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Molecular properties generated using the CDK
|Compound class||Synthetic organic|
|Approved drug?||Yes (FDA (2018))|
|International Nonproprietary Names|
|PF-00299804 | PF00299804 | Vizimpro®|
|Dacomitinib is a second-generation, irreversible pan inhibitor of HER tyrosine kinases (EGFR, and ERBBs) that is being developed by Pfizer.
Results from the ARCHER 1050 Phase 3 randomised, open-label trial (NCT01774721) that directly compared dacomitinib against gefitinib, as first-line treatment for patients with EGFR-mutation +ve non-small-cell lung cancer (NSCLC), reported that dacomitinib significantly increased progression-free survival and overall survival compared to gefitinib . Dacomitinib's use may be limited in NSCLC patients with brain metastases, as these patients were excluded from the trial because dacomitinib's ability to cross the blood-brain-barrier has not been fully confirmed. This is unlike osimertinib (another third-generation irreversible EGFR inhibitor) which has confirmed brain penetrance, and which does not appear to cause the same dose-limiting toxicities that afflict dacomitinib. In April 2018 both the FDA and EMA accepted regulatory submissions (New Drug Application and Marketing Authorization Application respectively) for review of dacomitinib as a therapy for metastatic NSCLC with EGFR-activating mutations. The FDA granted Priority Review status for the submitted NDA.
|CAS Registry No.||1110813-31-4|
|GtoPdb PubChem SID||178103994|
|RCSB PDB Ligand||1C9|
|Search Google for chemical match using the InChIKey||LVXJQMNHJWSHET-AATRIKPKSA-N|
|Search Google for chemicals with the same backbone||LVXJQMNHJWSHET|
|Search PubMed clinical trials||dacomitinib|
|Search PubMed titles||dacomitinib|
|Search PubMed titles/abstracts||dacomitinib|
|Search UniChem for chemical match using the InChIKey||LVXJQMNHJWSHET-AATRIKPKSA-N|
|Search UniChem for chemicals with the same backbone||LVXJQMNHJWSHET|
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Cat. No. 6231