CCR2 Program

ChemoCentryx has completed Phase I clinical trials for CCX140, which targets the CCR2 chemokine receptor. There is significant evidence that CCR2 plays an important role in the inflammatory response associated with metabolic diseases such as type 2 diabetes. Studies have shown that CCR2 may also be implicated in multiple sclerosis (MS) and inflammatory diseases of the cardiovascular system such as vascular restenosis.

CCX140 is chemically distinct from all publicly known antagonists of CCR2. Preclinical data show that the compound selectively inhibits CCR2-mediated migration of monocytes and does not inhibit migration mediated by other chemokine receptors, even when the compound is given at high doses. This high degree of target specificity is an important safety feature that may allow CCX140 to be effective while avoiding unwanted side effects.

Based on the data from our preclinical studies to date, we believe that CCX140 has a favorable safety and pharmacokinetic profile. In animal studies, CCX140 is well absorbed when given orally and the compound is well tolerated at dose levels much higher than those required to cause inhibition of CCR2 function. Moreover, CCX140 does not significantly inhibit the activity of a class of liver enzymes which are necessary for metabolizing other common drugs that patients may be taking. This lack of interference suggests that CCX140 may be safely used alongside other medications.

CCX140 is being developed as an orally delivered therapy for the treatment of type 2 diabetes, and potentially for other indications such as coronary artery restenosis following stenting. Because CCX140 is believed to work by blocking the macrophage infiltration that occurs only during inflammation, it is anticipated that administration of CCX140 will provide selective treatment of patients with these diseases without compromising general immune surveillance functions.

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