Cylene Pharmaceuticals Initiates Phase I Trial With CX-4945 -Breakthrough
First-in Class Inhibitor of CK2
SAN DIEGO, Jan. 5 /PRNewswire/ -- Cylene Pharmaceuticals announced today that
it has initiated a Phase I clinical trial of its oral CK2 protein kinase
inhibitor, CX-4945, in patients with advanced solid tumors, Castleman's
disease, or multiple myeloma. The primary endpoints of the oral dose
escalating trial are determination of safety, tolerance and PK properties of
CX-4945 and to select the appropriate dose for Phase II trials. In addition,
multiple mechanism-related pharmacodynamic biomarkers that were validated in
preclinical studies will also be evaluated in the trial to assess the ability
of CX-4945 to hit its target in patients.
CX-4945 is a first-in-class, orally administered small molecule anticancer
agent that delivers highly selective and potent inhibition of CK2, a
constitutively active protein kinase that is overexpressed in a wide range of
cancers. CK2 drives the excessive proliferation phenotype of cancer cells
through its potentiating role in key cell survival pathways and angiogenesis.
CX-4945 demonstrates potent tumor regression activity in murine xenograft
models, as well as favorable PK/ADMET and safety properties in preclinical
studies.
"CX-4945 is a breakthrough molecule for Cylene," said Dr. William Rice,
President and Chief Executive Officer of Cylene Pharmaceuticals. "CK2
overexpression drives key cell survival pathways and proliferation of cancer
cells, but it has been notoriously difficult to inhibit because it has an
unusual active site. CX-4945 represents the first potent and selective
inhibitor of CK2 with a favorable safety profile and the ability to promote
tumor regressions as a single agent in preclinical studies. We are delighted
to have advanced CX-4945 into the clinic ahead of schedule, and we are
thoughtfully planning our Phase II program in particular CK2 driven cancers."
In this Phase I trial, CX-4945 will be administered to patients orally twice a
day, for three consecutive weeks of a four week cycle, over a range of doses.
The primary objectives of the study will be to determine the maximum tolerated
dose (MTD) and dose limiting toxicities (DLTs) of CX-4945, and to define the
phase II dose. The secondary objectives are to characterize the
pharmacokinetics, as well as observe for signs of anti-tumor activity via
pharmacodynamic as well as radiographic assessments.
"CK2 is of central importance in driving cancer cell proliferation as well as
in angiogenesis. As such, CX-4945 is a truly novel therapeutic, particularly
against cancers and in other indications mediated by IL-6 and IL-8," added Dr.
Daniel Von Hoff, Cylene's Co-Founder and Vice President, Medical Affairs.
About CX-4945, an oral CK2 protein kinase inhibitor
CX-4945 is a first-in-class small molecule that has been optimized to
selectively inhibit CK2 activity. The CK2 protein kinase plays a
multifunctional role in cell cycle regulation, signal transduction,
transcriptional control, angiogenesis, apoptosis and inflammation. Because CK2
contributes to the cancer phenotype via multiple cellular events, CX-4945 has
been designed with the objective of creating a multifunctional inhibitor by
targeting a single protein and affecting potentially many cancers. CX-4945
demonstrates broad spectrum anti-proliferative activity against diverse cancer
cell lines, and the data attribute the anti-tumor activity of CX-4945 to
intracellular inhibition of the CK2 enzyme.
About Cylene Pharmaceuticals, Inc.
Cylene Pharmaceuticals is a biotech pharmaceutical company dedicated to the
discovery, development and commercialization of targeted small-molecule drugs
to treat life-threatening cancers. Cylene has created a diverse portfolio of
product candidates, including novel inhibitors of cancer-linked
serine/threonine protein kinases, as well as innovative nucleolus targeting
agents (NTAs) that target the abnormal nucleolar functions of cancer cells and
selectively kill cancer cells. More information can be found at
www.cylenepharma.com.
Cylene cautions you that statements included in this press release that are
not a description of historical facts, including implied statements relating
to future outcomes of clinical trials, may be forward-looking statements that
are subject to risks and uncertainties. Actual results may differ materially
from those set forth in this release due to the risks and uncertainties
inherent in Cylene's business including, without limitation, risks related to
difficulties or delays in, testing, obtaining regulatory approval for,
producing and marketing its products; unexpected adverse side effects or
inadequate therapeutic efficacy of its products that could delay or prevent
product development or commercialization, the scope and validity of patent
protection for its products; competition from other pharmaceutical or
biotechnology companies; and its ability to obtain additional financing to
support its operations. All forward-looking statements are qualified in their
entirety by this cautionary statement and Cylene undertakes no obligation to
revise or update this news release to reflect events or circumstances after
the date hereof.
SOURCE Cylene Pharmaceuticals
William Rice, Ph.D., President and CEO of Cylene Pharmaceuticals,
+1-858-875-5100, wrice@cylenepharma.com; or media, Karen Sparks of Mentus,
+1-858-455-5500, ext. 275, karen@mentus.com, for Cylene Pharmaceuticals
