.Pharmacolibrary.Drugs.L_AntineoplasticAndImmunomodulatingAgents.L01E_ProteinKinaseInhibitors.L01EB07_Dacomitinib.Dacomitinib

Information

Dacomitinib is an oral, irreversible second-generation tyrosine kinase inhibitor (TKI) targeting the epidermal growth factor receptor (EGFR). It is used for the treatment of non-small cell lung cancer (NSCLC) with EGFR-activating mutations. Dacomitinib is approved for clinical use.

Pharmacokinetics

Pharmacokinetic parameters are based on adult patients with advanced solid tumors including NSCLC in multiple phase I trials.

References

1. Piscitelli, J, et al., & Tan, W (2022). The Effect of Hepatic Impairment on the Pharmacokinetics of Dacomitinib. Clinical drug investigation 42(3) 221–235. DOI:10.1007/s40261-022-01125-x PUBMED:https://pubmed.ncbi.nlm.nih.gov/35195881

2. Takahashi, T, et al., & Yamamoto, N (2012). Phase I and pharmacokinetic study of dacomitinib (PF-00299804), an oral irreversible, small molecule inhibitor of human epidermal growth factor receptor-1, -2, and -4 tyrosine kinases, in Japanese patients with advanced solid tumors. Investigational new drugs 30(6) 2352–2363. DOI:10.1007/s10637-011-9789-z PUBMED:https://pubmed.ncbi.nlm.nih.gov/22249430

3. Chen, X, et al., & Hu, P (2018). Phase 1 study to investigate the pharmacokinetic properties of dacomitinib in healthy adult Chinese subjects genotyped for CYP2D6. Xenobiotica; the fate of foreign compounds in biological systems 48(5) 459–466. DOI:10.1080/00498254.2017.1342881 PUBMED:https://pubmed.ncbi.nlm.nih.gov/28648122

Revisions

• 06/2025 initial generated model