KineMed, Inc. Presents Innovative Measurement Of Reverse Cholesterol Transport At The American Heart Association Scientific Sessions 2005 Conference

EMERYVILLE, Calif., Nov. 15 /PRNewswire/ -- KineMed, Inc., a platform- based drug development and advanced medical diagnostics company, announced that today, KineMed's poster presentation at the American Heart Association's Scientific Sessions 2005 Conference held in Dallas Texas will present for the first time, measurements of RCT, including the effects of diet and drugs. The technical basis of the RCT assay will be described. RCT is now being measured routinely in both humans and pre-clinical animal models. KineMed's poster entitled "The Stable Isotope Method for the Measurement of Reverse Cholesterol Transport" will be presented in the session entitled HDL Metabolism (session # APS.14.3M) from 3:30-5:00 pm in the Dallas Convention Center Hall E.

Background on reverse cholesterol transport

Higher plasma concentrations of high-density lipoprotein (HDLc) are associated with lower cardiovascular risk. The cardioprotective effects of HDLc are based on epidemiologic studies, animal models, and some prospective clinical therapeutic trials.

The most widely accepted mechanistic explanation for these cardioprotective actions of HDLc is its role in reverse cholesterol transport (RCT). This refers to the process by which cholesterol is mobilized from tissues, carried through the blood and excreted from the body in the form of fecal sterols. RCT is the only pathway by which cholesterol can be removed from the body and, therefore, represents a key therapeutic target, particularly for reversing existing arteriosclerotic lesions.

Importance of measuring RCT

Although the molecular biology of RCT has become increasingly well understood over the past decade, there had been no way to measure the rate or efficiency of RCT in living animals. Technically, this requires a measurement of the flow of cholesterol, or flux, through the RCT pathway, which had not previously been possible. This technical limitation is particularly important as new drugs are developed that raise HDLc levels, (such as cholesterol-ester transfer protein inhibitors). The key question that must be answered for each agent is whether the increased HDL is actually functional: i.e., is RCT increased or not? The FDA will also clearly demand evidence that changes in HDLc are of functional benefit.

KineMed's test of RCT flux

KineMed, Inc., has developed a test that measures flux through the two arms of RCT-tissue cholesterol efflux into the bloodstream and blood cholesterol flux into fecal sterols-in animal models and in humans.

KineMed's poster at the AHA will present for the first time, measurements of RCT, including the effects of diet and drugs. The technical basis of the RCT assay will be described. RCT is now being measured routinely in both humans and pre-clinical animal models.

The rates of cholesterol efflux from tissues into the bloodstream have been quantified for the first time and will be presented. This includes the effects of dietary cholesterol manipulations and drug interventions.

The flux from blood cholesterol into excreted sterols, and the sources of excreted sterols, will also be presented.

Implications of RCT measurement

The capacity to measure flux through the RCT pathway in humans as well as preclinical animal models opens many possibilities. For preclinical drug development, leads can be screened and optimized, new targets or unanticipated actions of drugs can be discovered, and combination therapies can be evaluated. Many uses in clinical drug development trials are also possible. Identifying the optimal dose, combination or regimen of agents in phase II trials; patient selection and stratification; and identifying the next generation of RCT stimulators are among the many possible uses.

Ultimately, individualization of therapy to maximize RCT in an individual patient may be possible, with an assay of RCT flux.

David Fineman, President and CEO of KineMed, commented, "KineMed's first ever measure of cholesterol eflux can aid the development of the next generation of cholesterol lowering agents and also applies to understanding the genetics, physiology, and pathogenesis of RCT."

About KineMed, Inc.

KineMed, Inc. provides a proprietary set of tools for measuring the dynamics of molecular and cellular response to drugs in the intact organism, both in animals and humans. KineMed's technology is ideally suited to enable the discovery of entirely new, unanticipated uses for compounds (an approach called repurposing or repositioning) by screening for activity in vivo across a wide variety of disease states. The breadth of therapeutic targets covered by KineMarker(TM) assays allows high-throughput screening in conditions beyond those typically evaluated. KineMed's technology expedites the drug development process and provides real-time insight into conditions including metabolic disorders, cancer, and diseases of inflammation and neurodegeneration.

For further information about KineMed, please visit: http://www.kinemed.com/ .

KineMed, Inc.

CONTACT: Lisa Misell, Ph.D., Vice President of Business Development ofKineMed, +1-510-655-6525, ext. 117, or Media: Justin Jackson, BurnsMcClellan, +1-212-213-0006, jjackson@burnsmc.com, for KineMed, Inc.

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