Finding a new way to treat pulmonary arterial hypertension

Hit to lead small molecule biased apelin receptor agonists for the treatment of pulmonary arterial hypertension

Pulmonary arterial hypertension (PAH) is a rare but devastating condition where the blood vessels in the lung narrow, causing strain on the right side of the heart. This can lead to heart failure and ultimately death – around 15 per cent of people diagnosed with PAH die within one year. Current medicines for PAH treat the symptoms but do not slow the disease’s progression and can have unpleasant side-effects. Dr Anthony Davenport aims to bring us closer to an effective treatment for PAH. A chemical messenger called apelin is reduced in people with PAH. Dr Davenport’s team have discovered molecules that mimic the effects of apelin, and they’ve shown that they slow PAH progression in animals with the condition. Now the researchers need to begin to refine this treatment strategy by designing and discovering molecules that better mimic apelin. The challenge is that the molecules need to not only be effective replacements for apelin, but also have properties that make them practical as a medicine. The researchers’ aim is to create a medicine that can be taken once a day and that works alongside existing PAH treatments. They hope to bring new treatments to people with this devastating disease.