MGCD265 is a rationally designed, orally administered small molecule kinase inhibitor that targets the receptor tyrosine kinases (RTKs) Met, VEGFR 1,2,3 and Axl, as well as Tie2 and Ron. RTKs are key kinases involved in cancer, angiogenesis (a process whereby new blood vessels are formed to nourish the tumors), tumor cell metastasis, tumor development and survival. Met expression is elevated and associated with tumorigenesis in several solid tumor indications including non-small cell lung cancer (NSCLC), gastric, prostate, colorectal, bladder, breast, renal, hepatocellular and ovarian cancers. Phase I/II studies of single agent MGCD265 and combinations with erlotinib or docetaxel are currently underway. More than 200 patients have been treated to date in clinical studies of both single-agent and combination therapy with docetaxel or erlotinib.
In the ongoing Phase I 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: