On June 5, 2016 Tyrogenex, a privately held biopharmaceutical company, reported that data from its Phase I study of X-82, an oral dual anti-VEGFR/PDGFR tyrosine kinase inhibitor, with everolimus in solid tumors were presented at the American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) Annual Meeting 2016 held in Chicago, Illinois (Press release, Tyrogenex, JUN 5, 2016, View Source [SID:1234513093]).
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The data presented were from the Phase I study in which X-82 was combined with full dose everolimus in solid tumors to determine the dose limiting toxicities and recommended Phase II dose for pNET and RCC. Results were presented by Dr. Benjamin R. Tan, MD, Washington University School of Medicine, in a poster titled "Phase I study of X-82, an oral dual anti-VEGFR/PDGFR tyrosine kinase inhibitor, with everolimus in solid tumors."
"The results from this study provide critical information for moving forward with the development of X-82 in solid tumors," said Dr. Tan. "We have also seen favorable responses in renal cell carcinoma (RCC) and prolonged stable diseases (SD) in neuroendocrine tumors (NET) patients, which warrant further investigations in these tumor types. Tyrogenex continued to advances this program with the goal of providing patients suffering from a variety of solid tumors with a safe and effective treatment option."
About the Phase I Study
A 3+3 dose escalation design was utilized to determine the dose limiting toxicities and the recommended Phase II dose of daily oral X-82 plus everolimus at 10 mg PO daily for patients with solid malignancies. Key eligibility criteria included PS 0-1, measurable disease adequate organ function and normal LVEF.
Key conclusions from the study include:
Recommended Phase II dose is X-82 at 300 mg PO daily plus everolimus at 10 mg PO daily
Dose limiting toxicities include Grade 3 fatigue, mucositis and hypophosphatemia
Encouraging responses and prolonged stable disease seen in RCC and NETs
An expansion cohort for RCC and PNET are ongoing at Washington University and Vanderbilt University
About X-82
Tyrogenex’s lead compound is X-82. X-82 inhibits both VEGF and PDGFR. Tyrogenex believes X-82 targets the basic mechanisms of neovascular eye diseases, including angiogenesis, fibrosis and inflammation. X-82 is currently being evaluated for wet Age-Related Macular Degeneration (AMD) and solid tumors.