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Pharmacological Classification: Antineoplastic (Protein Kinase Inhibitor).
Pharmacology: Pharmacokinetics: Erlotinib is absorbed from the gastrointestinal tract, with a bioavailability of about 60%; this may increase up to almost 100% in the presence of food. Peak plasma concentrations are reached about 4 hours after a dose, and it is about 93% bound to plasma proteins. Erlotinib is metabolize predominantly by the cytochrome P450 isoenzyme CYP3A4, and to a lesser extent by CYP1A2. Metabolic pathways include demethylation, to metabolites OSI-420 and OSI-413, oxidation, and aromatic hydroxylation. Erlotinib has an elimination half-life of about 36 hours. More than 80% of a dose is excreted as metabolites in the feces.
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