Xcovery Presents Phase 1 Clinical Results at American Society of Clinical Oncology Annual Meeting

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X-82 Mechanism of Action

WEST PALM BEACH, FL and CHICAGO, IL--(Marketwire - June 04, 2012) - Xcovery, a developer of next-generation targeted therapeutics for cancer, today announced preliminary data presented from its Phase 1 clinical study which evaluated X-82, an oral VEGFR tyrosine kinase inhibitor (TKI), in patients with advanced solid tumors. The data were presented today in a poster presentation at the American Society of Clinical Oncology's (ASCO) Annual Meeting.

The preliminary data show that X-82 is well tolerated and preliminary signs of anti-tumor activity (7/16 on study ≥16wks; 1 complete response) exist. In addition, X-82 has a short half-life ( < 8 hours), with target inhibition levels of 100ng/ml achieved at all except the lowest dose, though they were not sustained for a full 24 hrs. Maximum tolerated dose and recommended Phase 2 dose have not been determined at this preliminary phase.

VEGFR tyrosine kinase inhibitors have characteristically demonstrated benefit in a variety of cancers, though it has been well documented that the dosage and use of this class in combination with other therapies has been limited by side effects. The X-82 data show that typical VEGFR-TKI related toxicities appear to be minimal. Intermittent inhibition of target, due to the short half-life, may explain the lack of significant toxicity.

"While the results shown on X-82 are preliminary, we are encouraged by the unique pharmacokinetic and pharmacodynamics properties," said Dr. Chris Liang, Executive Vice President and Chief Scientific Officer of Xcovery. "The data support our hypothesis that our dual VEGFR/PDGFR inhibitor X-82 has a low toxicity profile and will be a differentiated and ideal product candidate for combination therapy."

Johanna Bendell, M.D. of the Sarah Cannon Research Institute was the principal investigator on the study. A copy of the poster, "A Phase I First in Human Trial of an Oral VEGFR Tyrosine Kinase Inhibitor (TKI), X-82, in Patients with Advanced Solid Tumors," can be obtained at www.xcovery.com.

About Xcovery's Phase 1 Study
Sixteen patients with advanced solid tumors were enrolled using an accelerated titration scheme followed by 3+3 dose escalation design. X-82 was administered orally once daily (QD) or twice daily (BID) every 28 days. Patients were treated across eight dose levels: 20 (n=1), 40 (n=1), 80 (n=1), 160 (n=1), 300 (n=2), 400 mg QD (n=3), 140 mg BID (n=3) and 200 mg BID (n=4). The most common related adverse events (AEs) by patient were fatigue (4 G1, 1 G2), nausea (3 G1, 1 G2), diarrhea (3 G1), anorexia (1 G1, 1 G2), and vomiting (2 G1). G2 hypertension, resolved with treatment, was experienced by one patient. The maximally tolerated dose and recommended Phase 2 dose remain to be determined.

About Xcovery
Xcovery is a clinical-stage company focused on the development of next-generation targeted therapeutics for cancer. Founded by Sheridan G. Snyder and Chris Liang, PhD, Xcovery's vision is to successfully develop innovative oncology therapies to optimize patient outcomes. Through innovative drug design, Xcovery has developed a comprehensive pipeline of oncology therapies that target a wide range of advanced tumors. X-82 was developed by Tyrogenex, an Xcovery company, funded by Biocatalyst International.