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]

TKIErlotinibGefitinibAfatinibDacomitinibOsimertinib
Brand nameTarcevaIressaGilotrifVizimproTagrisso
Dose150 mg 1 h before or 2 h after food250 mg +/− food40 mg 1 h before or 2 h after food45 mg orally once daily80 mg +/− food
IndicationFirst generation for advanced NSCLCFirst generation for advanced NSCLCSecond generation for advanced NSCLCSecond generation for advanced NSCLCThird generation for advanced NSCLC
Side effectsRash, diarrhea, edema, cough, conjunctivitisskin reaction, rash, anorexia, stomatitis diarrhea, paronychiaEruption rash dry skin, diarrhea, loss of appetite, stomatitis, diarrheaDiarrhea, interstitial lung disease, stomatitis, rashQTc prolongation, ocular disorder cardiomyopathy
MOACompetitive; reversible
EGFR L858R, Del19
Competitive; reversible
EGFR L858R, Del19
Covalent; irreversible
EGFR L858R, L858R/T790M
Covalent; irreversible
EGFR L858R, L858R/T790M
Covalent; irreversible
Drug approval year20042003201320122015
StatusPhase 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