Xcovery Presents Phase 1 Clinical Results at Asco Annual Meeting
Study is First-in-Human Trial of an Oral VEGFR Tyrosine Kinase
Inhibitor (TKI) in Patients with Advanced Solid Tumors
West Palm Beach, FL & Chicago, IL June 4, 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.
Media Contact:
Amanda Murphy or Donna LaVoie
LaVoie Group
Office: 978.745.4200 x107/ x103
amurphy@lavoiegroup.com
dlavoie@lavoiegroup.com
Business Development Contact:
Cheryl Calhoun
Vice President
561.659.1945
cheryl@xcovery.com
Posted: June 2012
