Overview

ChemoCentryx is a biopharmaceutical company focused exclusively on discovering, developing and commercializing orally-administered therapeutics to treat autoimmune diseases, inflammatory disorders and cancer.

Our approach has been to target the chemokine system, a network of molecules including chemokine ligands and their associated receptors, as well as related chemo-attractant receptors, all of which are known to drive inflammation. Chemokine ligands concentrate at the site of an inflammatory event, serving as signals that attract and guide inflammatory cells to the tissue, where, based on the chemokine ligand and receptor combination, a specific inflammatory response is initiated. In certain diseases, discrete chemokine receptors that play a specific role in the pathology of interest have been identified, and the therapeutic goal is to specifically inhibit that receptor to provide clinical benefit. Accordingly, each of our drug candidates is a small molecule designed to target a specific chemokine or chemo-attractant receptor, thereby blocking the inflammatory response driven by that particular chemokine while leaving the rest of the immune system unaffected.

The ChemoCentryx approach is designed to discover, develop and commercialize therapeutics that we believe provide distinct advantages over currently marketed therapies in our disease areas of focus. These advantages include:

• Improved safety profile.
  Our drug candidates are designed to be highly selective to minimize the risk of off-target effects. Unlike several current therapies, which broadly suppress the body's immune system, we believe that our drug candidates, by selectively blocking a given chemokine-chemokine receptor combination, and leaving other chemokine-chemokine receptor interactions unaffected, can potentially bring even aggressive forms of chronic inflammation and autoimmune diseases under control in a safe, effective manner.

• Convenient dosing and improved patient compliance.
  Our current drug candidates are designed to be administered orally, providing what we believe to be an important improvement in patient convenience and the potential for improved patient compliance as compared to existing intravenous and subcutaneous treatments with biologics.

• Lower production costs.
  Unlike biologic agents, which require complex and expensive cell based systems to produce a given biologic agent, our drug candidates are typically cheaper to manufacture given that small molecules can be synthesized using standard chemistry processes.

ChemoCentryx has five drug candidates in clinical development and expect to advance one additional drug candidate into clinical development in 2012. Two of these drug candidates are wholly owned and are being developed independently by us while four are subject to our collaboration agreement with Glaxo Group Limited, or GSK, an affiliate of GlaxoSmithKline. GSK has already exercised its options to Traficet-EN and CCX354 and each of their two respective defined back-up compounds, and will have similar option rights to CCX168 and CCX832 if we establish clinical proof-of-concept. All of our drug candidates, including those under our collaboration agreement with GSK, have been internally discovered.

Our most advanced drug candidate, Traficet-EN™ (CCX282 or GSK'786), is intended to be a first-in-class, anti-inflammatory small molecule therapeutic targeting the chemokine receptor known as CCR9. We completed a Phase II clinical trial of Traficet-EN for the treatment of patients with moderate-to-severe Crohn's disease, called PROTECT-1. This study was designed to evaluate Traficet-EN for the induction of clinical response or remission in patients with Crohn's disease as well as to evaluate the utility of Traficet-EN as maintenance therapy.

Our lead independent drug candidate, CCX140, which targets the chemokine receptor known as CCR2, successfully completed a Phase II clinical trial in type 2 diabetics and is currently in two Phase II clinical trials in patients with diabetic nephropathy, a form of kidney disease. The CCR2 receptor is believed to be of central importance to certain inflammatory diseases, such as diabetic nephropathy and Type 2 diabetes. CCX354, which targets the chemokine receptor CCR1, successfully completed a Phase II proof-of-concept clinical trial for the treatment of rheumatoid arthritis, or RA. This successful Phase II proof-of-concept clinical trial triggered GSK's option rights under our collaboration agreement. GSK exercised its option to further develop and commercialize CCX354 in November of 2011 and has an exclusive right to initiate a Phase IIb clinical trial for CCX354 in RA. CCR1 plays a significant role in rheumatoid arthritis. CCX168, a complement 5a receptor antagonist, is currently in a Phase II proof-of-concept clinical trial for the treatment of anti-neutrophil cytoplasmic antibody, or ANCA-associated vasculitis, or AAV, and is subject to GSK's option. We recently completed a Phase 1 clinical trial for CCX832, an orally administered small molecule that targets the chemoattractant receptor ChemR23. The receptor is known to regulate inflammatory cells in disease such as psoriasis. Subject to further discussion with GSK, CCX832 is expected to enter a Phase II proof-of-concept clinical trial for the treatment of skin inflammation, and is subject to GSK's option. CCX662, our independent drug candidate for the treatment of glioblastoma multiforme, or GBM, is expected to enter a Phase I clinical trial in the second half of 2012.

We are also advancing several additional independent drug candidates through preclinical development, the most advanced of which target chemokine receptors involved in atopic dermatitis, inflammatory bowel disease, or IBD, including ulcerative colitis, liver inflammation, psoriasis, and RA. Programs in preclinical development include:

• Anticancer compounds that target CXCR7, a chemokine receptor we believe to be associated with tumor growth; and

• Additional compounds under evaluation targeting chemokine receptors for indications in liver disease and skin inflammation.

ChemoCentryx has developed a suite of proprietary technologies, called the EnabaLink® drug discovery engine, to better understand the chemokine system and to accelerate the identification of small molecule lead compounds that target and inhibit the function of specific chemokine receptors. ChemoCentryx has leveraged the EnabaLink drug discovery engine in our drug candidate programs and continue to apply these powerful research tools in our early stage drug discovery efforts.

We believe that our broad pipeline of oral drug candidates, our ability to advance unique, highly specific compounds into and through clinical development across diverse indications and our proprietary drug discovery technologies provide us with distinct advantages that will enable us to exploit the extensive pharmacologic potential of the chemokine system.

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