Selexipag

How it works

Selexipag and its active metabolite selectively stimulate the prostacyclin IP receptor, producing pulmonary vasodilatation and inhibition of vascular smooth-muscle proliferation, thereby reducing pulmonary vascular resistance.

Prescribing in practice

• Initiate and titrate under specialist supervision, increasing gradually to the highest tolerated level, as abrupt changes and the prostacyclin pharmacology drive dose-limiting effects.
• Common pharmacological effects include headache, jaw pain, flushing, diarrhoea, nausea and limb pain, which are most prominent during up-titration.
• Strong inhibitors of CYP2C8 markedly increase exposure and should be avoided, and the dose may need adjustment in hepatic impairment.

Monitoring

Monitor symptom control, functional status, tolerability during dose titration and concomitant interacting medicines, with specialist review of treatment response.

Counselling the patient

• Side effects such as headache, jaw pain and flushing are common, especially as the dose is increased, and often ease with time.
• Do not stop the medicine suddenly without specialist advice.
• Tell your team about any new medicines, as some can interact.

Evidence & guidelines

The GRIPHON trial showed selexipag reduced a composite of morbidity and mortality events in pulmonary arterial hypertension, supporting its place in combination therapy.