Drug intelligence / Profile preview

hydroxystilbamidine

Development stage
Unknown
Modality
Small Molecules
Administration
Intravenous, Intracerebral, Intraperitoneal
01

Overview

Hydroxystilbamidine is a synthetic diamidine compound with antifungal, antitrypanosomal, antimalarial, and carcinostatic activities. It acts primarily by binding to DNA and RNA in a non-intercalating manner and inhibiting ribonucleases. In protozoa such as trypanosomes, it binds selectively to kinetoplastic DNA and inhibits cell division. In yeast and other organisms it can bind extranuclear DNA causing mutations. Hydroxystilbamidine also accumulates in lysosomes where it may stabilize lysosomal membranes or increase the number of lysosome-like bodies. Clinically, it was used for the treatment of blastomycosis (a fungal infection) and leishmaniasis but has largely been replaced by amphotericin B due to safety concerns. Additionally, its fluorescent properties have led to its use as a retrograde neuronal tracer under the name Fluoro-Gold[1][2][3][4][5][7][8].

Other names
hydroxystilbamidine isethionatehydroxystilbamidine diisethionateFluoro-Gold2-hydroxy-4,4'-stilbenedicarboxamidine bis(2-hydroxyethanesulfonate)hydroxystilbamide
02

Targets

kDNA (Kinetoplast DNA)cfDNA (Cell-free DNA)

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