Non-small cell lung cancer, Pancreatic cancer

Erlotinib reversibly inhibits overall epidermal growth factor receptor (HER1/EGFR) - tyrosine kinase activity. Intracellular phosphorylation is inhibited which prevents further downstream signaling, resulting in cell death

Absorption:
1. ~60% on an empty stomach (food increases to ~100%)
2. The solubility is pH dependent and decreases as pH increases. (Avoid concomitant use with PPIs)
Distribution:
Protein binding: 93% to albumin and alpha1-acid glycoprotein
Metabolism:
Hepatic, via CYP3A4 (major); CYP1A1, 1A2, and 1C (minor)
t_1/2 elimination:
36.2 hours
Time to peak, plasma:
4 hours
Excretion:
Feces (83%); urine (8%)

Hypersensitivity to erlotinib or any component of the formulation.

Erlotinib crosses the placenta and may cause fetal harm if administered in pregnancy

Lactating women should not breastfeed during treatment and for 2 weeks after the final erlotinib dose.

Non-small cell lung cancer: 150 mg once daily until disease progression or unacceptable toxicity.
Pancreatic cance: 100 mg once daily (in combination with gemcitabine); continue until disease progression or unacceptable toxicity.

Grades 3/4 renal toxicity: Withhold erlotinib and consider discontinuing. If erlotinib is resumed, reinitiate with a 50 mg dose reduction after toxicity has resolved to baseline or ? grade 1.
Renal failure associated with hepatorenal syndrome or due to dehydration: Withhold erlotinib until renal toxicity is resolved. If erlotinib is resumed, reinitiate with a 50 mg dose reduction after toxicity has resolved.

If total bilirubin >3 times ULN or transaminases >5 times ULN: Interrupt erlotinib and consider discontinuing.
If erlotinib is resumed, reinitiate with a 50 mg dose reduction after bilirubin and transaminases return to baseline or ? grade 1.
Discontinue if hepatotoxicity does not improve within 3 weeks.

Store at room temperature below 30 degree C.