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o-desmethyl dacomitinib
- Development stage
- Unknown
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
O-desmethyl dacomitinib is a major circulating active metabolite of dacomitinib, an irreversible pan-human epidermal growth factor receptor (HER) inhibitor. It is formed primarily through the oxidative metabolism of dacomitinib by the cytochrome P450 enzyme CYP2D6. This small molecule metabolite exhibits similar in vitro pharmacologic activity to its parent drug, dacomitinib, which is approved for the first-line treatment of metastatic non-small cell lung cancer (NSCLC) with specific epidermal growth factor receptor (EGFR) mutations.
- Other names
- DACOMITINIB METABOLITE M20DACOMITINIB, O-DESMETHYL(E)-N-(4-(3-CHLORO-4-FLUORO-ANILINO)-7-HYDROXY-QUINAZOLIN-6-YL)-4-(1-PIPERIDYL)BUT-2-ENAMIDE
02
Targets
LCK (Proto-oncogene tyrosine-protein kinase Lck)ERBB2 (Erb-b2 receptor tyrosine kinase 2)EPHA6ERBB4 (Erb-b2 receptor tyrosine kinase 4)EGFR T790M (Epidermal growth factor receptor T790M mutant)MKNK1 (Mitogen‑activated protein kinase‑interacting serine/threonine-protein kinase 1)DDR1 (Discoidin domain receptor 1)DDR2 (Discoidin domain receptor tyrosine kinase 2)
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