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APG-115 + cytarabine
- Development stage
- Phase 1
- Lead developer
- Ascentage Pharma
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
**APG-115 + cytarabine** is an investigational drug combination consisting of APG-115, a novel, orally active small-molecule inhibitor of mouse double minute 2 homolog (MDM2), and cytarabine, a pyrimidine nucleoside analog chemotherapeutic. APG-115 blocks the interaction between MDM2 and p53, thereby activating the p53-mediated apoptosis pathway, inducing cell cycle arrest, and inhibiting proliferation of tumor cells in acute myeloid leukemia (AML). Cytarabine induces DNA damage and activates the ATM/ATR-p53/p21 signaling cascade, contributing to cell cycle arrest and apoptosis. When used together, APG-115 + cytarabine has shown synergistic antileukemic activity, significantly enhancing apoptosis and inhibiting cellular growth, especially in TP53 wild-type AML models. This combination is undergoing clinical investigation for relapsed/refractory AML and myelodysplastic syndromes (MDS)[1][3][4][7][9].
- Brand names
- Alrizomadlin
- Other names
- APG-115 + Ara-C
02
Targets
DNA polymerase familyMDM2 (Mouse double minute 2 homolog)TP53 (Cellular Tumor Antigen p53 R175H)
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