Erlotinib hydrochloride For Treat Non-small Cell Lung Cancer 183319-69-9
Erlotinib hydrochloride———Basic info
|Product Name||Erlotinib hydrochloride|
|Chemical Properties||Off-White Solid|
|Usage||Selective epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor. Antineoplastic
Erlotinib HCl is an HER1/EGFR inhibitor with IC50 of 2 nM.
Erlotinib HCl (OSI-744) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Phase 3.
Erlotinib hydrochloride (trade name Tarceva) is a drug used to treat non-small cell lung cancer (NSCLC), pancreatic cancer and several other types of cancer. It is a receptor tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR).
1. Erlotinib hydrochloride is a kind of small molecule epidermal growth factor receptor tyrosine kinase reversible inhibitor. It is mainly used for the second-line or third-line treatment of locally advanced or metastatic non-small cell lung cancer and for the treatment of pancreatic cancer.
2. HER-1/EGFR tyrosine kinase inhibitors.
3.Erlotinib has shown a survival benefit in the treatment of lung cancer in phase III trials. The SATURN (Sequential Tarceva in Unresectable NSCLC) study found that erlotinib added to chemotherapy improved overall survival by 19%, and improved progression-free survival (PFS) by 29%, when compared to chemotherapy alone.
4.The U.S. Food and Drug Administration (FDA) has approved erlotinib for the treatment of locally advanced or metastatic non-small cell lung cancer that has failed at least one prior chemotherapy regimen.
5.In November 2005, the FDA approved erlotinib in combination with gemcitabine for treatment of locally advanced, unresectable, or metastatic pancreatic cancer.
6.In lung cancer, erlotinib has been shown to be effective in patients with or without EGFR mutations, but appears to be more effective in patients with EGFR mutations. Overall survival, progression-free survival and one-year survival are similar to standard second-line therapy ( pemetrexed). Overall response rate is about 50% better than standard second-line chemotherapy.Patients who are non-smokers, and light former smokers, with adenocarcinoma or subtypes like BAC are more likely to have EGFR mutations, but mutations can occur in all types of patients. A test for the EGFR mutation in cancer patients has been developed by Genzyme.
7.Erlotinib has recently been shown to be a potent inhibitor of JAK2V617F activity. JAK2V617F is a mutant of tyrosine kinase JAK2, is found in most patients with polycythemia vera (PV) and a substantial proportion of patients with idiopathic myelofibrosis or essential thrombocythemia. The study suggests that erlotinib may be used for treatment of JAK2V617F-positive PV and other myeloproliferative disorders.