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INCB-057643
- Development stage
- Phase 2
- Lead developer
- Incyte
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
INCB‑057643 is an orally bioavailable small molecule inhibitor of the bromodomain and extra-terminal (BET) family of proteins, developed by Incyte for the treatment of hematologic malignancies such as myelofibrosis and myelodysplastic syndromes. It binds to acetylated lysine recognition motifs in the bromodomains of BET proteins, preventing their interaction with acetylated histones. This disrupts chromatin remodeling and gene expression, including downregulation of c‑Myc-dependent genes, leading to inhibition of tumor cell growth. The drug also modulates immune cells in the tumor microenvironment by reducing PD-L1 expression on macrophages and FOXP3 expression in CD4 T cells[1][3][5][6]. Clinical trials have evaluated it as monotherapy or in combination with ruxolitinib for advanced myeloid neoplasms[4][5].
- Other names
- 1820889-23-3UNII-87TZD0JEBSUNII87TZD0JEBSUNII 87TZD0JEBS
02
Targets
BRD3 (Bromodomain-containing protein 3)BRD2 (Bromodomain-containing protein 2)BRD4 (Bromodomain-containing protein 4)
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