Drug intelligence / Profile preview

emavusertib

Development stage
Phase 2
Lead developer
Curis
Modality
Small Molecules
Administration
Oral
01

Overview

Emavusertib is an orally bioavailable small molecule inhibitor that selectively targets interleukin‑1 receptor-associated kinase 4 (IRAK4), as well as Fms-like tyrosine kinase 3 (FLT3) and Cdc-like kinase (CLK). It is being developed primarily for the treatment of hematologic malignancies such as acute myeloid leukemia (AML), myelodysplastic syndromes (MDS), and certain lymphomas. By inhibiting IRAK4, emavusertib disrupts key signaling pathways involved in inflammation and cancer cell survival—specifically the toll-like receptor (TLR) and interleukin‑1 receptor (IL‑1R) pathways—which are often overactive in these diseases. The drug has shown antineoplastic and immunomodulatory activity in preclinical models and early clinical trials. Emavusertib is under investigation in multiple phase I/II studies for relapsed or refractory AML, MDS, non-Hodgkin's lymphoma, malignant melanoma, gastric cancer, esophageal cancer, anemia associated with these conditions, and other hematologic malignancies[2][3][4][5][6][10].

Other names
emavusertibN-[5-[(3R)-3-hydroxypyrrolidin-1-yl]-2-morpholin-4-yl-[1,3]oxazolo[4,5-b]pyridin-6-yl]-2-(2-methylpyridin-4-yl)-1,3-oxazole-4-carboxamide
02

Targets

GSG2 (Germ cell associated 2, haspin)CLK1 (CDC-like kinase 1)CLK2 (CDC-like kinase 2)CLK3 (CDC-like kinase 3)FLT3 (Fms related receptor tyrosine kinase 3)CLK4IRAK4 (Interleukin-1 receptor associated kinase 4)

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