Dacomitinib

Dacomitinib (trade name Vizimpro) is a drug candidate under development by Pfizer for the treatment of non-small-cell lung carcinoma (NSCLC). It is a selective and irreversible inhibitor of EGFR.[1]

Dacomitinib
Clinical data
Trade namesVizimpro
Other namesPF-00299804
AHFS/Drugs.comMonograph
MedlinePlusa618055
License data
Routes of
administration
By mouth
ATC code
Legal status
Legal status
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
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC24H25ClFN5O2
Molar mass469.95 g·mol−1
3D model (JSmol)

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

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

Dacomitinib was approved in the United States in 2018[6], in Japan in 2019 and in the European Union (EU) authorized by the European Medicines Agency (EMA) in 2019 [7] for the treatment of non-small cell lung cancer with EGFR gene mutation.

References

  1. "Dacomitinib". NCI Drug Dictionary.
  2. Zosia Chustecka (27 January 2014). "Dacomitinib Fails in Pretreated Non-small Cell Lung Cancer". Medscape.
  3. "Blow to Pfizer as dacomitinib fails in lung cancer trials". pmlive.com. 28 January 2014.
  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. Dacomitinib Sets PFS Record in Phase III NSCLC Trial. June 2017
  6. Shirley, Matt (2018). "Dacomitinib: First Global Approval". Drugs. 78 (18): 1947–1953. doi:10.1007/s40265-018-1028-x. PMID 30506139.
  7. "Vizimpro EPAR". European Medicines Agency (EMA). 5 June 2019. Retrieved 13 December 2019.
  • "Dacomitinib". Drug Information Portal. U.S. National Library of Medicine.
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