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Dacomitinib: Difference between revisions

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| OtherNames = PF-00299804
| OtherNames = PF-00299804
| Section1 = {{Chembox Identifiers
| Section1 = {{Chembox Identifiers
| IUPHAR_ligand = 7422
| CASNo = 1042385-75-0
| CASNo = 1042385-75-0
| ChEMBL = 2105719
| ChEMBL = 2105719

Revision as of 06:21, 17 June 2015

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
3D model (JSmol)
ChEMBL
ChemSpider
  • 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
  • COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)NC(=O)/C=C/CN4CCCCC4
Properties
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).

Dacomitinib (PF-00299804) is an experimental drug candidate under development by Pfizer for the treatment of non-small-cell lung carcinoma. It is a selective and irreversible inhibitor of EGFR.[1]

Dacomitinib has advanced to several Phase III clinical trials. The 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]

References

  1. ^ "Dacomitinib". NCI Drug Dictionary.
  2. ^ a b 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.