Dacomitinib

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Dacomitinib
Dacomitinib.svg
Clinical data
Pronunciationdak" oh mi' ti nib
Trade namesVizimpro
Other namesPF-00299804
AHFS/Drugs.comMonograph
MedlinePlusa618055
License data
Pregnancy
category
  • US: N (Not classified yet)
Routes of
administration
By mouth
ATC code
Legal status
Legal status
  • US: ℞-only
  • EU: Rx-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability80%
Protein binding98%
MetabolismCYP2D6, CYP3A4
MetabolitesO-desmethyl-dacomitinib
Elimination half-life70 hrs
Excretion79% faeces, 3% urine
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC24H25ClFN5O2
Molar mass469.95 g·mol−1
3D model (JSmol)

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.[1]

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.[2][3][4] Additional Phase III trials are ongoing[when?].[2]

In 2017, results of a trial comparing dacomitinib to gefitinib for NSCLC (driven by mutated EGFR) were announced.[5]

Dacomitinib was approved for medical use in the United States in September 2018,[6] in Japan in 2019, and in the European Union in 2019,[7] for the treatment of non-small cell lung cancer with epidermal growth factor receptor (EGFR) gene mutation.

References[edit]

  1. ^ "Dacomitinib". NCI Drug Dictionary. National Cancer Institute, U.S. Department of Health and Human Services.
  2. ^ a b Chustecka Z (27 January 2014). "Dacomitinib Fails in Pretreated Non-small Cell Lung Cancer". Medscape.
  3. ^ Taylor P (28 January 2014). "Blow to Pfizer as dacomitinib fails in lung cancer trials". pmlive.com.
  4. ^ "Pfizer Announces Top-Line Results From Two Phase 3 Trials Of Dacomitinib In Patients With Refractory Advanced Non-Small Cell Lung Cancer". Pfizer Press Release. 27 January 2014.
  5. ^ Smith M (6 June 2017). "Dacomitinib Sets PFS Record in Phase III NSCLC Trial". MedPage Today.
  6. ^ Shirley M (December 2018). "Dacomitinib: First Global Approval". Drugs. 78 (18): 1947–1953. doi:10.1007/s40265-018-1028-x. PMID 30506139. S2CID 54034570.
  7. ^ "Vizimpro EPAR". European Medicines Agency (EMA). 5 June 2019. Retrieved 13 December 2019.

External links[edit]

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