Montreal, Canada, October 22, 2012 – MethylGene Inc. (TSX: MYG) today announced that Phase I data for its novel clinical-stage antifungal, MGCD290, were presented at the 2012 IDWeek™ meeting, held in San Diego, California from October 17-21, 2012. Data describing the safety and pharmacokinetics of MGCD290 in four Phase I clinical trials in healthy adult volunteers were presented in a poster entitled “Safety and Pharmacokinetics of MGCD290, an Oral fungal Hos2 Inhibitor, Alone and in Combination with Fluconazole: Single and Multiple Ascending Dose Studies in Healthy Subjects (290-001, 002, 003, 004)” (presentation #1619).
Previous preclinical studies have established that MGCD290 enhances the antifungal activity of fluconazole, broadening its spectrum of activity and increasing the sensitivity of fungi to fluconazole. Data presented at the 2012 IDWeek™ described the safety profile of MGCD290 in humans under different dosing schedules and in the presence or absence of fluconazole. MGCD290 monotherapy was tested up to 1000 mg as a single dose and up to 540 mg daily in 14 day repeat dose studies (studies 290-001, 290-002). MGCD290 in combination with 150 mg fluconazole was tested up to 540 mg daily for 14 days (studies 290-003, 290-004). All doses and schedules tested were well tolerated, with no severe or serious adverse events reported. Pharmacokinetics were dose-dependent and MGCD290 demonstrated a large apparent volume of distribution and good tissue penetration. No drug-drug interactions were observed between MGCD290 and fluconazole.
“Data from these Phase I studies indicate that MGCD290 has an attractive pharmacokinetic and safety profile, supporting its ongoing clinical development,” said Dr. Rachel Humphrey, Executive Vice President and Chief Medical Officer of MethylGene. “We continue to be encouraged by the potential of this drug for vulvovaginal candidiasis and other indications such as systemic or invasive fungal infections.”
A randomized, placebo-controlled, double-blind, multi-center, Phase II trial is underway to evaluate MGCD290 plus fluconazole versus fluconazole alone in patients with moderate to severe vulvovaginal candidiasis (VVC). Topline data from this trial is expected in Q1 2013.
MGCD290 is a first-in-class, orally available, small molecule inhibitor of the fungal enzyme Hos2. In preclinical models the combination with azole antifungal agents results in broader coverage of fungal pathogens and decreases resistance to the most widely used antifungal agents. MGCD290 is being developed as a combination product with fluconazole, the most widely used triazole antifungal. In vitro, MGCD290 in combination with fluconazole reverses fluconazole resistance (primary and acquired) in a wide range of fungal species, including Candida glabrata. MGCD290 has completed multiple Phase I studies in healthy adult volunteers and has shown an excellent safety profile without drug-drug interactions in combination with fluconazole. A randomized, controlled Phase II study in moderate to severe VVC is underway.
MethylGene Inc. (TSX:MYG) is a drug development company that is advancing novel therapeutics for cancer and infectious disease in human clinical trials. The Company’s lead product candidates are: MGCD290, an oral antifungal agent targeting the fungal Hos2 enzyme that is in Phase II trials for vulvovaginal candidiasis, and MGCD265, an oral Met/VEGF receptor kinase inhibitor that is in Phase I/II clinical trials for patients with solid tumors. MethylGene owns all rights to its lead product candidates, and has partnerships with Otsuka Pharmaceutical Co. Ltd., Taiho Pharmaceutical Co. Ltd., and EnVivo Pharmaceuticals, Inc. for its other pipeline programs.
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