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ICP-248 + azacitidine
- Development stage
- Unknown
- Lead developer
- InnoCare Pharma
- Modality
- Small Molecules
- Administration
- Oral, Intravenous, Subcutaneous
01
Overview
ICP-248 + azacitidine is an investigational **combination therapy** being studied primarily for **acute myelogenous leukemia (AML)**, including newly diagnosed and relapsed/refractory cases. **ICP-248** (also known as mesutoclax) is an orally bioavailable, highly selective inhibitor of **B-cell lymphoma-2 (BCL2)**, a key protein blocking apoptosis in cancer cells. By inhibiting BCL2, ICP-248 promotes cancer cell death. **Azacitidine** is a well-established hypomethylating agent and nucleoside metabolic inhibitor, acting as a DNA methyltransferase inhibitor to induce DNA hypomethylation, leading to the reactivation of tumor suppressor genes and cytotoxicity in abnormal hematopoietic cells. The combination aims to leverage potential synergistic anti-leukemic effects. ICP-248 is being developed by **InnoCare Pharma** and is undergoing Phase 1 clinical evaluation as a combination with azacitidine for AML and myelodysplastic syndromes (MDS)[1][3][5][7][9].
- Other names
- ICP-248 + azacitidine
02
Targets
BCL-2 (BCL-2 family)DNMT (DNA methyltransferase)
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