Merck Launches Two Phase 3 Clinical Trials in China for Oral PCSK9 Inhibitor MK-0616

Dec 19, 2023 16:58 CST Updated 16:58

MSD

Pharmaceutical R&D and Manufacturer

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The official website of the Chinese Drug Clinical Trial Registration and Information Disclosure Platform announced,MSD has launched two international multi-center (including China) Phase 3 clinical trials for MK-0616 in China, targeting indications includingAtherosclerosis, Hypercholesterolemia. According to literature reports[2]，MK-0616 is the first oral small-molecule PCSK9 inhibitor to enter Phase 3 clinical trials.In an earlier Phase 2b clinical study, the drug reduced LDL-C levels by 41.2% to 60.9% in patients with hypercholesterolemia.

Screenshot source:China Drug Clinical Trial Registration and Information Disclosure Platform Official Website

Hypercholesterolemia is a condition in which the blood containsLow-Density Lipoprotein Cholesterol (LDL-C)Diseases with elevated levels.Dyslipidemia, especiallyLDL-CWaterIncrease in flat isAtherosclerotic Cardiovascular Disease (ASCVD)）The pathogenic risk factors can significantly reduce the incidence and mortality of ASCVD by lowering LDL-C levels.According to the "China Lipid Management Guidelines (2023)," in recent years, the lipid levels and the prevalence of dyslipidemia in the Chinese population have been on the rise, with abnormal blood lipids being common among adults.The overall prevalence is as high as 35.6%.Despite dietary modifications and statin therapy, many patients with hypercholesterolemia fail to achieve or maintain the guideline-recommended LDL-C reduction goals.

PCSK9Has become an emerging target in the cardiovascular field.PCSK9 Inhibitors as a New Type of Lipid-Lowering Drug with Potent LDL-C Lowering Effects Have Been Recommended by Lipid Management Guidelines Both in China and Abroad, and Are Widely Recognized by Clinicians. However, There Are Currently No Oral PCSK9 Inhibitors Available for Doctors and Patients.

MK-0616 is a product being developed by MSD.Oral PCSK9 Small Molecule Inhibitor. As a macrocyclic molecule, it can inhibit the interaction between PCSK9 and LDLR, allowing more low-density lipoprotein receptors (LDLR) to return to the cell surface, taking up more LDL-C from the blood and reducing its levels. Different fromCurrently approved injectable PCSK9 inhibitors,MK-0616InAdministered in the form of daily tablets。

MSD has launched two Phase 3 clinical trials in China, both conducted by Beijing Anzhen Hospital, Capital Medical University.Professor Ma ChangshengServed as the principal investigator. The two studies were: oneEvaluation of the Efficacy and Safety of MK-0616 in Adults with HypercholesterolemiaA Phase 3, randomized, double-blind, placebo-controlled study, which plans to enroll 170 participants in China and 2760 participants internationally.Evaluation of the Efficacy and Safety of MK-0616 in Reducing Major Adverse Cardiovascular Events in Subjects at High Cardiovascular RiskA Phase 3, randomized, placebo-controlled clinical study. This study plans to enroll 470 participants in China and 14,550 participants internationally.

EarlierThe results of the published Phase 2b clinical trial showed that patients with hypercholesterolemia were randomly treated with four different doses (6mg~30mg) of MK-0616 or a placebo. The trial results indicated,At Week 8, all doses of MK-0616 significantly reduced LDL-C compared to placebo, with reductions ranging from 41.2% (6 mg) to 60.9% (30 mg).The therapeutic effect reached a near-peak level after two weeks of medication and was maintained throughout the 8-week treatment period.

References:

[1] Official Website of the Chinese Drug Clinical Trial Registration and Information Disclosure Platform. Retrieved Dec 13, 2023, from http://www.chinadrugtrials.org.cn/clinicaltrials.searchlist.dhtml

[2] Norata GD, Tokgözoğlu L. Oral strategies to target proprotein convertase subtilisin/kexin type 9 and lipoprotein(a): the new frontier of lipid lowering. Eur Heart J. 2023 Nov 8:ehad682. doi: 10.1093/eurheartj/ehad682. Epub ahead of print. PMID: 37947270.

[3] Merck Initiates Phase 3 Clinical Program for Oral PCSK9 Inhibitor Candidate MK-0616. Retrieved August 25, 2023, from https://www.merck.com/news/merck-initiates-phase-3-clinical-program-for-oral-pcsk9-inhibitor-candidate-mk-0616/

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