ChemoCentryx Identifies Novel Small Molecule C5aR Antagonist
Development Candidate Triggers Milestone Payment from GlaxoSmithKline
Mountain View, CA May 5, 2009 ChemoCentryx, Inc., today announced that it has identified an orally bioavailable small molecule antagonist of the C5a receptor, CCX168, as a candidate for clinical development. The acceptance of the molecule as a development candidate triggered a $5.0 million milestone payment from the alliance with GlaxoSmithKline (NYSE: GSK). CCX168 is designed to specifically target the C5a receptor, a potent inflammatory mediator and component of the complement system, which is associated with the onset of autoimmune diseases such as lupus and certain types of vasculitis, among other diseases.
"In the quest to develop medicinally relevant inhibitor compounds, C5a receptor has been a target of epic difficulty in the pharmaceutical industry. CCX168 is a highly potent and specific C5a receptor small molecule antagonist, and unlike other compounds that have been developed to date. It adds another promising approach to addressing inflammatory and autoimmune diseases to ChemoCentryx's pharmaceuticals portfolio," said Thomas J. Schall, Ph.D., President and Chief Executive Officer. "I am gratified that the ChemoCentryx team has again demonstrated the broad capability of our proprietary technologies and our efficiency in developing a molecule with such excellent properties."
The complement system comprises a set of proteins that regulate certain types of inflammatory responses by the immune system. Fragments of these proteins, such as chemoattractant complement fragment C5a, work to recruit immune system cells including neutrophils and lymphocytes to the site of inflammation. The C5a receptor is highly expressed on innate immune cells, making it an attractive target for small molecule therapeutics. Given architectural similarities between the C5a receptor and chemokine receptors, ChemoCentryx researchers successfully applied the company's proprietary drug discovery technologies to identify and design small molecule C5aR antagonists and selected CCX168 based on its potency, selectivity and favorable pharmacokinetics. In preclinical models, C5a and its receptor C5aR have been shown to play a key role in the development of autoimmune disease. C5a also has been thought to play a role in age-related macular degeneration (AMD). C5aR is one of four defined chemokine and chemoattractant receptor targets covered under a 2006 alliance between ChemoCentryx and GlaxoSmithKline's Center of Excellence for External Drug Discovery (CEEDD), under which GSK has option rights to license certain product candidates.
About ChemoCentryx
ChemoCentryx, Inc., is a clinical-stage biopharmaceutical company focused on discovering, developing and
commercializing orally-administered therapeutics that target the chemokine and chemoattractant systems in
order to treat autoimmune diseases, inflammatory disorders and cancer. The chemokine system is a network
of secreted chemokine molecules, or ligands, and cell surface receptors that regulates inflammation. Based
on its proprietary drug discovery and drug development platform, ChemoCentryx has internally generated
multiple clinical and preclinical-stage programs, each targeting distinct chemokine and chemoattractant
receptors with different small molecule compounds. ChemoCentryx's lead compound, Traficet-EN, a specific
CCR9 antagonist, is in a Phase II/III multi-national clinical trial, called PROTECT-1, in patients with
moderate-to-severe Crohn's disease. CCX025, also a CCR9 antagonist, is in a Phase I clinical trial.
Additional clinical programs include the development of CCX140, which targets the CCR2 receptor, currently
in a Phase I clinical trial and intended for subsequent development to treat diseases such as Type 2
diabetes, multiple sclerosis and vascular restenosis, and CCX354, a CCR1 antagonist in a Phase I clinical
trial, being developed for inflammatory diseases such as rheumatoid arthritis. ChemoCentryx also has
several programs in preclinical development. ChemoCentryx is privately held. For more information, please
refer to www.chemocentryx.com.
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assumptions or future events or performance are not historical facts and are forward-looking statements.
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estimates or projections contained in the forward-looking statements include but are not limited to (i) the
initiation, timing, progress and results of ChemoCentryx's preclinical studies and clinical trials, (ii)
ChemoCentryx's ability to advance product candidates into clinical trials, (iii) GSK's exercise of its license
options, (iv) the commercialization of ChemoCentryx's product candidates, (v) the implementation of
ChemoCentryx's business model, strategic plans for its business, product candidates and technology, (vi)
ChemoCentryx's ability to maintain and establish collaborations or obtain additional government grant
funding, (vii) ChemoCentryx's estimates of its expenses, future revenues, capital requirements and its needs
for additional financing, (viii) the timing or likelihood of regulatory filings and approvals, (ix) the availability of
corporate partners, (x) the scope of protection ChemoCentryx is able to establish and maintain for intellectual
property rights covering its product candidates and technology, (xi) the impact of competitive products and
technological changes, (xii) the availability of capital and the cost of capital, (xiii) ChemoCentryx's financial
performance, (xiv) developments relating to ChemoCentryx's competitors and other vagaries in the
biotechnology industry and (xv) other risks.
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the date hereof. All forward-looking statements are qualified in their entirety by this cautionary statement and
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circumstances after the date hereof. This caution is made under the safe harbor provisions of Section 21E of
the Private Securities Litigation Reform Act of 1995.
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