SOURCEMGI PHARMA, Inc.

MINNEAPOLIS & MONTREAL-- MGI PHARMA, INC., (NasdaqMOGN - news) and MethylGene Inc., today announced the presentation of data regarding MG98 at this year's AACR-NCI-EORTC International Conference held in Miami Beach, Florida on October 29 - November 2, 2001. MG98 is a second-generation antisense oligonucleotide that inhibits the enzyme DNA methyltransferase. This conference is jointly sponsored by the American Association for Cancer Research (AACR), the National Cancer Institute (NCI), and the European Organization for the Research and Treatment of Cancer (EORTC).

"The role of DNA methylation in the causation and progression of human cancer is an area of very active recent research. Our research with our partner MethylGene on MG98 has demonstrated that selective inhibition of DNA methyltransferase results in tumor growth inhibition or tumor regression,'' notes Dr. Michael Cullen, vice president of clinical affairs and chief medical officer at MGI. "Targeting the re-expression of silenced tumor suppressor genes at the molecular level is considered one of the most exciting new approaches for cancer therapeutics today.''

A total of four posters were presented on the safety and antitumor activity of MG98. One presentation summarized the Phase 1 clinical experience with MG98 in patients with advanced or metastatic solid tumors. MG98 treatment was well tolerated with an improved side effect profile when compared to first-generation antisense oligonucleotides. Clear evidence of MG98 antitumor activity was observed in a patient with previously treated renal cell carcinoma that displayed an objective, partial tumor response of approximately 75 percent that was maintained for approximately one year on treatment. In addition, further evidence of MG98 antitumor activity was observed in two mesothelioma patients who displayed stable disease with durations of six and 14 months, respectively, while receiving MG98 treatment. (emphasis added).

One preclinical presentation reported the ability of MG98 to specifically inhibit the enzyme DNA methyltransferase-1, resulting in the re-expression of methylation-silenced tumor suppressor genes and causing inhibition of human tumor cell growth in both cell culture and animal models. A companion presentation highlighted the ability of combined administration of MG98 and 5-aza-deoxycytidine to produce synergistic reactivation of tumor suppressor genes as well as synergistic inhibition of human tumor cell growth in culture and in animal models. A fourth presentation reported a preclinical safety profile of MG98 in non-human primates that was very well tolerated.

About MG98

MG98 is a second-generation antisense oligonucleotide that targets mRNA for the nuclear enzyme DNA methyltransferase, which is responsible for silencing tumor suppressor genes. MGI and MethylGene are developing MG98 for the purpose of blocking production of DNA methyltransferase. Preventing DNA methyltransferase production may allow tumor suppressor genes that have been silenced by hypermethylation to be re-activated. MG98 is well tolerated and has already demonstrated anti-cancer activity in Phase 1 trials.

MGI and MethylGene initiated a Phase 2 trial of MG98 in head and neck cancer patients in November 2000, and initiated a Phase 2 trial of MG98 in renal cell carcinoma (kidney cancer) in August 2001. MGI and MethylGene intend to further evaluate MG98 in other cancers where silencing of tumor suppressor genes by DNA methyltransferase has been documented.

Along with MG98, MGI licensed a complementary small molecule inhibitor of DNA methyltransferase program that shares the same goal of preventing methylation and silencing tumor suppressor genes. The small molecules are being designed and screened for their potential to bind to DNA methyltransferase and block its activity, rather than prevent its production.

As part of MGI's agreement with its partner MethylGene Inc., MGI has the exclusive license to develop, market and sell in North America MG98 and any small molecule inhibitor of DNA methyltransferase derived from the two companies' cancer research collaborations. Earlier this year MGI and MethylGene announced the issuance of a key patent assigned to MethylGene entitled "Inhibition of DNA Methyltransferase'' (U.S. Patent No. 6,184,211). This patent provides significant intellectual property rights in the targeting of the enzyme as a therapeutic approach in cancer.

About MethylGene