Erlotinib

Erlotinib
Clinical data
Trade names	Tarceva
Other names	Erlotinib hydrochloride
AHFS/Drugs.com	Monograph
MedlinePlus	a605008
License data	US DailyMed: Erlotinib;
Pregnancy; category	AU: C;
Routes of; administration	By mouth
ATC code	L01EB02 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); UK: POM (Prescription only); US: ℞-only;
Pharmacokinetic data
Bioavailability	59%
Protein binding	95%
Metabolism	Liver (mainly CYP3A4, less CYP1A2)
Elimination half-life	36.2 hrs (median)
Excretion	>98% as metabolites, of which >90% via feces, 9% via urine
Identifiers
	IUPAC name N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy); quinazolin-4-amine; ;
CAS Number	183321-74-6 ;
PubChem CID	176870;
IUPHAR/BPS	4920;
DrugBank	DB00530 ;
ChemSpider	154044 ;
UNII	J4T82NDH7E;
KEGG	D07907 ;
ChEBI	CHEBI:114785 ;
ChEMBL	ChEMBL553 ;
CompTox Dashboard (EPA)	DTXSID8046454 ;
ECHA InfoCard	100.216.020
Chemical and physical data
Formula	C22H23N3O4
Molar mass	393.443 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES COCCOc1cc2c(cc1OCCOC)ncnc2Nc3cccc(c3)C#C;
	InChI 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) ; Key:AAKJLRGGTJKAMG-UHFFFAOYSA-N ;
	(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]

^ "Erlotinib (Tarceva) Use During Pregnancy". Drugs.com. 1 November 2019. Archived from the original on 12 November 2019. Retrieved 23 December 2019.
^ ^a ^b "Tarceva (Erlotinib hydrochloride)". Roche Products Pty Limited. Australian Product Information. 31 August 2022.
^ ^a ^b ^c "Tarceva- erlotinib hydrochloride tablet". DailyMed. 12 December 2018. Archived from the original on 6 August 2020. Retrieved 23 December 2019.
^ ^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.
^ "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.
^ Organization WH (2019). World Health Organization model list of essential medicines: 21st list 2019. World Health Organization. hdl:10665/325771.

[Drugs.com_pregnancy-1] "Erlotinib (Tarceva) Use During Pregnancy". Drugs.com. 1 November 2019. Archived from the original on 12 November 2019. Retrieved 23 December 2019.

[Tarceva_PI-2] "Tarceva (Erlotinib hydrochloride)". Roche Products Pty Limited. Australian Product Information. 31 August 2022.

[Tarceva_label-3] "Tarceva- erlotinib hydrochloride tablet". DailyMed. 12 December 2018. Archived from the original on 6 August 2020. Retrieved 23 December 2019.

[AHFS2019-4] ^ ^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.

[WHO21st-6] Organization WH (2019). World Health Organization model list of essential medicines: 21st list 2019. World Health Organization. hdl:10665/325771.

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