Clinical data | |
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Pronunciation | dak" oh mi' ti nib |
Trade names | Vizimpro |
Other names | PF-00299804 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a618055 |
License data |
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Routes of administration | By mouth |
ATC code | |
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Pharmacokinetic data | |
Bioavailability | 80% |
Protein binding | 98% |
Metabolism | CYP2D6, CYP3A4 |
Metabolites | O-desmethyl-dacomitinib |
Elimination half-life | 70 hrs |
Excretion | 79% faeces, 3% urine |
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PDB ligand | |
CompTox Dashboard (EPA) | |
Chemical and physical data | |
Formula | C24H25ClFN5O2 |
Molar mass | 469.95 g·mol−1 |
3D model (JSmol) | |
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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.
Gefitinib, sold under the brand name Iressa, is a medication used for certain breast, lung and other cancers. Gefitinib is an EGFR inhibitor, like erlotinib, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Therefore, it is only effective in cancers with mutated and overactive EGFR, but resistances to gefitinib can arise through other mutations. It is marketed by AstraZeneca and Teva.
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Alectinib (INN), sold under the brand name Alecensa, is an anticancer medication that is used to treat non-small-cell lung cancer (NSCLC). It blocks the activity of anaplastic lymphoma kinase (ALK). It is taken by mouth. It was developed by Chugai Pharmaceutical Co. Japan, which is part of the Hoffmann-La Roche group.
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