MethylGene Initiates Phase I Clinical Trial For Its Multi-Targeted (c-Met) Kinase Inhibitor, MGCD265, In Solid Tumor Cancers

MethylGene Inc. recently announced the dosing of the first patient in a Phase I clinical trial of MGCD265 in patients with solid tumor cancers. MGCD265 is an oral, small molecule, multi-targeted kinase inhibitor that targets c-Met, VEGFR1, VEGFR2, VEGFR3, Tie-2 and Ron receptor tyrosine kinases. These kinases appear to play key roles in tumor development, tumor survival, and the inappropriate formation of blood vessels (angiogenesis) that nourish the tumor.

In this dose-escalating Phase I trial (Trial 102), MGCD265 is administered orally to patients at an initial starting dose of 24 mg/m² daily on an intermittent basis (every other week) for a 28-day cycle. The purpose of this trial is to evaluate the safety, pharmacokinetics, pharmacodynamics, and the maximum tolerated dose of MGCD265 in patients with advanced metastatic or unresectable solid tumors that are refractory to standard therapy. The trial is expected to enroll 20 to 60 patients and will be conducted at the Karmanos Cancer Institute in Michigan and at the MD Anderson Cancer Center in Houston. MethylGene expects to initiate a second MGCD265 Phase I clinical trial with an alternative dosing schedule in the same patient population during the second quarter of 2008.

"We are very excited to be involved in this Phase I study with MGCD265," said Dr. Patricia LoRusso, Professor of Medicine, Karmanos Cancer Institute. "The target profile of c-Met along with all three VEGFRs is rather unique and quite promising considering these pathways collaborate in growth of malignancies. Additionally, c-Met expression is increased in numerous solid tumors."

"We believe the inhibition of kinases, especially the c-Met target, is an important area in cancer research due to the involvement of the c-Met receptor in both tumor development and angiogenesis," said Donald F. Corcoran, President and Chief Executive Officer of MethylGene Inc. "Because MGCD265 is multi-targeted, we are attempting to inhibit cancer with one inhibitor via several key and separate mechanisms."

MethylGene Keynote Presentation for MGCD265 and its Multi-targeted Kinase Inhibitor Program

Dr. Jeffrey M. Besterman, Executive Vice President Research and Development and Chief Scientific Officer of MethylGene Inc., will be presenting an overview of the Company's multi-targeted kinase inhibitor program, including MGCD265, on Monday, May 5, 2008 during the 3rd Annual Protein Kinases in Drug Discovery Conference in San Diego.

About Kinases
Kinases are a large set of enzymes which regulate the transmission of signals in cells that control biological processes such as cell growth and differentiation. Many kinases exist and each one has a particular role in normal cell function. Receptor tyrosine kinases (RTKs) are a family of signaling kinases. Although required for normal cell functions, RTKs may be inappropriately regulated and play a role in tumor development and angiogenesis, RTKs may also be appropriate targets for diseases in which the aberrant formation of blood vessels is involved, such as ocular diseases.

About MethylGene
MethylGene Inc. is a publicly-traded, clinical stage, biopharmaceutical company focused on the discovery, development and commercialization of novel therapeutics for cancer. The Company's lead product, MGCD0103, is an oral isoform-selective HDAC inhibitor presently in multiple clinical trials for solid tumors and hematological malignancies, including Phase II monotherapy and Phase I, Phase I/II and Phase II combination trials with Vidaza, Gemzar and Taxotere. MGCD265 is an oral, multi-targeted kinase inhibitor targeting the c-Met, Tie-2, Ron and VEGF receptor tyrosine kinases in Phase I clinical trials for solid tumor cancers. In addition, MethylGene's preclinical programs include: MGCD290, an HDAC inhibitor in combination with azoles for fungal infections, a kinase inhibitor program for ocular diseases, and a sirtuin inhibitor program for cancer. MethylGene's development and commercialization partners include Celgene Corporation, Otsuka Pharmaceutical Co. Ltd., Taiho Pharmaceutical and EnVivo Pharmaceuticals. Please visit our website at www.methylgene.com.

SOURCE: MethylGene Inc.