Abstract
Introduction: Human relaxin-2 (hRelaxin-2), a vasoactive hormone with hemodynamic, anti-fibrotic, and cardioprotective effects, has been pursued as a potential therapy for acute decompensated heart failure. It binds to RXFP1, its cognate receptor, and to a lesser extent to RXFP2. In clinical trials, intravenous (IV) administration of recombinant hRelaxin-2 (Serelaxin) improved markers of cardiac, renal, and hepatic damage and reduced congestion. However, these effects diminished rapidly upon treatment termination. We hypothesized that the transient treatment benefits could be due to the short half-life (T1/2=4.6 hours) of Serelaxin since continuous infusion of hRelaxin-2 using subcutaneous implanted minipump has resulted in long term benefits in animal studies (Hypertension. 2014;64:315-322). To test this hypothesis, we constructed a novel hRelaxin-2 fusion (hRLX2) and evaluated its activity in vitro and its pharmacokinetic (PK) profile in vivo.
Sign-in/Register to access full text options 
Free) 
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
