PrKORSUVA® is a first-in-class, kappa opioid receptor (KOR) agonist and the only treatment indicated in CKD-aP in Canada1,5*
KORSUVA’s mechanism of action*
The pathophysiology of CKD-aP is thought to be multifactorial, including:
an imbalance in the endogenous opioid system (e.g., overexpression of mu opioid receptors [MORs] and concomitant downregulation of KORs)
systemic inflammation
KORSUVA’s mechanism of action*
KORSUVA targets KORs, with low CNS penetration and with no binding or functional activity at mu-opioid receptors.
KORSUVA has a hydrophilic structure, which minimizes its passive diffusion (permeability) and active transport across the blood-brain barrier, thus limiting penetration into the CNS.
The activation of KORs on peripheral sensory neurons and immune cells by KORSUVA are considered mechanistically responsible for the antipruritic and anti-inflammatory effects.
Opioid receptors are known to modulate itch signals and inflammation, with KOR activation reducing itch and producing immunomodulatory effects.
Pharmacodynamics
In clinical studies, there were no signals of abuse, misuse, diversion, dependence or withdrawal with KORSUVA.1
* Comparative clinical significance has not been established.
