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ChemoCentryx Reports Positive Results and Completion of Phase I Clinical Studies of Novel CCR2 Antagonist, CCX140, at the European Association for the Study of Diabetes (EASD)

MOUNTAIN VIEW, Calif., Sept. 21 /PRNewswire/ -- ChemoCentryx, Inc., today announced that it reported positive preclinical and Phase I study results at the European Association for the Study of Diabetes (EASD).  CCX140, a novel, orally bioavailable small molecule antagonist of the chemokine receptor CCR2, improved metabolic function while significantly reducing inflammatory macrophages found in adipose tissue in an animal model, and was well tolerated in Phase I clinical trials.  These data were presented today in a poster presentation entitled "CCR2 Antagonist CCX140-B in Phase 2 for Diabetes" in Stockholm, Sweden.  Data from an ongoing Phase II clinical trial in patients with type 2 diabetes mellitus is expected by the end of 2010 or early 2011.  

Results showed that daily treatment with CCX140 significantly improved fasting glucose and ameliorated insulin resistance (HOMA-IR) in obese, diabetic mice over a 28 day treatment period without a corresponding increase in MCP-1 (also called chemokine ligand 2 (CCL2)), the main ligand for CCR2.  Circulating adiponectin levels were significantly reduced in obese, diabetic mice and this was reversed when treated with CCX140.  The metabolic improvements also correlated with a significant reduction in adipose tissue inflammatory macrophage numbers. The preclinical studies were followed by Phase I clinical trials in 88 healthy human subjects.  These Phase I studies comprised single and multiple ascending dose placebo-controlled administration of CCX140 at doses ranging from 0.05 mg to 10 mg per day.  CCX140 was well tolerated in the Phase I trials with a favorable pharmacokinetic profile suitable for 5 to 10 mg once-daily oral treatment.  A Phase II clinical trial in 140 subjects with type 2 diabetes mellitus on stable doses of metformin was initiated earlier this year based on these encouraging preclinical and Phase I clinical results. The Phase II clinical trial is ongoing.  

"These very encouraging results to date support further evaluation of CCX140 in advanced clinical trials for the treatment of patients with type 2 diabetes," said Thomas J. Schall, President and Chief Executive Officer of ChemoCentryx.  "In addition to a high degree of target specificity and metabolic benefits, CCX140 is clearly differentiated from other marketed products with its added potential to treat the underlying mechanisms of type 2 diabetes and associated complications such as nephropathy and retinopathy.   The results of these trials continue to lead us to believe that CCX140 will be a meaningful and novel treatment option for patients who suffer from type 2 diabetes."

About Type 2 Diabetes and CCR2

Type 2 diabetes is a common metabolic disorder of high blood glucose associated with insulin resistance. It is differentiated from type 1 diabetes in which the primary defect is the inability of the pancreas to produce insulin. Patients with type 2 diabetes often require medication to maintain glucose homeostasis. The incidence of type 2 diabetes has reached epidemic proportions, associated in part with the rise in the incidence of weight gain and sedentary lifestyle. Despite available therapies, such as metformin, sulfonylureas, thiazolidinediones, incretin mimetics and other therapies, an unmet medical need for safe and convenient treatments persists.

For decades, the presence of systemic markers of inflammation has been known to increase with obesity. The adipose tissue has been shown to express multiple inflammatory cytokines, including TNF-a, IL-6, and MCP-1, the expression levels of which correlate with the degree of adiposity. Several of these mediators, including MCP-1 (also called chemokine ligand 2 (CCL2)), the main ligand for CCR2, have been shown to impair insulin-stimulated glucose uptake in adipose tissue, skeletal muscle and liver, providing a link between inflamed adipose tissue and insulin resistance.

CCX140 is chemically distinct from all other known antagonists of CCR2 and works by blocking the monocyte/macrophage infiltration that occurs during inflammation and thus is designed to provide selective treatment of the disease without compromising other immune functions.

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 biological network that regulates inflammation via a collection of secreted chemokine molecules, or ligands, and their specific cell surface receptors. 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, completed a Phase II/III multi-national clinical trial, called PROTECT-1, in patients with moderate-to-severe Crohn's disease, where it demonstrated the ability to induce a clinical response and to maintain clinical remission over the course of the trial.  Phase III clinical trials of Traficet-EN are expected to initiate in the fourth quarter 2010.  In addition, CCX025, also a CCR9 antagonist, has successfully completed a Phase I clinical program. Other clinical programs include CCX140, which targets the CCR2 receptor, in Phase II clinical development for the treatment of type 2 diabetes mellitus; CCX354, a CCR1 antagonist in a Phase II clinical trial for the treatment of rheumatoid arthritis; and CCX168, a C5aR antagonist, in Phase I clinical development. ChemoCentryx also has several programs in preclinical development. ChemoCentryx is privately held. For more information, please refer to

Certain statements in this press release may constitute "forward-looking statements". These statements are made on the basis of current expectations, forecasts and assumptions that involve risks and uncertainties, including, but not limited to, economic, competitive, governmental and technological factors outside of our control, that may cause our business, strategy or actual results to differ materially from those expressed or implied. We do not intend, and undertake no obligation, to update any forward-looking statements, whether as a result of new information, future events or otherwise.

SOURCE ChemoCentryx, Inc.
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