Erlotinib

Erlotinib
Clinical data
Trade namesTarceva
Other namesErlotinib hydrochloride
AHFS/Drugs.comMonograph
MedlinePlusa605008
License data
Pregnancy
category
Routes of
administration		By mouth
ATC code
Legal status
Legal status
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 Edit this at Wikidata
Chemical and physical data
FormulaC22H23N3O4
Molar mass393.443 g·mol−1
3D model (JSmol)
  • 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) checkY
  • Key:AAKJLRGGTJKAMG-UHFFFAOYSA-N checkY
  (verify)

Erlotinib, sold under the brand name Tarceva among others, is a medication used to treat non-small cell lung cancer (NSCLC) and pancreatic cancer.[4] 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.[4] It is taken by mouth.[4]

Common side effects include rash, diarrhea, muscle pain, joint pain, and cough.[4][3] Serious side effects may include lung problems, kidney problems, liver failure, gastrointestinal perforation, stroke, and corneal ulceration.[4] Use in pregnancy may harm the baby.[4] It is a receptor tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR).[4]

Erlotinib was approved for medical use in the United States in 2004.[5][4][3] It is on the World Health Organization's List of Essential Medicines.[6]

  1. ^ "Erlotinib (Tarceva) Use During Pregnancy". Drugs.com. 1 November 2019. Archived from the original on 12 November 2019. Retrieved 23 December 2019.
  2. ^ a b "Tarceva (Erlotinib hydrochloride)". Roche Products Pty Limited. Australian Product Information. 31 August 2022.
  3. ^ a b c "Tarceva- erlotinib hydrochloride tablet". DailyMed. 12 December 2018. Archived from the original on 6 August 2020. Retrieved 23 December 2019.
  4. ^ a b c d e f g h "Erlotinib Monograph for Professionals". Drugs.com. Archived from the original on 24 December 2019. Retrieved 12 November 2019.
  5. ^ "Drug Approval Package: Tarceva (Erlotinib) NDA #021743". U.S. Food and Drug Administration (FDA). 28 March 2005. Archived from the original on 23 December 2019. Retrieved 23 December 2019.
  6. ^ Organization WH (2019). World Health Organization model list of essential medicines: 21st list 2019. World Health Organization. hdl:10665/325771.