Afatinib

CAT#: H200500

CAS#: 850140-72-6


Description: Afatinib, also know as BIBW 2992, is an orally bioavailable dual receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. EGFR/HER2 tyrosine kinase inhibitor BIBW 2992 irreversibly binds to and inhibits human epidermal growth factor receptors 1 and 2 (EGFR-1; HER2), which may result in the inhibition of tumor growth and angiogenesis. EGFR/HER2 are RTKs that belong to the EGFR superfamily; both play major roles in tumor cell proliferation and tumor vascularization and are overexpressed in many cancer cell types. Afatinib is approved in much of the world (including the United States, Canada, the United Kingdom and Australia) for the treatment of metastatic non-small cell lung carcinoma (NSCLC), developed by Boehringer Ingelheim. It acts as an angiokinase inhibitor.

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Synthetic Routes

Afatinib - Synthetic Route 1

Afatinib route01

Synthetic reference

Kovacevic, Tatjana; Mesic, Milan; Avdagic, Amir; Zegarac, Miroslav. An alternative synthesis of the non-small cell lung carcinoma drug afatinib. Tetrahedron Letters. Volume 59. Issue 47. Pages 4180-4182. Journal; Online Computer File. (2018).

Afatinib - Synthetic Route 2

Afatinib route02

Synthetic reference

Anon. Process for the preparation of afatinib. IP.com Journal. Volume 15. Issue 10A. Pages 1-3. Journal; Patent. (2015).

Afatinib - Synthetic Route 3

Afatinib route03

Synthetic reference

Li, Suyang; Xu, Qinxia; Cheng, Qingming. Method for preparation of afatinib. Assignee Suzhou BEC Biology Technology Co., Ltd., Peop. Rep. China. CN 108467388. (2018).

Afatinib - Synthetic Route 4

Afatinib route04

Synthetic reference

Zhang, Guimin; Zhao, Xuliang; Wang, Xiujuan. Intermediate of afatinib and preparation method thereof. Assignee Shandong New Time Pharmaceutical Co., Ltd., Peop. Rep. China. CN 107488194. (2017).

Afatinib - Synthetic Route 5

Afatinib route05

Synthetic reference

Zhang, Xiuju. A method for preparing afatinib. Assignee Kangbolai (Tianjin) Pharmaceutical R & D Co., Ltd., Peop. Rep. China. CN 104478863. (2015).