Overview
About MGCD265.
MGCD265 is a novel targeted cancer therapeutic discovered by MethylGene that inhibits the Met and VEGF receptor tyrosine kinases. The abnormal activation of Met is involved in tumor development, metastasis and survival and the VEGF kinase is responsible for the inappropriate formation of blood vessels (angiogenesis) that nourish the tumor. In preclinical studies, MGCD265 demonstrated nanomolar potency in enzyme and cellular assays and up to 100% of tumor growth inhibition in a broad range of xenograft models.
Clinical Status.
In the ongoing Phase 1 program, MGCD265 is being administered orally in patients with advanced cancers. The compound has demonstrated a favorable safety profile and can be combined safely with other cancer therapeutics such as docetaxel (Taxotere®) and erlotinib (Tarceva®). These therapeutics were selected for combination studies based on preclinical data that demonstrated the combination of MGCD265 and erlotinib and of MGCD265 and docetaxel showed greater anti-tumor activity compared to each drug administered alone. To date, the Company has initiated three clinical studies:
MGCD265 Clinical Trials.
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Next Steps.
MethylGene is pursuing the evaluation of MGCD265 in three cancer indications: non-small cell lung (NSCLC), gastric and prostate. The protocols for trials 265-101 and 265-103 have been amended to include expansion cohorts and an optimized formulation and patient enrollment has begun. The Company expects to report data from these trials in 2012.
Statistics. 1
Lung Cancer
In the United States, an estimated 221,130 new cases of lung cancer are expected in 2011, which accounts for about 14% of cancer diagnoses. Lung cancer accounts for more deaths than any other cancer in both men and women. An estimated 156,940 deaths, accounting for approximately 27% of all cancer deaths are expected to occur in 2011.
Gastric Cancer
Gastric cancer is a cancer that forms in the tissues that line the stomach. In the United States, an estimated 21,520 news cases of gastric cancer are expected to be diagnosed in 2011 with deaths estimated at 10,340.
Prostate Cancer
Prostate cancer forms in tissues of the prostate and is the most frequently diagnosed cancer in men. It is estimated that 240,890 new cases will be diagnosed and 33,720 deaths will occur in the United States in 2011.
1. American Cancer Society, Cancer Facts & Figures 2011