ERLOTINIB HYDROCHLORIDE

AbsorptionErlotinib is about 60% absorbed after oral administration. Peak plasma levels occur 4 hours after dosing. Effect of Food Food increased the bioavailability of erlotinib to approximately 100%. Distribution: Erlotinib is 93% protein bound to plasma albumin and alpha-1 acid glycoprotein (AAG). Erlotinib has an apparent volume of distribution of 232 liters.

EliminationErlotinib is eliminated with a median half-life of 36.2 hours in patients receiving the single-agent erlotinib 2 nd /3 nd...

14.1 Non-Small Cell Lung Cancer (NSCLC) – First-Line Treatment of Patients with EGFR Mutations

Study 1The safety and efficacy of erlotinib as monotherapy for the first-line treatment of patients with metastatic NSCLC containing EGFR exon 19 deletions or exon 21 (L858R) substitution mutations was demonstrated in Study 1, a randomized, open-label, clinical trial conducted in Europe. One hundred seventy-four (174) White patients were randomized 1:1 to receive erlotinib 150 mg once daily until disease progression (n = 86) or four cycles of a standard platinum-based doublet chemotherapy (n = 88); ...

The following serious adverse reactions, which may include fatalities, are discussed in greater detail in other sections of the labeling: Interstitial Lung Disease (ILD) [see Warnings and Precautions (5.1) ] Renal Failure [see Warnings and Precautions (5.2) ] Hepatotoxicity with or without Hepatic Impairment [see Warnings and Precautions (5.3) ] Gastrointestinal Perforation [see Warnings and Precautions (5.4) ] Bullous and Exfoliative Skin Disorders [see Warnings and Precautions (5.5) ] Cer...

None. None. ( 4 )

Interstitial lung disease (ILD): Occurs in 1.1% of patients. Withhold erlotinib for acute onset of new or progressive unexplained pulmonary symptoms, such as dyspnea, cough and fever. Discontinue erlotinib if ILD is diagnosed. ( 5.1 ) Renal failure: Monitor renal function and electrolytes, particularly in patients at risk of dehydration. Withhold erlotinib for severe renal toxicity. ( 5.2 ) Hepatotoxicity: Occurs with or without hepatic impairment, including hepatic failure and hepatorenal syndr...

7 DRUG INTERACTIONS CYP3A4 Inhibitors Co-administration of erlotinib with a strong CYP3A4 inhibitor or a combined CYP3A4 and CYP1A2 inhibitor increased erlotinib exposure. Erlotinib is metabolized primarily by CYP3A4 and to a lesser extent by CYP1A2. Increased erlotinib exposure may increase the risk of exposure-related toxicity [see Clinical Pharmacology (12.3) ]. Avoid co-administering erlotini...