Drug intelligence / Profile preview

dacomitinib + dextromethorphan

Development stage
Phase 1
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Dacomitinib (PF-00299804) is an irreversible small-molecule inhibitor of human epidermal growth factor receptors 1 (EGFR), 2 (HER2), and 4 (HER4). It is primarily developed for the treatment of non-small cell lung cancer. Dextromethorphan is a widely used antitussive agent that acts centrally to suppress cough by decreasing activity in the brain's cough center. In clinical pharmacokinetic studies, dacomitinib has been shown to significantly increase systemic exposure to dextromethorphan by inhibiting CYP2D6-mediated metabolism. This combination has been studied in healthy volunteers mainly for drug-drug interaction purposes rather than as a therapeutic regimen[1][3][7].

Other names
PF-00299804PF00299804PF 00299804dacomitinibdextromethorphan
02

Targets

EGFR (Epidermal growth factor receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)NMDAR (Glutamate receptor ionotropic, NMDA)SIGMAR1 (Sigma non-opioid intracellular receptor 1)

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