CCR2 Program

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

CCX140 is chemically distinct from all publicly known antagonists of CCR2. Preclinical data suggest 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.

A Phase I single-dose escalation clinical trial of CCX140 has been initiated in Switzerland to determine the drug's pharmacokinetic profile and an optimal dosing regimen. Based on the safety and tolerability of CCX140 in this single-dose study, a study may be initiated in healthy volunteers to determine the safety and tolerability of multiple doses of CCX140. Following completion of our Phase I clinical trials, we plan to initiate safety and proof-of-concept trials of CCX140 for the treatment of one or more additional inflammatory or metabolic diseases.

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