Drug intelligence / Profile preview

INCB053914 + azacitidine

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

Overview

INCB053914 + azacitidine is an investigational combination therapy consisting of the pan-PIM kinase inhibitor INCB053914 (also known as uzansertib) and the hypomethylating agent azacitidine. INCB053914 inhibits all three PIM kinases (PIM1, PIM2, and PIM3), which are involved in promoting cell proliferation and survival in hematologic malignancies[3][4][7]. Azacitidine is a cytidine analog that incorporates into DNA and RNA, resulting in inhibition of DNA methyltransferase and reactivation of tumor-suppressor genes, leading to cell death and differentiation. The combination is being studied primarily in acute myeloid leukemia (AML), particularly in newly diagnosed older patients who are unfit for intensive chemotherapy[1][5][8]. Preclinical and clinical trials indicate synergistic or additive anti-leukemic effects due to the overlapping mechanisms targeting leukemic cell survival and proliferation[3][7]. INCB053914 is developed by Incyte, and clinical trials indicate oral administration for INCB053914 and intravenous or subcutaneous administration for azacitidine[1][8].

Other names
INCB053914 + azacitidine
02

Targets

DNMT (DNA methyltransferase)PIM2 (Proto-oncogene serine/threonine-protein kinase Pim2)PIM1 (Proviral integration site for moloney murine leukemia virus kinase 1)PASK (Per-arnt-sim kinase)PIM3 (Proviral integration site for Moloney murine leukemia virus kinase 3)

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