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GSK3915393 + nintedanib
- Development stage
- Phase 1
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
GSK3915393 + nintedanib is an investigational combination drug intended for the treatment of idiopathic pulmonary fibrosis (IPF). **GSK3915393** is a novel, selective small molecule inhibitor of transglutaminase 2 (TG2) developed by GSK, designed to block fibrotic processes via inhibition of ECM cross-linking and myofibroblast activation[2][5]. **Nintedanib** is an approved small molecule kinase inhibitor developed by Boehringer Ingelheim that targets multiple receptor tyrosine kinases, including VEGFR, FGFR, and PDGFR, and acts as an antifibrotic by slowing pulmonary function decline[3]. Research is ongoing to establish the safety, efficacy, and pharmacokinetic properties of the combination, as GSK3915393 is being studied both as monotherapy and as an add-on to standard-of-care agents such as nintedanib for IPF. The combination may offer complementary or synergistic antifibrotic effects by targeting distinct pathways involved in the progression of pulmonary fibrosis[2].
- Brand names
- Vargatef
- Other names
- GSK3915393GSK-3915393GSK 3915393nintedanib
02
Targets
CSF1R (Macrophage colony-stimulating factor receptor)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR4 (Fibroblast growth factor receptor 4)FLT3 (Fms related receptor tyrosine kinase 3)LCK (Proto-oncogene tyrosine-protein kinase Lck)LYN (LYN proto-oncogene, Src family tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)SRC (Proto-oncogene tyrosine-protein kinase Src)TGM2 (Tissue Transglutaminase 2)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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