Clinical data | |
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Trade names | Tarceva |
Other names | Erlotinib hydrochloride |
AHFS/Drugs.com | Monograph |
MedlinePlus | a605008 |
License data | |
Pregnancy category |
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Routes of administration | By mouth tablets |
Legal status | |
Legal status | |
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 | |
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Chemical and physical data | |
Formula | C22H23N3O4 |
Molar mass | 393.443 g·mol−1 |
3D model (JSmol) | |
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Erlotinib, sold under the brand name Tarceva among others, is a medication used to treat non-small cell lung cancer (NSCLC) and pancreatic cancer.[3] 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.[3] It is taken by mouth.[3]
Common side effects include rash, diarrhea, muscle pain, joint pain, and cough.[3][4] Serious side effects may include lung problems, kidney problems, liver failure, gastrointestinal perforation, stroke, and corneal ulceration.[3] Use in pregnancy may harm the baby.[3] It is a receptor tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR).[3]
Erlotinib was approved for medical use in the United States in 2004.[5][3][4] It is on the World Health Organization's List of Essential Medicines.[6] In the United States, as of 2019[update], it costs about US$8,832 per month.[7] In the United Kingdom this amount costs the NHS about £1,632 per month.[8]
References
edit- ^ a b "Erlotinib (Tarceva) Use During Pregnancy". Drugs.com. 1 November 2019. Retrieved 23 December 2019.
- ^ "WHOCC - ATC/DDD Index". www.whocc.no. Retrieved 10 September 2020.
- ^ a b c d e f g h "Erlotinib Monograph for Professionals". Drugs.com. Retrieved 12 November 2019.
- ^ a b "Tarceva- erlotinib hydrochloride tablet". DailyMed. 12 December 2018. Retrieved 23 December 2019.
- ^ "Drug Approval Package: Tarceva (Erlotinib) NDA #021743". U.S. Food and Drug Administration (FDA). 28 March 2005. Retrieved 23 December 2019.
- ^ Organization, World Health (2019). "World Health Organization model list of essential medicines: 21st list 2019" (Document). hdl:10665/325771.
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(help) - ^ "Tarceva Prices, Coupons & Patient Assistance Programs". Drugs.com.
- ^ British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 950. ISBN 9780857113382.