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439081-18-2

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Afatinib (BIBW 2992) is the second-generation potent and irreversible dual inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) tyrosine kinase, developed by Boehringer Ingelheim, Germany. It is capable of irreversibly inhibiting the activity of the tyrosine kinase by undergoing the Michael reaction with the thiol group of cysteine at position 797 of the EGFR. On July 12, 2013, it became a new drug for anti-small cell lung cancer approved by the US FDA under the trade name of Gilotrif. This drug is a tablet. It is used for the treatment of the patients diagnosed with metastatic non-small cell lung cancer (NSCLC) with the loss of the 19th exon or L858R mutation in the 21th exon of the tumor epidermal growth factor receptor (EGFR) confirmed using the kit approved by FDA. The drug is also effective in the treatment of HER2-positive patients with advanced breast cancer.<br /> Boehringer Ingelheim Pharmaceuticals has applied for the protection of this compound by applying patents JP2004516283 US2010010023 WO2002050043 and so on.<br /> Lung cancer is the world's top tumor killer with the incidence in male being higher than that in women. The number of annually new diagnosed lung cancer patients can reach 1.6 million. However, lung cancer is not just a disease. Studies have shown that lung cancer contains many different types with different types of lung cancer needs to be given specific treatment. A specific subtype of lung cancer can be determined by EGFR (ErbB receptor family members) mutation detection. These patients are also those who can benefit from the most during the treatment with Afatinib in clinical trials.<br /> The registration approval for Afatinib in the United States is based on data from the pivotal LUX-Lung 3 trial. This trial had conducted comparison study on the Afatinib versus pemetrexed/cisplatin proposal. Data from the LUX-Lung 3 trial have demonstrated that patients who have received first-line therapy of Afatinib achieved a survival time of one year (median progression-free survival (PFS) period is about 11.1 months) before tumor growth resumed, While the value for patients receiving pemetrexed/cisplatin was slightly more than six months (PFS 6.9 months). In addition, NSCLC patients with two of the most common EGFR mutations (Del19 or L858R) had experienced a progression-free survival of over one year after receiving afatinib treatment (PFS, 13.6 months), whereas patients in the control group got a PFS of slightly more than six months (PFS 6.9 months).<br /> In addition, compared with patients receiving standard chemotherapy, the lung cancer symptoms and quality of life of patients receiving afatinib have also been greatly improved. <br /> In the afatinib treatment group, the most common three classes of adverse events associated with drugs were diarrhea (14%), rash (16%) and thyroid inflammation (paronychia) (11%). In the chemotherapy (pemetrexed/cisplatin), the most common drug-related AE was neutropenia (15%) and neutropenia (13%) and leukopenia (8%). Low incidence of discontinuation associated with treatment-related adverse events had been observed in the trial (8% discontinuation in the afatinib group and 12% discontinuation in the chemotherapy group). In the afatinib-treated group, only 1% of patients have discontinued the medication because of drug-related diarrhea.<br /> This information is compiled and edited by Xiao Nan of chemicalbook.
Lastest Price from Afatinib (BIBW 2992) manufacturers
  • Afatinib (BIBW 2992)
  • US $30.00 /KG
  • CAS:439081-18-2
  • Min. Order: 1KG
  • Purity: 99
  • Supply Ability: 999
  • 2020-11-16
  • Afatinib
  • US $0.00-0.00/KG
  • CAS:439081-18-2
  • Min. Order: 1g
  • Purity: 99.0%
  • Supply Ability: 50kg/month
  • 2020-07-22

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