Products
Dacomitinib was approved in the US in 2018 and in the EU and many countries in 2019 in film-coated tablet form (Vizimpro).
Structure and properties
Dacomitinib (C24H25ClFN5O2, Mr = 469.9 g/mol) is present in the drug product as dacomitinib monohydrate, a white to pale yellow powder.
Effects
Dacomitinib (ATC L01XE47) has antitumor and antiproliferative properties. The effects are based on irreversible inhibition of the tyrosine kinase activity of the human EGFR family (EGFR/HER1, HER2, and HER4) and of EGFR-activating mutations. The drug is therefore also known as a pan-HER inhibitor. Dacomitinib has a long half-life of up to 80 hours.
Indications
As monotherapy for first-line treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with activating exon 19 deletions or exon 21 (L858R) substitution mutations of the epidermal growth factor receptor (EGFR).
Dosage
According to the SmPC. Tablets are taken once daily, independent of meals.
Contraindications
- Hypersensitivity
- Pregnancy, lactation
Full precautions can be found in the drug label.
Interactions
Dacomitinib should not be combined with proton pump inhibitors and should not be combined with CYP2D6 substrates.
Adverse effects
The most common potential adverse effects include:
- Digestive tract: diarrhea, oral mucositis, lack of appetite, weight loss, nausea.
- Skin: rash, nail disease, dry skin, hair loss, itching.
