What is dacomitinib?

Dacomitinib, manufactured by Pfizer Inc., is a daily oral drug used as a first-line treatment for metastatic non-small cell lung cancer (NSCLC). It targets two specific cancer biomarkers detected by tests approved by the U.S. Food and Drug Administration (FDA): EGFR exon 19 deletion mutations and EGFR exon 21 L858R substitution mutations.

Dacomitinib is an irreversible small molecule inhibitor of the tyrosine kinase activity of the human epidermal growth factor receptor (EGFR) family (EGFR/HER1, HER2 and HER4). It forms an irreversible inhibitory effect by forming a covalent bond with the cysteine residue in the catalytic domain of the HER receptor. The affinity of dacomitinib has been demonstrated to have an IC50 of 6 nmol/L. Approximately 40% of cases show EGFR gene amplification, and 50% of cases have EGFRvIII mutations, which represent a deletion resulting in continuous activation of the receptor tyrosine kinase domain.

The original drug of dacomitinib has been launched in China and has entered the scope of Class B medical insurance. The price of the common specification 15mg*30 tablets per box may be more than 1,000 yuan; the European version of dacomitiniboriginal drug sold overseas, the specification 45mg*30 tablets may be more than 20,000 yuan per box (the price may fluctuate due to exchange rates). Currently, there are cheaper generic drugs of dacomitinib sold overseas. Their pharmaceutical ingredients are basically the same as those of the original drugs sold domestically and abroad. For example, the price of 45mg*30 tablets produced by a Lao pharmaceutical factory may be around a few hundred yuan per box (the price may fluctuate due to exchange rate effects).