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nintedanib + everolimus
- Development stage
- Phase 1
- Lead developer
- Boehringer Ingelheim
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
A combination of the small-molecule tyrosine kinase inhibitor nintedanib and the mTOR inhibitor everolimus. Nintedanib inhibits multiple receptor tyrosine kinases involved in angiogenesis and fibrosis, including VEGFR1-3, PDGFRα/β, FGFR1-3 (and FLT3 and certain Src-family kinases), thereby reducing fibroblast proliferation, migration, and angiogenic signaling. Everolimus forms a complex with FKBP12 to inhibit mTOR, blocking downstream signaling that drives cell-cycle progression, proliferation, angiogenesis, and glucose uptake. This combination is investigational; no fixed-dose co-formulation is approved. Potential pharmacokinetic interaction: nintedanib may decrease the metabolism of everolimus (raising exposure). Uses of each component separately include interstitial lung diseases and NSCLC for nintedanib, and various cancers and transplant-related indications for everolimus.
- Brand names
- Vargatef
- Other names
- Torpenz
02
Targets
FGFR2 (Keratinocyte growth factor receptor)FKBP1AFLT3 (Fms related receptor tyrosine kinase 3)VEGFR1/2/3 (Vascular endothelial growth factor receptor 1 (VEGFR1) / Vascular endothelial growth factor receptor 2 (VEGFR2) / Vascular endothelial growth factor receptor 3 (VEGFR3))Mechanistic target of rapamycin complex 1Mechanistic target of rapamycin kinase complex 2FGFR1 (Fibroblast growth factor receptor 1)FGFR3 (Fibroblast growth factor receptor 3)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)SRC (Proto-oncogene tyrosine-protein kinase Src)LCK (Proto-oncogene tyrosine-protein kinase Lck)LYN (LYN proto-oncogene, Src family tyrosine kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)
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