Mar 6, 2023 · Discovered and developed by Merck, MK-0616 is an investigational, potentially first oral PCSK9 inhibitor designed to lower low density lipoprotein (LDL) cholesterol. MK-0616 is a macrocyclic peptide that binds to PCSK9 and inhibits the interaction of PCSK9 with LDL receptors. About Hypercholesterolemia

MK-0616 is an oral macrocyclic peptide inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) in development for the treatment of hypercholesterolemia. This Phase 2b, randomized, double-blind, placebo-controlled, multicenter trial aimed to evaluate the efficacy and safety of MK-0616 in participants with hypercholesterolemia.

Aug 25, 2023 · MK-0616 is an investigational, potentially first oral PCSK9 inhibitor designed to lower LDL cholesterol via the same biological mechanism as currently approved injectable PCSK9 inhibitors but in a daily pill form.

May 1, 2023 · As such, MK-0616 could be a highly effective cholesterol-lowering therapy for patients who require LDL-C reduction. MK-0616 has the potential to overcome numerous barriers to treatment, allowing more patients to achieve LDL-C goals and reduce cardiovascular risk earlier in their treatment journey.

MK-0616 is a potent, oral macrocyclic peptide inhibitor of PCSK9 that is not only able to reduce LDL-cholesterol, non-HDL-cholesterol, and apoB, but can also lower Lp(a). Safety and tolerability studies reported to date are promising.

Nov 15, 2021 · MK-0616 reduced blood levels of free PCSK9 protein by more than 90% from baseline when administered to healthy men as a single dose of between 10 and 300 milligrams, regardless of the dose.

The CORALreef AddOn Study is evaluating an oral investigational PCSK9-inhibitor (PCSK9i), called MK-0616 (compared to ezetimibe and/or bempedoic acid alone or ezetimibe plus bempedoic acid), to see if it may help lower LDL-C (cholesterol) in adults with hypercholesterolemia who have atherosclerotic cardiovascular disease (ASCVD), or who are …

To evaluate the effect of the oral, macrocyclic peptide PCSK9 inhibitor, MK-0616, vs. placebo on % change from baseline in LDL-C at Week 8 in participants with hypercholesterolemia Primary Hypothesis At least 1 of the 4 doses of MK-0616 (6 mg, 12 mg, 18 mg, and 30 mg) is superior to placebo on % reduction from baseline in LDL-C at Week 8

Apr 3, 2024 · Merck’s macrocyclic PCSK9 protein-protein interaction (PPI) inhibitor, MK-0616, is a once-daily PCSK9-lowering and LDL-cholesterol-lowering small molecule that has recently demonstrated antibody-like efficacy as an oral agent in the clinic.

Mar 6, 2023 · At eight weeks, MK-0616 doses demonstrated significant reductions in LDL cholesterol compared with placebo, showing drops of over 60% in those receiving 30 mg; 59% in those receiving 18 mg; more than 55% in those receiving 12 mg; and 41% in those receiving 6 …