Drug intelligence / Profile preview

guanidinoacetate

Development stage
Unknown
Modality
Small Molecules
Administration
Oral
01

Overview

Guanidinoacetate (GAA), also known as glycocyamine or 2-carbamimidamidoacetic acid, is a naturally occurring amino acid derivative synthesized from glycine and arginine in the kidneys by the enzyme L-arginine:glycine amidinotransferase (AGAT)[1][7]. It is a direct precursor to creatine via methylation by the enzyme guanidinoacetate methyltransferase (GAMT), primarily in the liver[1][4][7]. Creatine is crucial for energy storage and use, particularly in muscle and brain tissues[7]. GAA is used as a dietary supplement in humans, primarily for its role in creatine biosynthesis and for potential benefits in muscle and brain bioenergetics, although evidence for efficacy in healthy individuals is limited. In some trials, GAA-creatine supplementation improved functional outcomes in the elderly, but clinical use as a pharmaceutical is not widespread[5]. In agriculture, GAA is an approved feed additive for poultry and swine to improve weight gain and feed conversion, especially in vegetarian diets[1]. Metabolically, GAA conversion to creatine depletes methyl groups, which may lead to elevated homocysteine levels, raising concerns about cardiovascular and skeletal risks if not co-supplemented with methyl donors like betaine[1].

Brand names
no specific brand names identified for pharmaceutical or supplement use in humans; may be sold as GAA in animal nutrition markets
Other names
glycocyamineGAA2-carbamimidamidoacetic acidguanidinoacetic acid
02

Targets

GAMT (Guanidinoacetate N-methyltransferase)GABRR (GABA-A receptor subunit rho)

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