Delving into the Latest Updates on BSG031 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target-

Action-

Mechanism-

Therapeutic Areas

Infectious Diseases

Active Indication-

Inactive Indication

Mycoses

Originator Organization

SINTEF Materials and Chemistry

Active Organization-

Inactive Organization

SINTEF Materials and Chemistry

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC47H73NO15

InChIKeyIQGJSAPAOXQRKO-BKZUNIJLSA-N

CAS Registry1114224-70-2

Seven polyene macrolides with alterations in the polyol region and exocyclic carboxy group were obtained via genetic engineering of the nystatin biosynthesis genes in Streptomyces noursei. In vitro analyses of the compounds for antifungal and hemolytic activities indicated that combinations of several mutations caused additive improvements in their activity-toxicity properties. The two best analogs selected on the basis of in vitro data were tested for acute toxicity and antifungal activity in a mouse model. Both analogs were shown to be effective against disseminated candidosis, while being considerably less toxic than amphotericin B. To our knowledge, this is the first report on polyene macrolides with improved in vivo pharmacological properties obtained by genetic engineering. These results indicate that the engineered nystatin analogs can be further developed into antifungal drugs for human use.

100 Deals associated with BSG031

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