Abstract
Objectives Riociguat, an oral soluble guanylate cyclase (sGC) stimulator, is a new candidate for treatment of pulmonary hypertension (PH). Riociguat increases cGMP production through a novel dual mode of action: direct NOindependent stimulation of sGC and increasing sensitivity of sGC to low levels of NO. Another sGC stimulator, BAY 41-2272, has shown anti-platelet activity in animal models, as have BAY 41-2272 and riociguat in washed human platelets, although bleeding has not been noted as an adverse event (AE) in riociguat clinical studies [1,2]. As riociguat and aspirin are likely to be used together in PH, it was of interest to investigate potential PD and PK interactions.
Highlights
All adverse event (AE) were mild except 1 case of moderate headache following riociguat administration
Riociguat PK values were independent of aspirin coadministration
One hour after coadministration of riociguat and aspirin, the mean increase in fraction unbound was 19% for riociguat and 24% for its metabolite M-1 (BAY 60-4552) indicating mild displacement by salicylic acid, the main aspirin metabolite
Summary
Methods In this randomized, open-label, crossover study, participants took 2.5 mg/day riociguat, two morning doses of 500 mg aspirin, or both drugs concomitantly. Six of 17 participants in the safety evaluation reported ≥1 treatmentemergent AE.
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
