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MethylGene Unveils HDAC Anti-Fungal Program

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MethylGene Unveils HDAC Anti-Fungal Program

12/16/2005 7:30:00 AM EST

http://www.genengnews.com/news/bnitem.aspx?

name=1128445XSL_NEWSML_TO_NEWSML_WEB.xml

MethylGene Inc. (TSX:MYG) a biopharmaceutical company, today

disclosed in two posters, preclinical results demonstrating the

potential use of an isotype-selective histone deacetylase (HDAC)

inhibitor in human fungal infections at the Interscience Conference

on Antimicrobial Agents and Chemotherapy (ICAAC) in Washington DC.

The Company described data from in vitro and in vivo experiments,

which demonstrate that:

-- Development of resistance to azole antifungal drugs may occur by

an HDAC mediated mechanism;

-- MethylGene's inhibitors may be more selective for fungal HDACs

than for the human ones: an important therapeutic prerequisite;

-- Enhanced activity and potency of current azole treatments against

key fungal pathogens occurs when these drugs are co-administered

with MethylGene's HDAC inhibitor;

-- MethylGene's HDAC inhibitor enhances the azole susceptibility of

otherwise drug-resistant fungi;

-- MG3290, when co-administered with ketoconazole (an azole),

significantly decreases the extent of fungal infection and increases

animal survival in a dose dependent manner; and

-- A lower dose of azoles can be given, when co-administered with

MethylGene's HDAC inhibitor. This may reduce the potential for

adverse azole drug to drug interactions.

" We believe that our compounds specifically target fungal HDACs.

This means that we may be able to develop a therapeutic allowing

current azoles to be more effective, " noted F. Corcoran,

President and CEO of MethylGene, " These experiments further validate

our approach of discovering and developing novel HDAC isotype-

selective inhibitors. We continue to aggressively push this program

forward with the goal of identifying a clinical candidate over the

next 12-18 months. "

Unlike the other comparator HDAC inhibitors tested, MethylGene's

HDAC inhibitors are: i) able to penetrate pathogenic fungi, and ii)

more specific against their targets. In addition, it appears in

vitro that co-administration of MethylGene's HDAC inhibitors with

certain azoles is effective against fungi typically insensitive to

azole treatment alone.

Details regarding these experiments can be found in two posters,

available on MethylGene's web site, presented at ICAAC

entitled, " Synergism of Histone Deacetylase (HDAC) Inhibitors with

Ketoconazole in Candida albicans and Candida glabrata. Relationship

to Their Effects on HDAC Activity in Protoplasts " (Abstract M-2154)

and " Synergism of Histone Deacetylase (HDAC) Inhibitors with

Ketoconazole in Aspergillus fumigatus. Relationship to Inhibitory

Effects on HDAC Activity in Protoplasts " (Abstract M-2165)

About Fungal Infections

Serious infections with yeasts and other fungi often occur in

hospital settings as a complication in immunocompromised patients.

Fungal infections are commonly treated with a class of drugs called

azoles. However, not all human fungal pathogens are susceptible to

azole antifungal medications and resistance is an increasing

problem. Infections caused by Candida and Aspergillus are especially

common and difficult to manage medically. Aspergillosis has a high

mortality rate and is an underserved market. In 2004, the market of

systemic antifungal drugs was estimated to be $5 billion USD

worldwide with azole sales being a major contributor to that market.

About MethylGene

MethylGene is a publicly-traded biopharmaceutical company focused on

the discovery, development and commercialization of novel

therapeutics in cancer and infectious disease. Two cancer product

candidates are currently in clinical trials: MGCD0103, partnered

with Taiho Pharmaceutical for certain Asian countries, and MG98,

partnered with MGI Pharma for North America. MethylGene has an

exclusive license agreement with Merck & Co. for the development and

commercialization of small molecule beta-lactamase inhibitors to

overcome antibiotic resistance. MethylGene has a portfolio of

preclinical programs for its multi-targeted kinase and histone

deacetylase (HDAC) inhibitors for both oncology and non-oncology

indications, and continues to seek partnering opportunities in these

areas. (www.methylgene.com.)

Except for historical information, this news release may contain

forward-looking statements, which reflect the Company's current

expectation regarding future events. These forward-looking

statements involve risk and uncertainties,(which can be found in the

Company's Annual Information Form dated December 31, 2004, and can

be found on www.sedar.com) which may cause but are not limited to,

changing market conditions, the successful and timely completion of

clinical studies, the establishment of corporate alliances, the

impact of competitive products and pricing, new product development,

uncertainties related to the regulatory approval process and other

risks detailed from time to time in the Company's ongoing quarterly

and annual reporting.

CONTACT:

MethylGene Inc. F. Corcoran President & CEO (514) 337-3333

ext. 224 Fax: (514) 337-0550 corcorand@... or

Gilpin, Ph.D. Director, IR & Project Mgmt (514) 337-3333 ext. 416

Fax: (514) 337-0550 gilpina@...

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