Table 2.

Oral agents for treatment and significant interactions of metastatic lung cancer.

TKIs	Recommended Dosage/Day	Indication	Common AEs	Drug-Drug Interactions
Erlotinib	150 mg 1 h before or 2 h after food	first-line for advanced NSCLC	rash, diarrhea, edema, cough, conjunctivitis	inducer of CYP1A2 inhibitor of CYP3A4, CYP1A1 and CYP2C8, medication that alter gastric pH
Gefitinib	250 mg +/− food	first-line for advanced NSCLC	skin reaction, rash, anorexia, stomatitis diarrhea, paronychia	inducers of CYP3A4, and CYP2D6, P-gp, inhibitors of CYP2C19 and CYP2D6, UGT1A1, medication that alter gastric pH
Afatinib	40 mg 1 h before or 2 h after food	second-line for advanced NSCLC	eruption rash dry ski, diarrhea, loss of appetite, stomatitis	negligible metabolism via CYP pathways; substrate and potential inhibitor of P-gp
Osimertinib	80 mg +/− food	third-line for advanced NSCLC	diarrhea, rash, dry skin, nail toxicity, ILD, QTc prolongation, ocular desorder cardiomyopathy	inducers of CYP3A

Abbreviations: QTc, QT interval corrected for heart rate, ILD Interstitial lung disease, CYP cytochrome P450, UGT, uridine diphosphate-glucuronosyltransferase, P-gp P-glycoprotein, +/− food with or without food, AEs adverse events, NSCLC non-small cell lung cancer.