Dacomitinib

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Dacomitinib
Dacomitinib.svg
Clinical data
Trade namesVizimpro
SynonymsPF-00299804
AHFS/Drugs.comvizimpro
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 (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 has advanced to several Phase III clinical trials. The Jan 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] and in Japan in 2019 for the treatment of non-small cell lung cancer with EGFR gene mutation.

References[edit]

  1. ^ "Dacomitinib". NCI Drug Dictionary.
  2. ^ a b Zosia Chustecka (January 27, 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. January 27, 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.

External links[edit]