Drug intelligence / Profile preview

Guanoxabenz

Development stage
Discontinued
Lead developer
Orfenix
Modality
Small Molecules
Administration
Oral, Sublingual, Intravenous
01

Overview

Guanoxabenz is an N-hydroxyamidinohydrazone that functions as a prodrug for the alpha-2 adrenoceptor agonist guanabenz. It undergoes enzymatic reduction by various systems, including mitochondrial amidoxime reducing component (mARC) proteins, xanthine oxidase, and microsomal enzymes, to form the active metabolite guanabenz. This conversion is crucial as guanabenz exhibits significantly higher affinity for alpha-2 adrenoceptors and is responsible for the drug's antihypertensive effects. Guanoxabenz itself has been shown to have mutagenic potential, which is mitigated upon its reduction to guanabenz.

Brand names
Benzérial
Other names
1-(2,6-dichlorobenzylidene-amino)-3-hydroxyguanidine
02

Targets

MTARC1 (Mitochondrial amidoxime-reducing component 1)MTARC2 (Mitochondrial amidoxime reducing component 2)

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