Drug intelligence / Profile preview

sparsomycin

Development stage
Discontinued
Lead developer
National Cancer Institute
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Sparsomycin is a cytotoxic antitumor antibiotic originally isolated from the bacterium Streptomyces sparsogenes. It acts as a potent inhibitor of protein synthesis by binding to the large (50S) ribosomal subunit and blocking peptide bond formation through inhibition of peptidyl transferase activity. Sparsomycin inhibits protein synthesis in both prokaryotic (70S) and eukaryotic (80S) ribosomes. While it demonstrated broad-spectrum in vitro activity against various tumor cell lines and was investigated for anticancer use, its clinical development was halted due to significant toxicity—most notably retinopathy observed during early human trials. Today, it is primarily used as a research tool to study mechanisms of translation and ribosome function[1][2][3][4][5][7].

Other names
sparsomycinesparsomicinasparsomycinesparsomycinum
02

Targets

PTC (50S ribosomal peptidyl transferase center)

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