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beta-guanidinopropionic acid
- Development stage
- Unknown
- Lead developer
- Inspirna
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Beta-guanidinopropionic acid (β-GPA) is a small molecule, orally active creatine analogue that acts as a competitive inhibitor of the ATP-regenerating enzyme creatine kinase (CK). By inhibiting CK, it depletes intracellular phosphocreatine and ATP levels, which in turn activates the AMP-activated protein kinase (AMPK) pathway. This mechanism has been explored for multiple therapeutic applications: in hypertension, it is studied for its ability to lower blood pressure by reducing CK activity; in metabolic disorders, it increases insulin sensitivity via GLUT4 upregulation; and in oncology (specifically colorectal cancer), it targets the SLC6A8 creatine transporter to inhibit energy metabolism in tumor cells. It has been investigated in clinical trials by the Academisch Medisch Centrum (Amsterdam UMC) for hypertension and by Inspirna (as RGX-202/ompenaclid) for cancer.
- Other names
- ompenaclid3-guanidinopropionic acidbeta-GPAN-(aminoiminomethyl)-beta-alanine
02
Targets
AMPK (Adenosine monophosphate–activated protein kinase)SLC2A4 (Solute carrier family 2 facilitated glucose transporter member 4)SLC6A8 (Sodium- and chloride-dependent creatine transporter 1)
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