Clinical Status of recently approved drugs [24, 25]. The fundamental functional principle and clinical aspect of the four FDA-approved EGFR-TKIs that are most frequently used are summarised in this gefitinib (Iressa), erlotinib (Tarceva), osimertinib (Tagrisso), afatinib (Gilotrif), and dacomitinib (Vizimpro) [26]
TKI | Erlotinib | Gefitinib | Afatinib | Dacomitinib | Osimertinib |
---|---|---|---|---|---|
Brand name | Tarceva | Iressa | Gilotrif | Vizimpro | Tagrisso |
Dose | 150 mg 1 h before or 2 h after food | 250 mg +/− food | 40 mg 1 h before or 2 h after food | 45 mg orally once daily | 80 mg +/− food |
Indication | First generation for advanced NSCLC | First generation for advanced NSCLC | Second generation for advanced NSCLC | Second generation for advanced NSCLC | Third generation for advanced NSCLC |
Side effects | Rash, diarrhea, edema, cough, conjunctivitis | skin reaction, rash, anorexia, stomatitis diarrhea, paronychia | Eruption rash dry skin, diarrhea, loss of appetite, stomatitis, diarrhea | Diarrhea, interstitial lung disease, stomatitis, rash | QTc prolongation, ocular disorder cardiomyopathy |
MOA | Competitive; reversibleEGFR L858R, Del19 | Competitive; reversibleEGFR L858R, Del19 | Covalent; irreversibleEGFR L858R, L858R/T790M | Covalent; irreversibleEGFR L858R, L858R/T790M | Covalent; irreversible |
Drug approval year | 2004 | 2003 | 2013 | 2012 | 2015 |
Status | Phase III approved (2012) | Phase III approved (2019) | Phase III approved (2021) | Phase III approved (2018) | Phase III approved (2021) |
NSCLC: non-small cell lung cancer; MOA: mechanism of action
Authors are thankful to the Management of Dr Vishwanath Karad MIT-World Peace University, Kothrud, Pune 411038.
PSW: Writing—original draft, Data curation. ARC: Conceptualization, Writing—review & editing. KGR: Data curation, Validation, Visualization. BGP: Writing—review & editing. SCJ: Supervision, Validation.
The authors declare no conflicts of interest.
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© The Author(s) 2024.