Drug intelligence / Profile preview

AMG 925

Development stage
Discontinued
Lead developer
Amgen
Modality
Small Molecules
Administration
Oral
01

Overview

AMG 925 is a **potent, selective, and orally available small molecule** developed as a *dual kinase inhibitor* that targets both **Fms-like tyrosine kinase 3 (FLT3)** and **cyclin-dependent kinase 4 (CDK4)**, as well as exhibiting potent inhibition of **CDK6**. Its main mechanism is the inhibition of cell proliferation and survival in acute myeloid leukemia (AML) cells, particularly those harboring FLT3 mutations, including mutants that confer resistance to other FLT3 inhibitors. AMG 925 inhibits downstream signaling pathways such as STAT5 and RB phosphorylation, thereby inducing apoptosis in AML cell lines and in vivo tumor models. The drug is being investigated as a strategy to **overcome resistance** to current FLT3 inhibitors, and its antitumor activity is correlated with biomarkers of kinase inhibition. AMG 925 was developed by Amgen and has progressed into Phase 1 clinical trials for the treatment of AML[1][2][3][5][7][9].

Other names
1401033-86-0
02

Targets

CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)FLT3 (Fms related receptor tyrosine kinase 3)

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