Dacomitinib

Dacomitinib
Names
	IUPAC name (2E)-N-{4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl}-4-(1-piperidinyl)-2-butenamide
	Other names PF-00299804
Identifiers
CAS Number	1110813-31-4 ;
3D model (JSmol)	Interactive image;
ChEBI	CHEBI:132268;
ChEMBL	ChEMBL2105719;
ChemSpider	9685914;
IUPHAR/BPS	7422;
KEGG	D09883;
PubChem CID	11511120;
UNII	2XJX250C20 ;
	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; InChI=1/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-AATRIKPKBC;
	SMILES COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)NC(=O)/C=C/CN4CCCCC4;
Properties
Chemical formula	C24H25ClFN5O2
Molar mass	469.95 g·mol−1
	Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
	Infobox references

Dacomitinib (PF-00299804) 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]

As of August 2018, Pfizer has filed drug applications with the US FDA and the European Medicines Agency.^[6]

References

↑ "Dacomitinib". NCI Drug Dictionary.
1 2 Zosia Chustecka (January 27, 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. January 27, 2014.
↑ Dacomitinib Sets PFS Record in Phase III NSCLC Trial. June 2017
↑ H. Spreitzer (13 August 2018). "Neue Wirkstoffe - Dacomitinib". Österreichische Apothekerzeitung (in German) (17/2018).

External links

Dacomitinib Fact Sheet, Pfizer

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[1] "Dacomitinib". NCI Drug Dictionary.

[medscape-2] 1 2 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

[Spreitzer-6] H. Spreitzer (13 August 2018). "Neue Wirkstoffe - Dacomitinib". Österreichische Apothekerzeitung (in German) (17/2018).