Drug intelligence / Profile preview

AG205

Development stage
Preclinical
Modality
Small Molecules
Administration
Intravenous, Intrathecal, Subcutaneous
01

Overview

AG205 is a **small molecule compound** initially identified as a ligand and antagonist of **progesterone receptor membrane component 1 (PGRMC1)**. It inhibits cell cycle progression and cell viability in cancer cell lines, disrupts progesterone-induced cytosolic calcium increases in GnRH neurons, and demonstrates anticancer effects in preclinical studies, particularly in breast cancer[1][2][3][4][5]. However, more recent research shows AG205 is not entirely specific and also inhibits sphingolipid biosynthesis (notably, reduces sulfatide and galactosylceramide levels), suggesting multiple cellular targets beyond PGRMC1[5]. Separately, AG205 has also been described as a potent inhibitor of the **FabK enoyl-acyl carrier protein reductase** in *Streptococcus pneumoniae*, showing antibacterial activity by disrupting fatty acid biosynthesis[7]. AG205 is used primarily as a research tool rather than a clinical drug; there is no evidence of clinical trials for AG205 in human subjects[6].

Brand names
AG205AG-205AG 205
Other names
AG205AG-205AG 205
02

Targets

PGRMC1UGT8 (UDP-galactose:ceramide galactosyltransferase)

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