Enlicitide tablet sharply reduces cholesterol in high-risk patients

WASHINGTON (AP) – A new type of tablet has substantially lowered artery-blocking cholesterol in people who remain at considerable risk of heart attacks despite using statins, researchers reported on Wednesday.

The treatment remains experimental, but it removes cholesterol from the body through a mechanism currently available only with injectable medicines. If authorised by the US Food and Drug Administration, the tablet, called enlicitide, could provide a simpler option for millions of people.

Enlicitide and LDL cholesterol reduction

Statins, the mainstay of treatment, reduce some of the liver’s cholesterol production. However, even at the highest doses, many patients require further treatment to lower LDL, or “bad”, cholesterol sufficiently to meet medical guidelines.

For a major trial, more than 2,900 high-risk patients were randomly allocated to take either a daily enlicitide tablet or a dummy drug alongside their usual treatment. Over six months, those using enlicitide experienced LDL cholesterol reductions of as much as 60 percent, the researchers reported in the New England Journal of Medicine.

Patients can add other tablets to their statin treatment, “but none come close to the degree of LDL cholesterol lowering that we see with enlicitide,” said the study’s lead author, Dr Ann Marie Navar, a cardiologist at UT Southwestern Medical Center.

After a year, the benefit had declined only slightly, and researchers found no safety difference between people taking the tablet and those receiving a placebo. There is one caveat: it must be taken on an empty stomach.

Statins, PCSK9 inhibitors and heart disease risk

Heart disease is the leading cause of death in the United States, while high LDL cholesterol – which leads to plaque accumulating in arteries – is a major risk factor for heart attacks and strokes.

Although an LDL level of 100 is regarded as acceptable for healthy people, doctors advise reducing it to at least 70 after someone develops high cholesterol or heart disease. Those at very high risk should lower it even further.

Statin tablets such as Lipitor and Crestor, along with their inexpensive generic versions, are very effective at reducing LDL. For people needing extra help, some potent injectable treatments operate differently by blocking PCSK9, a liver protein that restricts the body’s capacity to clear cholesterol from the blood.

Still, only a small proportion of people who could benefit from PCSK9 inhibitors take them. Although the prices of these expensive injections have fallen recently, patients may still dislike giving themselves injections, and Navar said they are more complicated for doctors to prescribe.

Merck funded Wednesday’s trial, which supplies some of the final information required to seek FDA approval for enlicitide. The FDA has placed the drug in a programme that promises ultra-fast reviews.

The findings provide “compelling evidence” that the new tablet lowers cholesterol by roughly as much as PCSK9 injections, wrote Dr William Boden of Boston University and the VA New England Healthcare System, who did not take part in the study, in the journal.

Boden warned that there is not yet evidence that the tablet’s cholesterol-lowering effect results in fewer heart attacks, strokes and deaths. Demonstrating that would take considerably longer than a year. Merck has a study involving more than 14,000 patients under way to determine this.