Pioneering a new era in cholesterol management
1 billion
people affected by high cholesterol worldwide
100 million
adults in the United States are affected by high cholesterol
18.6 million
lives lost annualy due to Atherosclerotic Cardiovascular Disease (ASCVD)
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Cardiovascular Disease is the number 1 cause of death worldwide, responsible for ~31% of all annual global deaths
Hypercholesterolemia (high cholesterol), particularly elevated levels of Low-Density Lipoprotein Cholesterol (LDL-C), is a significant contributor to cardiovascular disease (CVD), including coronary artery disease, heart attacks, strokes, and other atherosclerotic and vascular disorders.
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The liver’s dual role in cholesterol management
The liver plays a dual role in cholesterol management — It produces cholesterol to support the production of hormones, vitamin D, and bile acids essential for digestion and vital functions while simultaneously clearing excess cholesterol from the bloodstream. The balance between these functions is crucial for maintaining healthy cholesterol levels.
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PCSK9 & LDL receptors
Low-Density Lipoprotein Receptors (LDL-R), which are located on the surface of liver cells, are essential components of cholesterol regulation. These receptors, which are recycled, bind to Low-Density Lipoprotein (LDL), commonly known as ‘bad’ cholesterol, facilitating its uptake into liver cells for degradation and removal from circulation.
However, Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9), a protein synthesized by liver cells (hepatocytes), interferes with this process. PCSK9 binds to LDL-R, promoting their degradation in lysosomes and reducing the liver’s ability to recycle LDL-R and clear LDL cholesterol from the bloodstream.
Increased PCSK9 activity reduces the number of LDL-R available for recycling, leading to higher circulating LDL cholesterol levels. With fewer LDL-R, LDL clearance from the bloodstream decreases, raising blood cholesterol levels and increasing the risk of atherosclerosis (plaque buildup in arteries).
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How PCSK9 inhibitors (PCSK9i) are transforming cholesterol treatment
PCSK9 inhibitors (PCSK9i) prevent LDL-R degradation. By blocking PCSK9’s ability to mark LDL-R for degradation, PCSK9i allow LDL-R to recycle back to the cell surface, enhancing the liver’s ability to remove LDL from the bloodstream and lowering cholesterol levels.
PCSK9 inhibitors have shown superior efficacy in lowering LDL compared to traditional statins like Lipitor® and Crestor®, which have collectively generated over $10 billion in annual revenue for more than a decade.
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Commercially available PCSK9 inhibitors
PRALUENT® (REGENERON® & SANOFI®)
REPATHA® (AMGEN®)
LEQVIO® (NOVARTIS®)
Together, these injectable therapies generate over $2 billion annually and have become a preferred treatment option for cholesterol management in high-risk patients, thanks to their superior efficacy, fewer side effects and contraindications compared to statins.
Despite their advantages, high costs and patient compliance challenges—primarily due to the need for siRNA or monoclonal antibodies—have hindered widespread adoption.
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Revolutionizing cholesterol management with AQR-008
At Aqur, we are developing AQR-008, an innovative oral PCSK9 inhibitor designed to effectively lower LDL cholesterol and reduce the risk of life-threatening cardiovascular events, such as heart attacks and strokes.
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A novel approach to PCSK9 inhibitors
Unlike existing PCSK9 inhibitors that rely on monoclonal antibodies or siRNA injections, AQR-008 takes a completely new approach:
Targets the EGF-A domain of LDL receptors (LDL-R) instead of directly inhibiting PCSK9.
Prevents PCSK9 from binding to LDL-R, allowing LDL to be recycled and continue clearing clearing LDL cholesterol from the bloodstream.
Doe not suppress PCSK9 production or interfere with its essential functions, thereby preserving other functions of PCSK9 that are still in the early stages of research.
By leveraging this innovative mechanism of action, AQR-008 has the potential to redefine cholesterol management—offering a more effective, convenient, and accessible alternative to existing treatments.
At Aqur, we’re not just lowering cholesterol ...
... we’re saving lives, one breakthrough at a time!
AQR-008 marks the commencement of Aqur’s journey
We are committed to expanding our drug pipeline with high-impact therapies targeting cardiovascular disease and other critical health challenges. Our goal is to build a comprehensive portfolio that addresses unmet medical needs and enhances patient care.
Beyond cardiovascular health: exploring new frontiers
As research into PCSK9’s multifaceted roles in cancer and immune modulation progresses, Aqur plans to explore its peptides for potential applications in oncology and immunology. This initiative will leverage our current focus on metabolic diseases to investigate novel therapeutic opportunities.
Aqur: Leading the way in the future of cholesterol management
Guided by scientific research and focused on patient care, we are not merely following innovation—we are at the creating it.
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