Drug intelligence / Profile preview

danusertib

Development stage
Phase 2
Lead developer
Nerviano Medical Sciences
Modality
Small Molecules
Administration
Intravenous
01

Overview

Danusertib is a small molecule 3‑aminopyrazole derivative and investigational anticancer agent that acts as a potent pan-inhibitor of the Aurora kinase family (Aurora A, B, and C), which are serine/threonine kinases involved in cell division. By inhibiting these kinases—particularly Aurora B—danusertib disrupts mitosis and induces cell cycle arrest and apoptosis in tumor cells with overexpressed Aurora kinases. In addition to its activity against Aurora kinases, danusertib also inhibits several cancer-related tyrosine kinases including Abelson murine leukemia viral oncogene homolog 1 (ABL1) (notably the T315I mutant), Tropomyosin receptor kinase A (TrkA), Fibroblast growth factor receptor 1 (FGFR1), and Ret proto-oncogene (RET). It has been studied primarily for chronic myeloid leukemia (CML), prostate cancer, solid tumors, and leukemia. The drug was originally developed by Nerviano Medical Sciences[1][3][5][6].

Other names
danusertib(R)-N-(5-(2-methoxy-2-phenylacetyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-4-(4-methylpiperazin-1-yl)benzamide
02

Targets

RET (Rearranged during transfection receptor tyrosine kinase)BCR-ABL1 T315I (Bcr-Abl T315I mutant protein)AURKC (Aurora kinase C)FGFR1 (Fibroblast growth factor receptor 1)AURKB (Aurora kinase B)AURKA (Aurora kinase A)NTRK1 (Tropomyosin-related receptor kinase A)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)

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