Drug intelligence / Profile preview

nintedanib + gefitinib + erlotinib + afatinib + osimertinib

Development stage
Unknown
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

This is a hypothetical combination of five small molecule tyrosine kinase inhibitors: nintedanib, gefitinib, erlotinib, afatinib, and osimertinib. All five drugs are orally administered and primarily used in the treatment of non-small cell lung cancer (NSCLC), particularly in patients with specific mutations in the epidermal growth factor receptor (EGFR). Nintedanib is a triple angiokinase inhibitor targeting vascular endothelial growth factor receptors (VEGFRs), fibroblast growth factor receptors (FGFRs), and platelet-derived growth factor receptors (PDGFRs). Gefitinib, erlotinib, afatinib, and osimertinb are EGFR tyrosine kinase inhibitors; afatinb irreversibly inhibits EGFR as well as HER2/ErbB2 and HER4/ErbB4. Osimertinb is notable for its activity against T790M resistance mutations in EGFR. This combination has not been described or approved for clinical use as a single regimen; however, individual agents or dual combinations have been studied for advanced NSCLC[1][3][5][6][7].

Brand names
Vargatef
Other names
BIBF 1120 (nintedanib)ZD1839 (gefitinib)OSI-774 (erlotinib)BIBW 2992 (afatinib)AZD9291 (osimertinib)
02

Targets

SFK (SRC family kinases)ERBB4 (Erb-b2 receptor tyrosine kinase 4)PDGFRA (Platelet-derived growth factor receptor alpha)FGFR2 (Keratinocyte growth factor receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)EGFR T790M (Epidermal growth factor receptor T790M mutant)JAK3 (Janus kinase 3)FLT3 (Fms related receptor tyrosine kinase 3)

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