Dacomitinib

Names
Pronunciation	dak" oh mi' ti nib
Trade names	Vizimpro
Other names	PF-00299804
IUPAC name (2E)-N-{4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl}-4-(1-piperidinyl)-2-butenamide
Clinical data
Drug class	EGFR inhibitor[1]
Main uses	Non-small-cell lung carcinoma (NSCLC)[2]
Routes of use	By mouth
Typical dose	45 mg OD[3]
External links
AHFS/Drugs.com	Monograph
MedlinePlus	a618055
Legal
License data	US DailyMed: Dacomitinib
Legal status	US: ℞-only EU: Rx-only In general: ℞ (Prescription only)
Pharmacokinetics
Bioavailability	80%
Protein binding	98%
Metabolism	CYP2D6,CYP3A4
Metabolites	O-desmethyl-dacomitinib
Eliminationhalf-life	70 hrs
Excretion	79% faeces, 3% urine
Chemical and physical data
Formula	C24H25ClFN5O2
Molar mass	469.95 g·mol−1
3D model (JSmol)	Interactive image
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 nameVizimpro, is a medication used to treatnon-small-cell lung carcinoma (NSCLC).^[2] Specifically it is used for cases with certainepidermal 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 includeinterstitial lung disease.^[3] Use in pregnancy may harm the baby.^[2] It is atyrosine 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 theNHS about £2,700.^[5]

Medical uses

Dosage

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

Mechanism of action

The mode of action of dacomitinib works by binding to kinase domains ofEGFR family(EGFR/HER1,HER2,HER4). As a consequence this inhibits tyrosine kinase autophosphorylation, which causes a reduction in tumor growth^[6]

Research

Dacomitinib has advanced to severalPhase III clinical trials.The January 2014 results of the first trials were disappointing, with a failure to meet the study goals.^[7][8][9]

Additional Phase III trials are ongoing.^[7]

References

External links

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