Erlotinib (Tarceva)
(Genentech, OSI Pharmaceuticals (US), Roche (elsewhere)) Bioavailability significantly enhanced by food to nearly 100%; 60% absorption following oral dosing; peak plasma levels 4 h after dosing;
Vd= 232 L Metabolized mainly by hepatic CYP3A4 and to a lesser extent by CYP1A2 and extrahepatic isoform CYP1A1 150 mg (for non-small cell lung cancer); 100 mg (pancreatic cancer);
93% binding (AAG, HSA) Interstitial lung disease associated with erlotinib; approximately 1 percent of patients treated with erlotinib develop pulmonary toxicity, within the first few months of treatment (223) (140)