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news.Exelixis has reported encouraging data from an ongoing Phase I trial of a potent inhibitor of MET, RET, and VEGFR kinases, in patients with advanced solid tumors or lymphoma.
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Consistent with the anti-VEGFR activity of XL184, preliminary pharmacodynamic analyses show reductions in several biomarkers of angiogenesis. Anti-tumor activity has been observed in a variety of cancers at doses that are not associated with significant toxicity.
Preliminary analyses of pharmacodynamic samples show changes in VEGF-A, sVEGFR2 and PIGF consistent with effects observed with other antiangiogenic agents. Preliminary pharmacokinetic analyses of nine dose levels (0.08-11.52 mg/kg) indicate a long half-life of XL184 of 59 to 136 hours.
George Scangos, president and CEO of Exelixis, said: “In this study of XL184, we observed partial responses in patients with medullary thyroid cancer and tumor shrinkage in a patient with papillary renal cell cancer, which frequently have mutational activation or overexpression of RET or MET, respectively. We believe the data to date demonstrate the potential of simultaneous inhibition of MET, RET, and VEGFR, and validate our ability to discover and develop compounds that simultaneously inhibit critical pathways in cancer. We intend to advance XL184 into a phase II program by the end of 2007.”