Pronounce: | dak" oh mi' ti nib |
Tradename: | Vizimpro |
Dailymedid: | Dacomitinib |
Routes Of Administration: | By mouth |
Atc Prefix: | L01 |
Atc Suffix: | EB07 |
Legal Ca: | Rx-only |
Legal Ca Comment: | [1] [2] |
Legal Us: | Rx-only |
Legal Eu: | Rx-only |
Legal Status: | Rx-only |
Bioavailability: | 80% |
Protein Bound: | 98% |
Metabolism: | CYP2D6, CYP3A4 |
Metabolites: | O-desmethyl-dacomitinib |
Elimination Half-Life: | 70 hrs |
Excretion: | 79% faeces, 3% urine |
Index2 Label: | as salt |
Cas Number: | 1110813-31-4 |
Pubchem: | 11511120 |
Drugbank: | DB11963 |
Chemspiderid: | 9685914 |
Unii: | 2XJX250C20 |
Kegg: | D09883 |
Kegg2: | D10514 |
Chebi: | 132268 |
Chembl: | 2105719 |
Iuphar Ligand: | 7422 |
Pdb Ligand: | 1C9 |
Synonyms: | PF-00299804 |
Iupac Name: | (2E)-N--4-(1-piperidinyl)-2-butenamide |
C: | 24 |
H: | 25 |
Cl: | 1 |
F: | 1 |
N: | 5 |
O: | 2 |
Smiles: | COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)NC(=O)/C=C/CN4CCCCC4 |
Stdinchi: | 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+ |
Stdinchikey: | LVXJQMNHJWSHET-AATRIKPKSA-N |
Dacomitinib, sold under the brand name Vizimpro, is a medication for the treatment of non-small-cell lung carcinoma (NSCLC). It is a selective and irreversible inhibitor of EGFR.[3]
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,[4] [5] [6] but additional Phase III trials continued.[4] In 2017, results of a trial comparing dacomitinib to gefitinib for NSCLC (driven by mutated EGFR) were announced.[7]
Dacomitinib was approved for medical use in the United States in September 2018,[8] in Japan in 2019, and in the European Union in 2019,[9] for the treatment of non-small cell lung cancer with epidermal growth factor receptor (EGFR) gene mutation.