Erlotinib
- Atc Codes:L01XE03
- CAS Codes:183319-69-9#183321-74-6
- PHARMGKB ID:183319-69-9#183321-74-6
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Tarceva; Belgium: Tarceva; Cyprus: Tarceva; Czech Republic: Tarceva; Denmark: Tarceva; Estonia: Tarceva; Finland: Tarceva; France: Tarceva; Germany: Tarceva; Greece: Tarceva; Hungary: Tarceva; Ireland: Tarceva; Italy: Tarceva; Latvia: Tarceva; Lithuania: Tarceva; Netherlands: Tarceva; Poland: Tarceva; Portugal: Tarceva; Romania: Tarceva; Slovakia: Tarceva; Slovenia: Tarceva; Spain: Tarceva; Sweden: Tarceva; UK: Tarceva.
North America
Canada: Tarceva; USA: Tarceva.
Latin America
Argentina: Tarceva; Mexico: Tarceva.
Asia
Japan: Tarceva.
Drug combinations
Chemistry
Erlotinib Hydrochloride: C~22~H~23~N~3~O~4~ HCl. Mw: 429.90. (1) 4-Quinazolinamine, N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-, monohydrochloride; (2) 4-(m-Ethynylanilino)-6,7-bis(2-methoxyethoxy)quinazoline monohydrochloride. CAS-183319-69-9; CAS-183321-74-6 (erlotinib)(2001).
Pharmacologic Category
Other Antineoplastic Agents; Protein Kinase Inhibitors. Tyrosine Kinase Inhibitor. Epidermal Growth Factor Receptor Inhibitor. (ATC-Code: L01XE03).
Mechanism of action
An inhibitor of human epidermal growth factor receptor type 1/epidermal growth factor receptor (HER1/EGFR) tyrosine kinase, erlotinib is an antineoplastic agent. It appears to inhibit the intracellular phosphorylation of tyrosine kinase associated with EGFR, expressed on the surface of normal and cancer cells.
Therapeutic use
Used for the treatment of locally advanced or metastatic non-small cell lung cancer refractory to at least one prior chemotherapy regimen. Pancreatic cancer (first-line therapy in combination with gemcitabine).
Pregnancy and lactiation implications
The drug may cause fetal deformities or loss of pregnancy.
Unlabeled use
Contraindications
Hypersensitivity to erlotinib or any component of the formulation. Pregnancy.
Warnings and precautions
Hazardous agent. Cerebrovascular accidents, MI, myocardial ischemia, and/or microangiopathic hemolytic anemia with thrombocytopenia reported (use with caution in cardiovascular disease). Rare, sometimes fatal, pulmonary toxicity (interstitial pneumonia, interstitial lung disease, obliterative bronchiolitis, pulmonary fibrosis). Liver enzyme elevations reported. Hepatic failure and hepatorenal syndrome also reported, particularly in baseline hepatic impairment (use with extreme caution in total bilirubin >3 times ULN). Acute renal failure, renal insufficiency, and hepatorenal syndrome reported (use with caution in patients with or at risk for renal impairment). Use caution with concomitant anticoagulant therapy (elevated INR and bleeding events reported). MI, CVA, and microangiopathic hemolytic anemia with thrombocytopenia noted in patients receiving concomitant erlotinib and gemcitabine. High potential for CYP interactions. Erlotinib levels may be lower in patients who smoke.