Dacomitinib

Dacomitinib
Names
Pronunciationdak" oh mi' ti nib
Trade namesVizimpro
Other namesPF-00299804
IUPAC name
  • (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]
WHO AWaReUnlinkedWikibase error: ⧼unlinkedwikibase-error-statements-entity-not-set⧽
Routes of
use		By mouth
Typical dose45 mg OD[3]
External links
AHFS/Drugs.comMonograph
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)
SMILES
  • COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)NC(=O)/C=C/CN4CCCCC4
InChI
  • 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. 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.[6]

References

  1. 1 2 "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. 1 2 3 4 5 6 "Dacomitinib Monograph for Professionals". Drugs.com. Archived from the original on 1 January 2022. Retrieved 17 December 2021.
  3. 1 2 3 4 5 "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. 1 2 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.
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