Dacomitinib

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Dacomitinib
Dacomitinib.svg
Names
Pronunciationdak" oh mi' ti nib
Trade namesVizimpro
Other namesPF-00299804
  • (2E)-N-{4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl}-4-(1-piperidinyl)-2-butenamide
Clinical data
Drug classEGFR inhibitor[1]
Main usesNon-small-cell lung carcinoma (NSCLC)[2]
Routes of
use
By mouth
Typical dose45 mg OD[3]
External links
AHFS/Drugs.comMonograph
US NLMDacomitinib
MedlinePlusa618055
Legal
License data
Legal status
  • US: ℞-only
  • EU: Rx-only
  • In general: ℞ (Prescription only)
Pharmacokinetics
Bioavailability80%
Protein binding98%
MetabolismCYP2D6, CYP3A4
MetabolitesO-desmethyl-dacomitinib
Elimination half-life70 hrs
Excretion79% faeces, 3% urine
Chemical and physical data
FormulaC24H25ClFN5O2
Molar mass469.95 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 used to treat non-small-cell lung carcinoma (NSCLC).[2] Specifically it is used for cases with certain epidermal growth factor receptor (EGFR) mutations.[2] It is taken by mouth.[2]

Common side effects include diarrhea, rash, mouth inflammation, conjunctivitis, itching, liver problems, and nausea.[3] Other side effects may include interstitial lung disease.[3] Use in pregnancy may harm the baby.[2] It is a tyrosine kinase inhibitor of EGFR.[1]

Dacomitinib was approved for medical use in the United States in 2018 and Europe in 2019.[2][3] In the United States it costs about 14,300 USD per month as of 2021.[4] This amount in the United Kingdom costs the NHS about £2,700.[5]

Medical uses

Dosage

The typical dose is 45 mg per day.[3]

Research

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.[6][7][8] Additional Phase III trials are ongoing[when?].[6]

References

  1. 1.0 1.1 "Dacomitinib". NCI Drug Dictionary. National Cancer Institute, U.S. Department of Health and Human Services. Archived from the original on 28 April 2015. Retrieved 31 May 2021.
  2. 2.0 2.1 2.2 2.3 2.4 2.5 "Dacomitinib Monograph for Professionals". Drugs.com. Archived from the original on 1 January 2022. Retrieved 17 December 2021.
  3. 3.0 3.1 3.2 3.3 3.4 "Vizimpro EPAR". European Medicines Agency (EMA). 5 June 2019. Archived from the original on 13 December 2019. Retrieved 13 December 2019.
  4. "Vizimpro Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 28 May 2019. Retrieved 17 December 2021.
  5. BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 1021. ISBN 978-0857114105.
  6. 6.0 6.1 Chustecka Z (27 January 2014). "Dacomitinib Fails in Pretreated Non-small Cell Lung Cancer". Medscape. Archived from the original on 13 June 2017. Retrieved 31 May 2021.
  7. Taylor P (28 January 2014). "Blow to Pfizer as dacomitinib fails in lung cancer trials". pmlive.com. Archived from the original on 5 March 2019. Retrieved 31 May 2021.
  8. "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. Archived from the original on 11 June 2019. Retrieved 31 May 2021.

External links

External sites:
Identifiers: