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MGCD-265 is a multi-target and ATP-competitive inhibitor of c-Met and VEGFR1, 2, 3 with IC50 values of 1 nM, 3 nM, 3 nM and 4 nM, respectively. [1]

In Non-small cell lung cancer xenograft models including one that harbored the TKI resistant EGFR mutation T790M, MGCD265 combined with either paclitaxel, docetaxel or erlotinib. Each combination elicited greater tumor response than agent alone, and displayed antiangiogenic properties with docetaxel [2].

MGCD265 has been studied in a variety of advanced solid tumors including NSCLC, as a monotherapy and in combination with either docetaxel or erlotinib. In a phase I study, MGCD265 was given orally from 24 mg/m2 daily to 235 mg/m2 twice daily uninterrupted to patients with advanced solid malignancy until disease progression [3]. In a phase I standard 3+3 dose escalation, MGCD265 (96 mg/m2 once daily up to 162 mg/m2 bid) was combined with erlotinib at 100 or 150 mg daily to determine safety, and 45 patients have been enrolled. In a separate phase I dose escalating trial, MGCD265 was combined with docetaxel (50 then 75 mg/m2 iv once every 3 weeks) in advanced solid tumors (n=34), including 9 NSCLC patients. The MTD of the microionized formulation of MGCD265 is 72 mg/m2 bid and docetaxel 75 mg/m2 every 3 weeks but has not been reached with the new formulation. [4][5]

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