:CYP2D6, CYP3A4
Metabolites:O-desmethyl-dacomitinib
Elimination Half-Life:70 hrs
Excretion:79% faeces, 3% urine
Index2 Label:as salt
Cas Number:1110813-31-4
Pubchem:11511120
Drugbank:DB11963
Chemspiderid:9685914
Unii:2XJX250C20
Kegg:D09883
Kegg2:D10514
Chebi:132268
Chembl:2105719
Iuphar Ligand:7422
Pdb Ligand:1C9
Synonyms:PF-00299804
Iupac Name:(2E)-N--4-(1-piperidinyl)-2-butenamide
C:24
H:25
Cl:1
F:1
N:5
O:2
Smiles:COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)NC(=O)/C=C/CN4CCCCC4
Stdinchi: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+
Stdinchikey: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. The January 2014 results of the first trials were disappointing, with a failure to meet the study goals,[4] [5] [6] but additional Phase III trials continued.[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.

External links

Notes and References

  1. Web site: Vizimpro Product information . Health Canada . 25 April 2012 . 29 May 2022.
  2. Web site: Summary Basis of Decision (SBD) for Verzenio . . 23 October 2014 . 29 May 2022.
  3. Web site: Dacomitinib. NCI Drug Dictionary . National Cancer Institute, U.S. Department of Health and Human Services .
  4. News: Dacomitinib Fails in Pretreated Non-small Cell Lung Cancer . Medscape . Zosia . Chustecka . vanc . January 27, 2014 .
  5. News: Phil . Taylor . vanc . Blow to Pfizer as dacomitinib fails in lung cancer trials . 28 January 2014 . pmlive.com.
  6. Web site: Pfizer Announces Top-Line Results From Two Phase 3 Trials Of Dacomitinib In Patients With Refractory Advanced Non-Small Cell Lung Cancer . January 27, 2014 . Pfizer Press Release.
  7. Web site: Michael . Smith . vanc . Dacomitinib Sets PFS Record in Phase III NSCLC Trial . 6 June 2017 . MedPage Today .
  8. Shirley M . 54034570 . Dacomitinib: First Global Approval . Drugs . 78 . 18 . 1947–1953 . December 2018 . 30506139 . 10.1007/s40265-018-1028-x . free .
  9. Web site: Vizimpro EPAR . European Medicines Agency (EMA) . 5 June 2019 . 13 December 2019.