Erlotinib

Category: pharmacological

Aliases: Tarceva

Pharmacological Mechanism

EGFR tyrosine kinase inhibitor — competitive ATP-site blockade. First-line therapy for EGFR-mutant non-small-cell lung cancer. CYP3A4 substrate. Acneiform rash (~75%) correlates with response. Smoking induces CYP1A2-mediated clearance, lowering levels.

Half-Life (t½)

PO: 36h

Dosing Guidelines

• PO: Typical 150 mg (Range: 100–150 mg)

Target Organ Systems

• respiratory
• digestive

Pathways It Modulates

• MAPK / ERK (RAS-RAF-MEK-ERK) cascade (inhibitor) — EGFR (upstream RTK)
• Tyrosine kinase inhibition (inhibitor) — EGFR kinase

Chemical Identifiers

• PubChem CID: 176870
• Formula: C22H23N3O4
• Molecular weight: 393.44 g/mol
• InChIKey: AAKJLRGGTJKAMG-UHFFFAOYSA-N
• SMILES: COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC

References

• PMID 24474302
• PMID 9354447