Drug intelligence / Profile preview

namoline

Development stage
Preclinical
Lead developer
University of Freiburg
Modality
Small Molecules
Administration
Oral
01

Overview

Namoline is a small molecule, reversible inhibitor of **Lysine-specific demethylase 1A (KDM1A)**, also known as **LSD1**. It was identified as a chemical probe that targets the catalytic activity of LSD1, an epigenetic enzyme frequently overexpressed in various cancers, including prostate cancer. Namoline specifically impairs the ability of LSD1 to act as a co-activator for the **androgen receptor (AR)**, leading to the downregulation of androgen-responsive genes. Research indicates that namoline can inhibit the proliferation and invasion of prostate cancer cells, particularly when used in combination with other epigenetic inhibitors like KDM5 inhibitors (e.g., CPI-455). It was primarily developed by researchers at the **University of Freiburg** to explore the therapeutic potential of targeting histone demethylases in castrate-resistant prostate cancer (CRPC).

02

Targets

KDM1A (LSD1)

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