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Drug intelligence / Profile preview
2X-121 + dovitinib
- Development stage
- Discontinued
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
**2X-121 + dovitinib** is an investigational combination therapy being studied for the treatment of advanced solid tumors. 2X-121 (also known as E7449 or stenoparib) is an orally available small molecule inhibitor targeting poly(ADP-ribose) polymerase 1 (PARP1) and poly(ADP-ribose) polymerase 2 (PARP2), as well as tankyrase. By inhibiting these enzymes, it prevents DNA repair via the base excision repair pathway, leading to accumulation of DNA damage and promoting cancer cell death. Dovitinib is a small molecule multi-targeted tyrosine kinase inhibitor that blocks several receptor tyrosine kinases involved in tumor growth and angiogenesis, including fibroblast growth factor receptor (FGFR), vascular endothelial growth factor receptor (VEGFR), and platelet-derived growth factor receptor (PDGFR). The combination aims to enhance antitumor activity by simultaneously disrupting DNA repair mechanisms and inhibiting key signaling pathways required for tumor proliferation and survival[1][2][3][5].
- Other names
- Parp inhibitor 2x-121E-7449E7449E 7449
02
Targets
CSF1R (Macrophage colony-stimulating factor receptor)FGFR1 (Fibroblast growth factor receptor 1)FGFR3 (Fibroblast growth factor receptor 3)FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PARP1 (Poly (adp-ribose) polymerase 1)PARP2 (Poly (adp-ribose) polymerase 2)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)TNKS (Poly(ADP-ribose) Polymerase 5a)TNKS2 (Tankyrase 2)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)Pol II (RNA polymerase II elongation factors)
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