Epidermal growth factor receptor inhibitors
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Epidermal growth factor receptor inhibitors, abbreviated EGFR inhibitors, is a class of drugs that blocks the EGF receptor.
EGFR
- EGFR (aka. ErbB1 or HER1) is a membranous receptor expressed in epithelial cells.
- Most of activating mutations in NSCLC are in Exon 18-21 (kinase domain).
- 45% of the mutations are p.DEL19, approx 40-45% are p.L858R, approx 2% are p.T790M.
Drugs
First generation:
Second generation:
- Dacomitinib (Vizimpro, Pfizer) - not effective when EGFR T790M mutation present.[2]
- Afatinib (Gilotrif) - esp. effective when del19 is present.[3]
Third generation:
- Osimertinib [4]
- Nazartinib
Note:
- Both gefitinib and erlotinib are also classified as tyrosine kinase inhibitors (TKIs). After 10-12 months, tumors usu. develop resistencies.
Use
References
- ↑ 1.0 1.1 Sun Y, Ren Y, Fang Z, et al. (October 2010). "Lung adenocarcinoma from East Asian never-smokers is a disease largely defined by targetable oncogenic mutant kinases". J. Clin. Oncol. 28 (30): 4616–20. doi:10.1200/JCO.2010.29.6038. PMID 20855837.
- ↑ Mok, TS.; Cheng, Y.; Zhou, X.; Lee, KH.; Nakagawa, K.; Niho, S.; Lee, M.; Linke, R. et al. (Jun 2018). "Improvement in Overall Survival in a Randomized Study That Compared Dacomitinib With Gefitinib in Patients With Advanced Non-Small-Cell Lung Cancer and EGFR-Activating Mutations.". J Clin Oncol: JCO2018787994. doi:10.1200/JCO.2018.78.7994. PMID 29864379.
- ↑ Yang, JC.; Wu, YL.; Schuler, M.; Sebastian, M.; Popat, S.; Yamamoto, N.; Zhou, C.; Hu, CP. et al. (Feb 2015). "Afatinib versus cisplatin-based chemotherapy for EGFR mutation-positive lung adenocarcinoma (LUX-Lung 3 and LUX-Lung 6): analysis of overall survival data from two randomised, phase 3 trials.". Lancet Oncol 16 (2): 141-51. doi:10.1016/S1470-2045(14)71173-8. PMID 25589191.
- ↑ Alsharedi, M.; Bukamur, H.; Elhamdani, A. (Jun 2018). "Osimertinib for the treatment of patients with". Drugs Today (Barc) 54 (6): 369-379. doi:10.1358/dot.2018.54.6.2817668. PMID 29998228.