Drug intelligence / Profile preview

dacomitinib

Development stage
Approved
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Dacomitinib is an oral, irreversible small molecule tyrosine kinase inhibitor that targets the human epidermal growth factor receptor (EGFR) family, specifically EGFR (HER1), HER2, and HER4. It covalently binds to cysteine residues in the catalytic domains of these receptors, leading to sustained inhibition of their kinase activity. Dacomitinib is primarily indicated for the first-line treatment of metastatic non-small cell lung cancer (NSCLC) with specific EGFR mutations—namely exon 19 deletion or exon 21 L858R substitution—as detected by an FDA-approved test. By blocking aberrant signaling through these mutated receptors, dacomitinib slows or halts tumor cell proliferation and survival[1][3][7][10]. The drug was developed by Pfizer in collaboration with SFJ Pharmaceuticals[10].

Brand names
Vizimpro
Other names
dacomitinib monohydrate
02

Targets

DDR1 (Discoidin domain receptor 1)DDR2 (Discoidin domain receptor tyrosine kinase 2)LCK (Proto-oncogene tyrosine-protein kinase Lck)ERBB2 (Erb-b2 receptor tyrosine kinase 2)MKNK1 (Mitogen‑activated protein kinase‑interacting serine/threonine-protein kinase 1)EGFR T790M (Epidermal growth factor receptor T790M mutant)EPHA6ERBB4 (Erb-b2 receptor tyrosine kinase 4)

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