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.
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
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
US DMF