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Ilorasertib + azacitidine
- Development stage
- Unknown
- Lead developer
- AbbVie
- Modality
- Small Molecules
- Administration
- Oral, Subcutaneous, Intravenous
01
Overview
Ilorasertib (ABT-348) is a potent, novel small molecule inhibitor that targets Aurora A, B, and C kinases as well as all members of the vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) receptor tyrosine kinase families. It acts as an adenosine triphosphate competitive inhibitor. Azacitidine is a pyrimidine nucleoside analogue and demethylating agent that inhibits DNA methyltransferase, leading to hypomethylation of DNA and direct cytotoxicity to abnormal hematopoietic cells by incorporation into RNA and DNA. The combination of ilorasertib with azacitidine has been investigated in phase 1 clinical trials for advanced hematologic malignancies such as acute myeloid leukemia (AML), acute lymphoblastic leukemia (ALL), chronic myelogenous leukemia (CML), chronic lymphocytic leukemia (CLL), and myelodysplastic syndromes (MDS). AbbVie developed ilorasertib; azacitidine was originally developed by Pharmacia & Upjohn but is now marketed under the brand name Vidaza by Bristol Myers Squibb[2][3][6][8].
- Brand names
- Vidaza
- Other names
- 5-azacytidine5-azacitidine
02
Targets
PDGFRB (Platelet-derived growth factor receptor beta)AURKB (Aurora kinase B)VEGFR2 (Vascular endothelial growth factor receptor 2)DNMT1 (DNA (cytosine-5)-methyltransferase 1)AURKC (Aurora kinase C)PDGFRA (Platelet-derived growth factor receptor alpha)AURKA (Aurora kinase A)VEGFR-1 (Vascular endothelial growth factor receptor 1)
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