Delving into the Latest Updates on FR209603 with Synapse

Overview

Basic Info

Drug Type

Chemical drugs

Synonyms

Target

1,3-beta-glucan synthase

Action

inhibitors

Mechanism

1,3-beta-glucan synthase inhibitors

Therapeutic Areas

Infectious DiseasesOther Diseases

Active Indication-

Inactive Indication

AspergillosisCandidiasis

Originator Organization

Fujisawa Pharmaceutical Co., Ltd.

Active Organization-

Inactive Organization

Fujisawa Pharmaceutical Co., Ltd.

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC50H80N8O20S

InChIKeyJXFZOXKIGUVSTD-FIMXDVNNSA-N

CAS Registry785760-84-1

Novel antifungal lipopeptides, FR209602, FR209603 and FR209604, were isolated from the fermentation broth of a fungal strain No. 738 which was identified as Coleophoma crateriformis from morphological and physiological characteristics. The antibiotics were purified by solvent extraction, HP-20, YMC-ODS and silica gel column chromatography and lyophilization. These compounds were structurally similar to FR901379 previously reported by ourselves which had a sulfate residue in the cyclic peptide portion.

01 Mar 2006·The Journal of AntibioticsQ4 · MEDICINE

FR209602 and Related Compounds, Novel Antifungal Lipopeptides from Coleophoma crateriformis No. 738

Q4 · MEDICINE

Article

Author: Hashimoto, Seiji ; Furukawa, Shigetada ; Fujie, Akihiko ; Kanasaki, Ryuichi ; Abe, Fumie ; Hino, Motohiro ; Yoshikawa, Koji ; Hori, Yasuhiro

The biological activities of the novel echinocandin-like lipopeptides, FR209602, FR209603 and FR209604, were evaluated. These compounds showed antifungal activity against Candida albicans and Aspergillus fumigatus attributed to inhibition of 1,3-beta-glucan synthesis. The minimum effective concentrations of these compounds against C. albicans and A1. fumigatus ranged from 0.02 to 0.04 microg/ml by microbroth dilution assay, and the IC50 values on C. albicans 1,3-beta-glucan synthase were 0.49, 0.64 and 0.72 microg/ml, respectively. FR209602 and FR209603 showed good efficacy by subcutaneous injection against C. albicans in a murine systemic infection model, with ED50 values of 2.0 and 1.9 mg/kg, respectively.

100 Deals associated with FR209603

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