Drug intelligence / Profile preview

ilorasertib

Development stage
Phase 1
Lead developer
AbbVie
Modality
Small Molecules
Administration
Oral
01

Overview

Ilorasertib is an orally bioavailable, ATP-mimetic small molecule that acts as a multitargeted kinase inhibitor. It selectively inhibits Aurora kinases (A, B, and C), vascular endothelial growth factor receptors (VEGFRs), platelet-derived growth factor receptors (PDGFRs), and the Src family of tyrosine kinases. By inhibiting these targets, ilorasertib disrupts mitotic checkpoint control and angiogenesis pathways critical for tumor cell proliferation and survival. Developed by AbbVie (originating from Abbott Laboratories) as an antineoplastic agent, it has been investigated primarily in hematologic malignancies such as acute myelogenous leukemia (AML) and myelodysplastic syndromes (MDS), as well as in advanced solid tumors. Clinical trials reached up to phase II before development was discontinued for solid tumors[1][2][3][4][5][7].

Other names
ilorasertibIlorasertib [USAN]1227939-82-3
02

Targets

AURKB (Aurora kinase B)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRB (Platelet-derived growth factor receptor beta)SFK (SRC family kinases)PDGFRA (Platelet-derived growth factor receptor alpha)CSF1R (Macrophage colony-stimulating factor receptor)VEGFR3 (Vascular endothelial growth factor receptor 3)AURKA (Aurora kinase A)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR-1 (Vascular endothelial growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)AURKC (Aurora kinase C)

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