METHYLGENE PRESENTS MGCD265 DATA AT THE 2012 AMERICAN SOCIETY OF CLINICAL ONCOLOGY (ASCO) ANNUAL MEETING
Montreal, Canada. June 4, 2012 – MethylGene Inc. (TSX:MYG) today announced that clinical data for its Met/VEGFR multi- kinase inhibitor MGCD265 was presented in a poster session at the 2012 ASCO Annual Meeting held in Chicago, Illinois. The poster, entitled “MGCD265, a multitargeted oral tyrosine kinase receptor inhibitor of Met and VEGFR: Dose-escalation Phase I study” (Abstract #3039) provided an interim update on the monotherapy trial 265-101.
Trial 265-101 is an ongoing Phase I, multicenter, open-label trial. In this trial patients are treated with MGCD265 alone, dosed orally every day over a 21 day cycle. Data was presented on 57 patients with advanced metastatic or unresectable solid malignancies that were refractory to standard therapy and/or unlikely to derive clinical benefit from existing therapies.
In an ex vivo system designed to assess the biological activity of MGCD265 using plasma samples from study patients, increased plasma concentration of MGCD265 was associated with inhibition of Met phosphorylation in a dose-dependent manner, suggesting coverage of the biological target, Met, in the clinical setting.
Stable disease was observed in 23 patients (of a total of 57 enrolled). No objective responses were observed to date. MGCD265 continues to be well-tolerated. Adverse events were mostly mild to moderate at all doses tested. The most frequent treatment-related adverse events (all grades) included diarrhea, anorexia, nausea, fatigue and vomiting. Seven (7) treatment-related grade 3 events were reported and of these, 3 were considered dose-limiting: fatigue, pituitary hemorrhage and elevated lipase. All dose limiting events occurred in cycle 1 at daily doses ≥ 250 mg/m2.
“The safety profile of MGCD265 continues to be favorable at exposures that show pharmacodynamic and biological effect”, said Dr. Rachel Humphrey, Executive Vice President and Chief Medical Officer of MethylGene Inc. “We continue to be excited about the potential for MGCD265, both as a monotherapy and in combination with other anti-cancer agents.” Dose escalation continues in trial 265-101 and final data will be presented at a future medical meeting. A series of expansion cohorts is planned when the maximum tolerated dose is determined.
MGCD265 is a novel, oral small molecule inhibitor that targets a unique spectrum of receptor tyrosine kinases: Met, VEGFR 1, 2, and 3, Tie-2 and Ron. These kinases play key roles in tumor development, survival and metastasis as well as the inappropriate formation of blood vessels (angiogenesis) that nourish the tumor. MGCD265 has completed one Phase 1 single agent study, and is nearing completion of one Phase 1 single agent clinical trial and one Phase 1/2 combination clinical trial (with erlotinib and docetaxel) in solid tumors.
MethylGene Inc. (TSX:MYG) is a small molecule drug development company that is advancing two 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 currently in Phase 2 trials for vulvovaginal candidiasis, and MGCD265, an oral Met/VEGF receptor kinase inhibitor that is in Phase 1/2 clinical trials for solid tumor cancers. 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.