Daily Oral PCSK9 Inhibitor Encouraging in Phase 1 Trials

The investigational PCSK9 inhibitor of Merck, MK-0616 — comes in pill form, in contrast to the three currently available PCSK9-lowering drugs that must be given in injections separated by weeks to months. In two phase-1 studies with a total of 100 participants, MK-0616 was given daily for 2 weeks on a background of statin therapy for 14 days The drug exhibited a dose-dependent increase in plasma exposure and > 90% mean maximum reduction of free plasma PCSK9 levels from baseline at all dose levels studied At 14 days of treatment, participants receiving MK-0616 exhibited 65% reduction in the low-density-lipoprotein cholesterol (LDL-C) MK-0616 was well tolerated at doses up to 300 mg with no deaths, serious adverse events, or clinically meaningful trends in laboratory safety tests, vital signs, or ECGs as a function of the study intervention. MK-0616 represents the first oral PCSK9i with clinical data supporting its potential to be a powerful oral cholesterol-lowering agent for the treatment of hypercholesterolemia and coronary heart disease. An oral PCSK9i would provide greater convenience and patient access and these data support further development of MK-0616 in a range of hypercholesterolemic patients. Disclaimer: Lupin makes no representation or warranty of any kind, expressed or implied, regarding the accuracy, adequacy, validity, reliability, availability, or completeness of any scientific information shared by the HCP on the ­­­STAR UPDATE podcast. You should not allow the contents of this to substitute for your own medical judgment, which you should exercise in evaluating the information on this website.