CER-001, investigational product candidate that mimics the action of high density lipoprotein (HDL) to treat patients with acute coronary syndromes, has been found safe and effective in early-phase human studies.
CER-001 is a complex of human ApoA-I and phospholipids. CER-001 is designed to mimic HDL, the “good” cholesterol, to promote the removal of excess cholesterol and other lipids from artery walls and enhance reverse lipid transport.
Cerenis Therapeutics has completed phase 1 study to provide evidence that the investigational therapy was safe and well-tolerated at all dose levels evaluated, including those intended for future clinical development.
The phase 1 randomized, double-blind, placebo-controlled, cross-over, single rising dose study of 32 healthy dyslipidemic human volunteers, was designed to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of single intravenous infusions of CER-001.
In this study, each subject received dosages up to 45 mg/kg and placebo in a two period crossover design. No drug related adverse events were reported for CER-001, and cholesterol mobilization was observed at dose levels of 2mg/kg and higher.
The results from this study were consistent with pre-clinical findings in demonstrating evidence of dose-related cholesterol mobilization, as well as evidence of substantial increases in HDL-cholesterol levels.
Because of these properties, we believe that administration of CER-001 may promote reverse cholesterol transport and stimulate cholesterol removal in patients.
“These positive results represent an important milestone for the CER-001 program and Cerenis’ approach to developing potent HDL mimetics,” stated Jean-Louis Dasseux, CEO of Cerenis.
The data are strongly supportive of continued clinical development of CER-001 as a treatment for patients with high-risk atherosclerosis, including acute coronary syndromes, he added.
Cerenis Therapeutics is a biopharmaceutical company dedicated to the discovery and development of novel HDL therapies for the treatment of cardiovascular and metabolic diseases.
HDL is the primary facilitator of the reverse lipid transport, or RLT, pathway by which excess cholesterol is removed from arteries and are transported to the liver for elimination from the body.
Cerenis is developing a portfolio of HDL therapies, including HDL mimetics for the rapid regression of atherosclerotic plaque in high-risk patients, and HDL elevators for patients with low HDL. Cerenis is well positioned to become the leader in the HDL therapeutic market with a broad portfolio of programs in development.
Research suggests that HDL slows and may even reverse atherosclerosis. During reverse lipid transport (RLT), a natural cardioprotective process, HDL particles scour the walls of the arteries, pick up excess lipids and carry them to the liver where they are passed from the body. By inhibiting the buildup of atherosclerotic plaque, HDL offers significant protection against a variety of atherosclerotic diseases such as coronary artery disease, stroke, and peripheral vascular disease.
Leading cardiologists and cardiovascular health experts agree that developing effective HDL therapies is a very promising target for preventing and treating atherosclerosis-related diseases. Data from several major clinical studies over the last 20 years clearly show the health benefits of HDL.
For example, researchers administering the Framingham Heart Study – one of the most prolific and long-running epidemiological medical studies ever performed – made a definite correlation between high levels of HDL cholesterol and a decreased likelihood of death from coronary heart disease (CHD).
Based on the results of this study, it was determined that for every 1 mg/dL increase in HDL, the risk of CHD decreased by 2 to 3%. Since this discovery, the National Heart Lung and Blood Institute (NHLBI) incorporated HDL-cholesterol levels as one of seven criteria in its 10-Year Heart Attack Risk Calculator.