Drug intelligence / Profile preview

2X-121 + dovitinib

Development stage
Unknown
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

PDGFRB (Platelet-derived growth factor receptor beta)TNKS (Poly(ADP-ribose) Polymerase 5a)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)PDGFRA (Platelet-derived growth factor receptor alpha)CSF1R (Macrophage colony-stimulating factor receptor)FGFR3 (Fibroblast growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)TNKS2 (Tankyrase 2)FGFR1 (Fibroblast growth factor receptor 1)FLT3 (Fms related receptor tyrosine kinase 3)PARP2 (Poly (adp-ribose) polymerase 2)

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