CETP inhibitors are clinically approved in China

Obicetrapib is an adjunct to dietary and maximum tolerated dose lipid-lowering therapy, according to an announcement on the official website of the Drug Evaluation Center (CDE) of the State Food and Drug Administration of China on March 23. For the treatment of adult patients with familial heterozygous hypercholesterolemia (HeFH) or diagnosed atherosclerotic cardiovascular disease (ASCVD) requiring additional reduction in low density lipoprotein cholesterol (LDL-C).

Obicetrapib is an oral selective cholesterol ester transfer protein (CETP) inhibitor being developed by NewAmsterdam, according to public information. In January, The company announced the completion of the first patient administration of obicetrapib in a Phase 3 study in the same group of patients with the same indication approved in China.

High levels of LDL-C, also known as "bad" cholesterol, in the blood. Despite the important improvements statins have made to lipid-lowering treatments, more than 100 million people around the world are failing to meet LDL-C targets, putting them at significantly increased risk of heart attack, stroke and other adverse cardiovascular outcomes and therefore highly unmet medical needs.

Studies have shown that CETP is a potential therapeutic target for reducing major adverse cardiovascular events such as heart attack and stroke by lowering both LDL-C and Apolipoprotein B (ApoB). At the same time, blocking CETP can also increase patients' high density lipoprotein cholesterol (HDL-C), which has an impact on blood lipid.

As a CETP inhibitor, Obicetrapib is being developed to reduce LDL-C and prevent major adverse cardiovascular events. In a randomized, double-blind, placebo-controlled Phase 2A TULIP trial, obicetrapib was well tolerated as a single agent or in combination with statins, effectively reducing LDL-C in 364 patients with mild dyslipidemia. The results have been published in the Prestigious medical journal The Lancet.
In November 2021, NewAmsterdam announced the full results of the phase 2 randomized study of obicetrapib (the ROSE study). This is a placebo-controlled, double-blind, randomized, phase 2 dose-exploration study designed to evaluate the efficacy, safety, and tolerability of obicetrapib as adjunctive therapy with high-intensity statins (HIS). A total of 120 patients were randomized to receive either placebo, 5 mg or 10 mg of Obicetrapib for 8 weeks. Both doses met their primary endpoint. Patients treated with statins and 5mg obicetrapib had a 42% reduction in ldl-c from baseline, those in the 10mg cohort had a 51% reduction from baseline, and those in the placebo cohort had a 7% reduction. In addition, apolipoprotein a-i (APOA1) HDL levels increased by 45% and 48% in patients receiving 5mg or 10mg obicetrapib, respectively.

For this reason, NewAmsterdam has initiated a Phase 3 trial of obicetrapib (BROADWAY trial) and announced the first patient enrollment in January 2022. This study will evaluate the effect of obicetrapib on LDL-C levels on day 84 in adults with familial heterozygous hypercholesterolemia or diagnosed atherosclatheroascular cardiovascular disease as an adjunct to diet and maximum tolerated lipid-lowering therapy.

The approval of obicetrapib in China means that it will soon start clinical trials in China. We look forward to the smooth follow-up clinical study of this product, so as to bring better treatment options for patients as soon as possible.