Author: Predrag Novak ; Igor Bratoš ; Predrag Tepeš ; Miljenko Dumić ; Zdenko Hameršak ; Amir Avdagić ; Marina Ilijaš ; Vesna Gabelica Marković ; Ines Fistrić

Successful use of LC-NMR and LC-MS for rapid identification of an impurity in a novel antifungal drug icofungipen has been demonstrated. Complementary information obtained from the two methods made it possible to determine the structure of A1 prior to its isolation and purification. Stop-flow LC-NMR ((1)H and DQFCOSY), LC-MS and LC-MS/MS spectra have shown that A1 is structurally related to icofungipen. It was later isolated and prepared synthetically and its structure was corroborated by high-resolution NMR spectroscopy.

01 Sep 2006·Antimicrobial Agents and ChemotherapyQ2 · MEDICINE

In Vitro Activity and In Vivo Efficacy of Icofungipen (PLD-118), a Novel Oral Antifungal Agent, against the Pathogenic Yeast Candida albicans

Q2 · MEDICINE

Article

Author: Ergović, Gabrijela ; Geschke, Ulrich ; Mittendorf, Joachim ; Schmidt, Axel ; Skerlev, Mihael ; Hasenoehrl, Andreja ; Maršić, Nataša ; Schoenfeld, Wolfgang ; Galić, Tatjana

ABSTRACT Icofungipen (PLD-118) is the representative of a novel class of antifungals, beta amino acids, active against Candida species. It has been taken through phase II clinical trials. The compound actively accumulates in yeast, competitively inhibiting isoleucyl-tRNA synthetase and consequently disrupting protein biosynthesis. As a result, in vitro activity can be studied only in chemically defined growth media without free amino acids that would compete with the uptake of the compound. The MIC of icofungipen was reproducibly measured in a microdilution assay using yeast nitrogen base medium at pH 6 to 7 after 24 h of incubation at 30 to 37°C using an inoculum of 50 to 100 CFU/well. The MICs for 69 Candida albicans strains ranged from 4 to 32 μg/ml. This modest in vitro activity contrasts with the strong in vivo efficacy in C. albicans infection. This was demonstrated in a lethal model of C. albicans infection in mice and rats in which icofungipen showed dose-dependent protection at oral doses of 10 to 20 mg/kg of body weight per day in mice and 2 to 10 mg/kg/day in rats. The in vivo efficacy was also demonstrated against C. albicans isolates with low susceptibility to fluconazole, indicating activity against azole-resistant strains. The efficacy of icofungipen in mice and rats was not influenced by concomitant administration of equimolar amounts of l -isoleucine, which was shown to antagonize its antifungal activity in vitro. Icofungipen shows nearly complete oral bioavailability in a variety of species, and its in vivo efficacy indicates its potential for the oral treatment of yeast infections.

01 Aug 2005·Current opinion in investigational drugs (London, England : 2000)

Icofungipen (PLIVA).

Review

Author: Yeates, Clive

Icofungipen is a cyclic beta-amino acid being development by PLIVA, under license from Bayer, for the potential oral treatment of fungal infection. As of September 2002, the first phase II efficacy study was underway.

100 Deals associated with Icofungipen

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Indication	Highest Phase	Country/Location	Organization	Date
Candidiasis	Phase 1	-	Teva Pharmaceutical Industries Ltd.	-
Candidiasis	Phase 1	-	Bayer AG	-
Candidiasis	Phase 1	DE	-	-
Candidiasis, Vulvovaginal	Phase 1	US	-	-

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