Afatinib

CAS 850140-73-7

About the API

Systematic name (2E)-N-{4-[(3-Chloro-4-fluorophenyl)amino]-7-[(3S)-tetrahydro-3-furanyloxy]-6-quinazolinyl}-4-(dimethylamino)-2-butenamide (2Z)-2-butenedioate (1
Trade name(s) Gilotrif
Technology Synthetic Organic Chemistry
Molecular Formula C32H33ClFN5O11
Molecular Weight 718.082723 g/mol
Physical properties White to yellow-brown powder
Therapeutic category Oncology
Available formulations Oral Solid
Regulations US DMF Flag US DMF

General Information

Afatinib dimaleate, the dimaleate salt form of afanitib, is an orally available antineoplastic agent. It 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.

 

Developed by Boehringer Ingelheim Pharmaceuticals, afatinib dimaleate was approved by the FDA in 2013 as an orphan drug under the trade name Gilotrif.  It is chemically synthesized using standard methods.