Erlotinib

Erlotinib, sold under the brand name Tarceva among others, is a medication used to treat non-small cell lung cancer (NSCLC) and pancreatic cancer. Specifically it is used for NSCLC with mutations in the epidermal growth factor receptor (EGFR) — either an exon 19 deletion (del19) or exon 21 (L858R) substitution mutation — which has spread to other parts of the body. It is taken by mouth.

Erlotinib
Clinical data
Trade namesTarceva
Other namesErlotinib hydrochloride
AHFS/Drugs.comMonograph
MedlinePlusa605008
License data
Pregnancy
category
  • AU: C
Routes of
administration		By mouth
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: ℞-only
Pharmacokinetic data
Bioavailability59%
Protein binding95%
MetabolismLiver (mainly CYP3A4, less CYP1A2)
Elimination half-life36.2 hrs (median)
Excretion>98% as metabolites, of which >90% via feces, 9% via urine
Identifiers
    • N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)
    • quinazolin-4-amine
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.216.020
Chemical and physical data
FormulaC22H23N3O4
Molar mass393.443 g·mol−1
3D model (JSmol)
SMILES
  • COCCOc1cc2c(cc1OCCOC)ncnc2Nc3cccc(c3)C#C
  • InChI=1S/C22H23N3O4/c1-4-16-6-5-7-17(12-16)25-22-18-13-20(28-10-8-26-2)21(29-11-9-27-3)14-19(18)23-15-24-22/h1,5-7,12-15H,8-11H2,2-3H3,(H,23,24,25) Y
  • Key:AAKJLRGGTJKAMG-UHFFFAOYSA-N Y
  (verify)

Common side effects include rash, diarrhea, muscle pain, joint pain, and cough. Serious side effects may include lung problems, kidney problems, liver failure, gastrointestinal perforation, stroke, and corneal ulceration. Use in pregnancy may harm the baby. It is a receptor tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR).

Erlotinib was approved for medical use in the United States in 2004. It is on the World Health Organization's List of Essential Medicines.

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