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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors
dacomitinib
L01EB07
Forms & Strengths
- Oral tablets: 15 mg
- Oral tablets: 30 mg
- Oral tablets: 45 mg
Adult Dosing
- Metastatic non-small cell lung cancer (NSCLC): 45 mg orally once daily
- Administer continuously until disease progression or unacceptable toxicity
- Dose reduction for adverse reactions: first reduction to 30 mg daily, second reduction to 15 mg daily
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- First-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) harboring epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R substitution mutations
Mechanism of Action
- Irreversible kinase inhibitor of the human epidermal growth factor receptor (HER) family, including EGFR (HER1), HER2, and HER4
- Binds covalently to target kinases, leading to sustained inhibition of kinase activity and downstream oncogenic signaling
Adverse Reactions
- Diarrhea
- Rash / dermatitis acneiform
- Stomatitis
- Paronychia
- Decreased appetite
- Dry skin
- Pruritus
- Weight decreased
- Alopecia
- Elevated ALT and AST
Drug Interactions
- Strong CYP2D6 inhibitors: may increase dacomitinib exposure; avoid concurrent use or monitor closely
- CYP2D6 substrates: dacomitinib may increase exposure of co-administered sensitive CYP2D6 substrates
- Gastric acid-reducing agents (PPIs, H2 antagonists, antacids): may decrease dacomitinib absorption and efficacy; avoid PPIs, use caution with H2 antagonists or antacids
Curated Content: Needs Vetting Before Put to Clinical Use