Merck’s MK-0616, an Investigational Oral PCSK9 Inhibitor, …
WEBMar 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.
Merck Initiates Phase 3 Clinical Program for Oral PCSK9 Inhibitor ...
WEBAug 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.
Oral PCSK9 Inhibitor Substantially Reduces Cholesterol in Phase 2 …
WEBMar 6, 2023 · PCSK9 inhibitors are usually taken alongside statins—the standard first-line therapy for treating high cholesterol—and can be used alone in people who cannot take statins. Results from the phase 2 trial showed MK-0616 reduced LDL cholesterol by around 60% among people taking 30 mg or 18 mg daily, compared to those taking a placebo.
A Series of Novel, Highly Potent, and Orally Bioavailable Next ...
WEBNov 25, 2021 · Proprotein convertase subtilisin-like/kexin type 9 (PCSK9) is a key regulator of plasma LDL-cholesterol (LDL-C) and a clinically validated target for the treatment of hypercholesterolemia and coronary artery disease.
Oral PCSK9 inhibitor found to be safe, effective to lower …
WEBDALLAS, Nov. 15, 2021 — Results from two early clinical studies show the first version of an oral PCSK9-inhibitor cholesterol-lowering medicine was well tolerated and highly effective at reducing high levels of LDL cholesterol, according to late-breaking research presented today at the American Heart Association’s Scientific Sessions 2021 ...
Series of Novel and Highly Potent Cyclic Peptide PCSK9 ... - PubMed
WEBNov 25, 2020 · Proprotein convertase subtilisin-like/kexin type 9 (PCSK9) is a key regulator of plasma LDL-cholesterol (LDL-C) and a clinically validated target for the treatment of hypercholesterolemia and coronary artery disease.
Merck readies oral, macrocyclic PCSK9 inhibitor for phase II test
WEBNov 18, 2021 · PCSK9 is a secreted protease that degrades the LDL receptor, and a poster child for genetically validated targets. Gain-of-function mutations lead to increased cholesterol levels, and...
Phase 2b Randomized Trial of the Oral PCSK9 Inhibitor MK-0616:
WEBAn oral PCSK9 inhibitor that can achieve robust reductions in LDL-C and is well tolerated may offer potential advantages over injectable PCSK9 inhibitors in terms of simplicity of dosing, patient preference, and access.
mRNA Display Reaches for the Clinic with New PCSK9 Inhibitor
WEBAug 26, 2022 · Merck & Co. recently reported one of the first mRNA display-derived clinical candidates in a bioavailable inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9).
Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 …
WEBMay 1, 2023 · This work validates the use of mRNA display technology for identification of novel oral therapeutic agents, exemplified by the identification of an oral PCSK9 inhibitor, which has the potential to be a highly effective cholesterol lowering therapy for patients in need. Clinical Perspective. What Is New? •.