Inhibiting HDL to LDL Conversion with Obicetrapib to Manage Hypercholesterolemia
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Reviewed by Dat Tien Nguyen, B.A, ScM.
Translated by Nhi Phuong Quynh Le, B.A |
Posted on July 23rd, 2025
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High serum low-density lipoprotein (LDL) cholesterol level had been associated with a higher risk of cardiovascular events. Treatment such as statin might not yield the needed degree of clinical improvement and dose escalation might be limited by side effects. With funding from New Amsterdam Pharma, a study was conducted to evaluate the usage of obicetrapib to manage blood cholesterol level.
The clinical study included 2530 participants with an average age of 65 years old who had been diagnosed with either atherosclerosis, hypercholesteremia, or both. All of the participants were being treated with statin, with around 26% being treated with ezetimibe and 3% with PCSK9 inhibitors. Biochemical analysis found the cohort has a baseline LDL cholesterol level of around 98 mg/dL. The participants were randomly assigned to be treated with placebo or 10 mg of obicetrapib. The treatment was taken orally once a day. Obicetrapib is a cholesteryl ester transfer protein inhibitor; thus, obicetrapib can inhibit the transformation from high-density lipoprotein (HDL) cholesterol to LDL cholesterol.
After 365 days of treatment, the researcher found that obicetrapib was effective at reducing the LDL cholesterol level by 30% from baseline. Additionally, obicetrapib can also reduce the level of apolipoprotein B and increase the amount of HDL cholesterol. The researchers concluded that these promising results might suggest that using obicetrapib in conjunction with statin might be effective at managing hypercholesterolemia. The high efficacy of obicetrapib might be explained by its hydrophilic structure which facilitates its maintenance in circulation instead of accumulation in adipose tissue.
The clinical study included 2530 participants with an average age of 65 years old who had been diagnosed with either atherosclerosis, hypercholesteremia, or both. All of the participants were being treated with statin, with around 26% being treated with ezetimibe and 3% with PCSK9 inhibitors. Biochemical analysis found the cohort has a baseline LDL cholesterol level of around 98 mg/dL. The participants were randomly assigned to be treated with placebo or 10 mg of obicetrapib. The treatment was taken orally once a day. Obicetrapib is a cholesteryl ester transfer protein inhibitor; thus, obicetrapib can inhibit the transformation from high-density lipoprotein (HDL) cholesterol to LDL cholesterol.
After 365 days of treatment, the researcher found that obicetrapib was effective at reducing the LDL cholesterol level by 30% from baseline. Additionally, obicetrapib can also reduce the level of apolipoprotein B and increase the amount of HDL cholesterol. The researchers concluded that these promising results might suggest that using obicetrapib in conjunction with statin might be effective at managing hypercholesterolemia. The high efficacy of obicetrapib might be explained by its hydrophilic structure which facilitates its maintenance in circulation instead of accumulation in adipose tissue.