Opportunity
Atherosclerosis or "hardening of the arteries" is the leading cause of death in the United States. Statins, which lower levels of plasma cholesterol to prevent the formation of arterial plaques, represent a $23 billion per year market. Shrinking existing plaques by RCT is a similar potential market and one of the most sought-after therapeutic strategies for big pharma today. For example, drugs that increase RCT are now in clinical development at leading pharmaceutical companies, including Pfizer, Pfizer/Esperion, and Atherogenics/Astra Zeneca.

Reverse cholesterol transport
RCT is the process of moving cholesterol from tissues and plaques and ultimately out of the body. This two-part metabolic process involves export of cholesterol from tissue to the blood. Cholesterol in the blood is then excreted from the body.

Cholesterol is necessary for cellular functions and thus, cholesterol levels within the body are tightly controlled. Cholesterol is a major component of atherosclerotic plaques. Removing cholesterol can stop plaques from increasing in size and potentially decrease existing plaques.

The goal of using RCT to reverse atherosclerosis is to increase the rate of cholesterol export or "efflux" from the tissues and plaques. An increase in this cholesterol efflux rate should shrink arterial plaques by decreasing their static accumulation of cholesterol.

While some currently marketed drugs have a positive impact on RCT by increasing the rate of cholesterol excretion from the body, no drug has yet been approved to increase the rate of cholesterol efflux from the tissues.

Drug screening and development with KineMed technology
Tissue-cholesterol efflux is the leading mechanistic approach for drug therapies aimed at cardiovascular disease and atherosclerosis.

• KineMed is unique in its ability to measure RCT in animals and/or patients.
• KineMed can screen drug candidates for their ability to improve RCT in accepted animal models. Drugs with confirmed activity that would support reversal of atherosclerosis are licensed and can be rapidly advanced into clinical development.
• In clinical development, KineMed utilizes its unique technology to detect real-time effects on RCT to demonstrate the drug's therapeutic activity in First-in-Man studies.
• In 2006, KineMed initiated evaluation studies with multiple partners. In 2007, we will expand our partner development collaborations.