Afatinib Dimaleate CAS 850140-73-7 Purity >99.5% (HPLC) API

Afatinib Dimaleate (CAS: 850140-73-7), the dimaleate salt form of afanitib, is an orally available antineoplastic agent. Afatinib Dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib Dimaleate is indicated for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test. In the past, standard treatment with a platinum-based chemotherapy doublet regimen was considered standard first-line therapy for all patients with NSCLC. However, emerging evidence has identified subpopulations in which targeted therapy is more effective, leading to the development of mutation-specific drugs. Afatinib Dimaleate was Developed by Boehringer Ingelheim Pharmaceuticals, Afatinib Dimaleate was approved by the FDA in 2013 as an orphan drug under the trade name Gilotrif. Afatinib Dimaleate is chemically synthesized using standard methods. Afatinib Dimaleate is not only active against EGFR mutations targeted by first generation TKIs like erlotinib or gefitinib, but also against mutations such as T790M which are not sensitive to these standard therapies. Because of its additional activity against Her2, it is being investigated for breast cancer as well as other EGFR and Her2 driven cancers.