MethylGene Inc.
TSX : MYG

MethylGene Inc.

October 15, 2008 07:30 ET

MethylGene Initiates Phase I Clinical Study With MGCD290 for Fungal Infections

MONTREAL, QUEBEC--(Marketwire - Oct. 15, 2008) - MethylGene Inc. (TSX:MYG) today announced the administration of MGCD290 as a single agent to the first cohort of healthy adult volunteers in a Phase I clinical study. MGCD290 is an orally available fungal Hos2 inhibitor designed to be used in combination with azoles for the treatment of fungal infections. Azoles are a widely-prescribed class of drugs that comprise almost half of the approximately U.S. $5 billion worldwide antifungal market.

This double-blind, placebo-controlled Phase I study (Study 290-001), is expected to enroll up to 60 adult healthy volunteers. MGCD290 will be administered orally at an initial starting dose of 100mg and dosing levels will increase with each new cohort. The purpose of this trial is to evaluate MGCD290's safety, pharmacokinetics and tolerability.

"We continue to make progress with our proprietary product pipeline and are pleased to have advanced our antifungal program into human clinical trials. Our goal is to complete single and multiple dosing in this study followed by combination studies of MGCD290 and fluconazole in healthy volunteers," said Donald F. Corcoran, President and Chief Executive Officer of MethylGene. "In addition, we will evaluate potential partnering opportunities and funding requirements prior to advancing MGCD290 into Phase II trials."

In preclinical studies performed by key antifungal experts, the combination of MGCD290 with azoles increased the potency of the azole and expanded its antifungal spectrum of activity. In particular, the combination of MGCD290 and fluconazole broadened the spectrum of azole activity in vitro and increased fungal sensitivity to fluconazole in vitro and in vivo, including fluconazole-resistant clinical isolates.

"Opportunistic fungal infections are serious because they can invade every organ in the body," said Michael Pfaller MD, Professor Emeritus, Clinical Microbiology at the University of Iowa. "Azoles are a widely-used treatment for fungal infections; however, they have limitations and there is a medical need to broaden their antifungal spectrum, reduce their side effects and allow for more flexible dosing options. We are encouraged by the significant synergy we observed in our labs with MGCD290 in combination with various azoles in clinical-resistant fungal isolates. We look forward to presenting this data to the scientific community at the upcoming ICAAC/IDSA conference this month in Washington, DC."

About MGCD290

MGCD290 is an orally available, small molecule inhibitor that targets the fungal Hos2 enzyme. This compound was designed to be used in combination with azoles, a widely-prescribed class of drugs for the treatment of fungal infections. MGCD290 appears to potentiate and broaden the antifungal spectrum of azole activity against human fungal pathogens, including azole-resistant isolates.

The demand for more effective antifungals is driven by a rising incidence of invasive fungal infections in immunocompromised patients such as surgical patients, organ transplant patients and cancer patients undergoing chemotherapy or bone marrow transplants. Due to these more aggressive medical interventions, the frequency of invasive fungal infections has increased in this expanding patient population. Current antifungal agents are limited by an inadequate spectrum of activity, toxicities, drug-drug interactions and drug resistance. Emerging infections caused by certain Candida and Aspergillus species are particularly difficult to treat in immunocompromised patients and are associated with significant morbidity and mortality.

About MethylGene

MethylGene Inc. (TSX:MYG) is a publicly-traded, clinical stage, biopharmaceutical company focused on the discovery, development and commercialization of novel therapeutics for cancer. The Company's product candidates include: MGCD265, an oral, multi-targeted kinase inhibitor targeting the c-Met, Tie-2, Ron and VEGF receptor tyrosine kinases which is in Phase I clinical trials for solid tumor cancers; MGCD290, a fungal Hos2 (HDAC) inhibitor used in combination with azoles for fungal infections which is also in a Phase I clinical trial; and MGCD0103, an oral, isoform-selective HDAC inhibitor which has been in multiple clinical trials for solid tumors and hematological malignancies and is licensed to Celgene Corporation and Taiho Pharmaceutical. In addition, MethylGene's preclinical programs include: a kinase inhibitor program for ocular diseases and a sirtuin inhibitor program for cancer. MethylGene's development and commercialization partners include Celgene Corporation, Taiho Pharmaceutical Co. Ltd., Otsuka Pharmaceutical Co. Ltd. and EnVivo Pharmaceuticals. Please visit our website at www.methylgene.com.

Certain statements contained in this news release, other than statements of fact that are independently verifiable at the date hereof, may constitute forward-looking statements. Such statements, based as they are on the current expectations of management of MethylGene, inherently involve numerous risks and uncertainties, known and unknown, many of which are beyond MethylGene's control. These risks and uncertainties could cause future results, performance or achievements to differ significantly from the results, performance or achievements expressed or implied by such forward-looking statements. Such results, performance or achievements include, but are not limited to, the timing and effects of regulatory action; the continuation of collaborations; the results of clinical trials; the timing of enrollment or completion of clinical trials; the success, efficacy or safety of MGCD0103, MGCD265 or MGCD290; the ability to scale up, formulate and manufacture sufficient GMP, clinical or commercialization quantities of MGCD0103, MGCD265 or MGCD290, and the relative success or the lack of success in developing and gaining regulatory approval and/or market acceptance for any compound or new product including MGCD0103, MGCD265 or MGCD290. Such risks include, but are not limited to, the impact of general economic conditions, economic conditions in the pharmaceutical industry, changes in the regulatory environment in the jurisdictions in which MethylGene does business, stock market volatility, fluctuations in costs, expectations with respect to our intellectual property position and our ability to protect our intellectual property and operate our business without infringing upon the intellectual property rights of others, changes in the competitive landscape including changes in the standard of care for the various indications in which MethylGene is involved, and changes to the competitive environment due to consolidation, as well as other risks, which you are urged to read, as described in MethylGene's Annual Information Form for the fiscal year ending December 31, 2007, under the heading 'risk factors,', and all other documents filed by the Company that can be found at www.sedar.com. Consequently, actual future results may differ materially from the anticipated results expressed in the forward-looking statements. The reader should not place undue reliance on the forward-looking statements included in this presentation. These statements speak only as an update on the date they are made and MethylGene is under no obligation to revise such statements as a result of any event, circumstance or otherwise except in accordance with law.

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