Pharmacokinetics, safety and tolerability of serelaxin in patients with hepatic impairment

Serelaxin is a recombinant human relaxin-2 that is approved in Russia for the treatment of acute heart failure.

Aim

To evaluate the pharmacokinetics (PK) of serelaxin in patients with hepatic impairment.

Material and methods

In this open-label, parallel group study non-compartmental PK parameters of serelaxin and standard safety assessments following a single 24 h intravenous infusion 30 μg/kg/day were compared between patients with mild, moderate or severe hepatic impairment (cirrhosis Child-Pugh class A, B or C) and healthy matched controls.

Results

In all groups the serum concentration of serelaxin increased within the first few hours of infusion, reached steady-state at 12-24 h and then declined following completion of infusion, with a mean terminal half-life of 7-8 h. All PK parameters were comparable between each group of patients with hepatic impairment and healthy controls. No serious adverse events or discontinuations due to adverse events were reported.

Conclusion

The PK and safety profile of serelaxin were not affected by hepatic impairment. No dose adjustment is needed for serelaxin treatment of 48 h infusion in patients with hepatic impairment.

Key words

Serelaxin, pharmacokinetics, safety, hepatic impairment.