Merck's Oral Cholesterol-Lowering Peptide Gets FDA Approval

The US Food and Drug Administration (FDA) has approved Merck & Co's Lipfendra (enlicitide), an oral cholesterol-lowering peptide, after a decade in development. Enlicitide is the first oral inhibitor of PCSK9 and offers an alternative to injected antibodies for patients who haven't seen sufficient LDL-C reduction with standard statin treatment.

David Thaisrivongs, Merck's executive director head of biocatalysis, said 'it's been long time coming' after the success of injectable PCSK9 inhibitors like Regeneron's Praluent (alirocumab) and Amgen's Repatha (evolocumab), which have been on the market since 2015.

Enlicitide is a macrocyclic peptide with chemical crosslinks that improve its stability and efficacy, allowing it to disrupt complex protein, protein interactions. Despite the challenge of manufacturing such a large molecule, Merck's team was able to develop a biocatalytic synthesis using 13 different engineered enzymes.

Preventative cardiologist Michael Shapiro praised enlicitide for being 'just as effective' as injectable PCSK9 antibodies and noted that oral drugs might be more accessible to patients due to general practitioner prescribing. However, he cautioned that cost will remain an issue until the medication goes generic.