.Pharmacolibrary.Drugs.L_AntineoplasticAndImmunomodulatingAgents.L01E_ProteinKinaseInhibitors.L01EB01_Gefitinib.Gefitinib_1

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

Population PK in Chinese NSCLC patients, both sexes, median age ~55; normal hepatic and renal function.

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