Drug intelligence / Profile preview

INCB057643 + azacitidine

Development stage
Unknown
Lead developer
Incyte
Modality
Small Molecules
Administration
Oral, Intravenous, Subcutaneous
01

Overview

**INCB057643 + azacitidine** is an investigational combination therapy being studied primarily in advanced malignancies, especially acute myeloid leukemia (AML) and high-risk myelodysplastic syndromes (HR-MDS). INCB057643 is a selective, oral, small molecule inhibitor of bromodomain and extra-terminal (BET) proteins, which epigenetically regulate transcription of oncogenic drivers such as c-Myc. Azacitidine is a hypomethylating agent that incorporates into DNA and RNA, inhibiting DNA methyltransferase and resulting in DNA demethylation and cytotoxicity, used widely in the treatment of AML and MDS. This combination is being evaluated in clinical trials for relapsed/refractory AML and HR-MDS, aiming to leverage complementary mechanisms—epigenetic modulation by INCB057643 and DNA hypomethylation by azacitidine—to enhance anti-tumor activity in hematologic malignancies[3].

02

Targets

BRD3 (Bromodomain-containing protein 3)BRD2 (Bromodomain-containing protein 2)DNMT1 (DNA (cytosine-5)-methyltransferase 1)BRD4 (Bromodomain-containing protein 4)

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