Dacomitinib

Dacomitinib
Clinical data
Trade names	Vizimpro
Other names	PF-00299804
AHFS/Drugs.com	Monograph
MedlinePlus	a618055
License data	US DailyMed: Dacomitinib;
Routes of; administration	By mouth
ATC code	L01XE47 (WHO) ;
Legal status
Legal status	US: ℞-only ;
Pharmacokinetic data
Bioavailability	80%
Protein binding	98%
Metabolism	CYP2D6, CYP3A4
Metabolites	O-desmethyl-dacomitinib
Elimination half-life	70 hrs
Excretion	79% faeces, 3% urine
Identifiers
	IUPAC name (2E)-N-{4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl}-4-(1-piperidinyl)-2-butenamide;
CAS Number	1110813-31-4 ;
PubChem CID	11511120;
IUPHAR/BPS	7422;
DrugBank	DB11963;
ChemSpider	9685914;
UNII	2XJX250C20;
KEGG	D09883;
ChEBI	CHEBI:132268;
ChEMBL	ChEMBL2105719;
CompTox Dashboard (EPA)	DTXSID50149493 ;
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 (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 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

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

External links

"Dacomitinib". Drug Information Portal. U.S. National Library of Medicine.

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[1] "Dacomitinib". NCI Drug Dictionary.

[medscape-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.