MethylGene Inc. (TSX:MYG) today announced that preclinical data for its novel clinical-stage antifungal, MGCD290, was presented at the 52nd Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) taking place in San Francisco, California. The poster, entitled "MGCD290, an Oral Fungal Hos2 Inhibitor, Enhances the Antifungal Properties of Fluconazole following Multiple or Single Oral Dose Administration in Pre- and Post-Infection Settings" (Presentation #M-1711), demonstrated that MGCD290 plus fluconazole was superior to fluconazole alone in a murine model of systemic candidiasis under multiple dosing schedules.

Fluconazole is the most widely used triazole antifungal, and previous in vitro and in vivo studies have established that MGCD290 enhances the antifungal activity of fluconazole, broadening its spectrum of activity and increasing the sensitivity of fungi to fluconazole.

Today's poster details how, under different dosing schedules in a mouse model of systemic candidiasis, the combination of MGCD290 plus fluconazole significantly decreased the fungal kidney burden versus fluconazole alone. The combination of MGCD290 plus fluconazole was superior in both fluconazole-sensitive candidiasis and fluconazole-resistant candidiasis. Dosing schedules tested included a single dose of fluconazole plus MGCD290 administered after infection, or prophylactic dosing followed by a second post-infection treatment.

"The preclinical data reported today demonstrates the activity of MGCD290 under conditions relevant to mucosal and life-threatening systemic antifungal indications, as well as supporting the ability of MGCD290 to overcome azole resistance, an increasing problem." said Dr. Jeffrey Besterman, MethylGene's Executive Vice President, Research and Development and Chief Scientific Officer.

Enrollment in MethylGene's randomized, multicenter, blinded, placebo-controlled, Phase II trial in the U.S. is over 50% complete. This study is evaluating MGCD290 plus fluconazole versus fluconazole alone in patients with moderate to severe vulvovaginal candidiasis (VVC), a form of yeast infection for which current treatments have limited efficacy. Topline data from this trial is expected around the end of 2012.

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Tuesday, September 11, 2012
New antifungal drugs