AstraZeneca acquires oral PCSK9 inhibitor programme from Dogma Therapeutics

AstraZeneca is acquiring the preclinical oral PCSK9 inhibitor programme from Dogma Therapeutics.

The company aims to take the programme forward into clinical development for dyslipidaemia – or abnormal amount of lipids in the blood – and familial hypercholesterolemia, a common genetic condition that causes high cholesterol.

PCSK9 is a protein that regulates the level of low-density lipoprotein (LDL), or ‘bad’  cholesterol in the blood. Increased activity of PCSK9 is associated with high LDL cholesterol.

The acquired PCSK9 inhibitors are small molecules that bind directly to a novel part of PCSK9 and have shown to block its activity and lower LDL cholesterol in preclinical models.

There are currently no oral PCSK9 inhibitors available to patients or in clinical development.

Mene Pangalos, Executive Vice President of BioPharmaceuticals R&D at AstraZeneca, said: “Raised LDL cholesterol is a key risk factor for cardiovascular disease and is estimated to cause 2.6 million deaths worldwide every year.

“Whilst PCSK9 is a well validated target for lowering LDL cholesterol it has been a hugely challenging target to inhibit with small molecules.

“This agreement with Dogma Therapeutics offers us the opportunity to develop the first small molecule, orally bioavailable PCSK9 inhibitor, for patients at risk of cardiovascular disease.”

AstraZeneca anticipates entering clinical development in 2021.

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