New pill for cholesterol when statins don’t work

A new daily pill which dramatically lowered cholesterol in trials could soon be available to patients with particularly high levels of ‘bad’ LDL cholesterol.

MK-0616 has been shown to reduce levels of cholesterol by more than 60 per cent — depending on the dose.

The drug is a type of monoclonal antibody therapy — man-made proteins that bind to targets on the body. MK-0616 works by de-activating a protein in the liver called proprotein convertase subtilisin/kexin type 9 (PCSK9).

The liver usually processes two-thirds of LDL, removing it from the bloodstream. But the more of this protein a person produces, the more cholesterol remains in their blood — that’s because PCSK9 breaks down cholesterol receptors in liver cells that are responsible for removing cholesterol from the bloodstream.

MK-0616 has been shown to reduce levels of cholesterol by more than 60 per cent — depending on the dose. Pictured: Cholesterol in the blood vessels. [File image] 

More than two in five people in England have high cholesterol, which puts them at risk of cardiovascular disease, leading to heart attack or stroke.

Around 6.5 million adults in England are currently taking cholesterol-lowering drugs such as statins, according to NHS England. These drugs work by reducing the amount of cholesterol made by the liver and helping it to remove cholesterol that is already in the blood.

‘Statins are the first-line treatment for high cholesterol,’ explains Chris Gale, a professor of cardiovascular medicine and an honorary consultant cardiologist at Leeds Teaching Hospitals NHS Trust.

‘Statins do lower cholesterol, but not always to the necessary level, and some patients may not be able to tolerate the high doses needed to reach the recommended target,’ he says.

Results of a new trial, published earlier this month in the Journal of the American College of Cardiology, showed that the new pill reduced LDL cholesterol in adults by 41.2 per cent at the lowest dose (6 mg) and 60.9 per cent at the highest dose (30 mg) after eight weeks of therapy.

There were no reports of serious side-effects and low rates of minor side-effects — typically flu-like symptoms, nausea, back pain and joint pain.

There are injectable forms of PCSK9 inhibitor drugs (such as alirocumab and evolocumab), which are given every few weeks — these are approved for use by the NHS for patients whose cholesterol levels are still too high despite being on statins.

Another PCSK9 inhibitor, inclisiran, is delivered as an injection twice a year.

However, the new PCSK9 inhibitor drug can be taken as a daily pill, so is likely to overcome downsides of the injectables, including skin reactions at the injection site and the fact that they are expensive.

The developer of MK-0616, pharmaceutical company MSD, is starting further clinical trials in patients later this year, where the drug will be compared with the best available treatments — with the hope of having it approved and launched in 2026.

Commenting on the research, Professor Gale said: ‘The results of this new drug trial are very promising and, if the drug proves to be effective, will add to the options available to patients to help control their cholesterol.

‘MK-0616 seems to be very effective and has a low rate of side-effects.’

‘The injectables are available on the NHS for patients who have not reached their goals on statins alone, and they are effective but the take-up has been slower than expected,’ says Professor Gale. ‘A daily pill may be preferable.’

Although drugs reduce cardiovascular risk, the cornerstone of treatment of high cholesterol is a healthy lifestyle.

Priya Tew, a dietitian based in Southampton who works in the NHS, says: ‘Nutrition is always a great complement to medications, and often making dietary changes can help improve the results of the medication.

‘This is not just about nutrition, but also being more active, getting adequate sleep and having stress management solutions.

‘Aim to reach an optimum weight, avoid smoking, exercise regularly — and stick to a diet low in saturated fat and rich in fibre, fruit and vegetables and oily fish.’