Drug intelligence / Profile preview

pyrazofurin

Development stage
Preclinical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravenous, Subcutaneous
01

Overview

Pyrazofurin is a pyrimidine nucleoside analogue originally isolated from *Streptomyces candidus*. It functions as an antimetabolite by inhibiting key enzymes in the de novo pyrimidine biosynthesis pathway, specifically orotidine 5'-monophosphate (OMP) decarboxylase (also known as UMP synthase) and orotate-phosphoribosyltransferase. This inhibition leads to a depletion of uridine nucleotides, subsequently blocking DNA synthesis and cell proliferation. Pyrazofurin exhibits antitumor, antiviral, and antibiotic properties. While it was previously evaluated in human clinical trials for cancer, these efforts were largely unsuccessful due to severe side effects. However, recent research has identified pyrazofurin as a potential candidate for repurposing, particularly for the treatment of Hepatitis E virus infections.

Other names
pirazofurinpyrazomycin4-Hydroxy-5-β-D-ribofuranosyl-1H-pyrazole-3-carboxamide
02

Targets

OPRT (Orotidine 5'-phosphate decarboxylase)

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