Dacomitinib

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: