.Pharmacolibrary.Drugs.L_AntineoplasticAndImmunomodulatingAgents.L01E_ProteinKinaseInhibitors.L01EB01_Gefitinib.Gefitinib

Information

Gefitinib is an oral, selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor used primarily in the treatment of non-small cell lung cancer (NSCLC) harboring EGFR mutations. It is approved and widely used for advanced NSCLC therapy.

Pharmacokinetics

Typical pharmacokinetic parameters in adult patients with solid tumors receiving oral gefitinib; median age about 60 years; both sexes; no significant renal/hepatic impairment.

References

1. Ballard, P, et al., & Cross, D (2016). Preclinical Comparison of Osimertinib with Other EGFR-TKIs in EGFR-Mutant NSCLC Brain Metastases Models, and Early Evidence of Clinical Brain Metastases Activity. Clinical cancer research : an official journal of the American Association for Cancer Research 22(20) 5130–5140. DOI:10.1158/1078-0432.CCR-16-0399 PUBMED:https://pubmed.ncbi.nlm.nih.gov/27435396

2. Xiong, W, et al., & Girard, P (2022). Population pharmacokinetic analysis of tepotinib, an oral MET kinase inhibitor, including data from the VISION study. Cancer chemotherapy and pharmacology 89(5) 655–669. DOI:10.1007/s00280-022-04423-5 PUBMED:https://pubmed.ncbi.nlm.nih.gov/35385993

3. Sanford, M, & Scott, LJ (2009). Gefitinib: a review of its use in the treatment of locally advanced/metastatic non-small cell lung cancer. Drugs 69(16) 2303–2328. DOI:10.2165/10489100-000000000-00000 PUBMED:https://pubmed.ncbi.nlm.nih.gov/19852530

Revisions

• 06/2025 initial generated model