Identification
Name Hydroxystilbamidine Isethionate
Accession Number DB01040 (APRD01024)
Type small molecule
Description Hydroxystilbamidine Isethionate is used in the therapy of some patients with nonprogressive blastomycosis of the skin, and pulmonary or systemic blastomycosis in children, with fewer side effects than amphotericin B. Hydroxystilbamidine Isethionate is also used in pathology for diagnostic purposes.
Structure
Categories (*)
Molecular Weight 532.588
Groups approved
Monoisotopic Weight 532.129769894
Pharmacology
Indication Used in the treatment of nonprogressive blastomycosis of the skin and other mycoses.
Mechanism of action Hydroxystilbamidine isethionate (HSB) acts on extracellular DNA and lysosomes. In Trypanosomes there is extensive and selective binding of HSB to the kinetoplastic DNA. This inhibits cell division and reproduction. In yeast there is evidence of binding to extranuclear DNA causing numerous mutations. HSB is also taken up in the lysosomes and leads to a significant increase in the number of lysosome-like bodies and secretion granules in trypanosomal organisms. HSB may also stabilize lysosomal membranes. HSB has also been found to bind RNA and is a powerful inhibitor of cellular ribonucleases.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms
  • Yeast, Molds, Trypanosomes
Interactions
Drug Interactions Not Available
Food Interactions Not Available
DNA
Name DNA
Gene Name Not Available
Pharmacological action yes
Actions other/unknown
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
  • Folds JD, Orlando G, Spitznagel JK: Immunosuppression by hydroxystilbamidine isethionate, a lysosome-stabilizing, anti-proteolytic, antifungal drug. Infect Immun. 1975 Mar;11(3):441-4. - Pubmed
DTHybrid score Not Available