Difelikefalin

Chemical formula: C₃₆H₅₃N₇O₆  Molecular mass: 679.863 g/mol  PubChem compound: 24794466

Active ingredient description

Difelikefalin is a selective kappa opioid receptor agonist with low central nervous system penetration. The pathophysiology of chronic kidney disease-associated pruritus is thought to be multifactorial, including systemic inflammation and an imbalance in the endogenous opioid system (e.g., overexpression of mu opioid receptors and concomitant downregulation of kappa opioid receptors). The activation of kappa opioid receptors on peripheral sensory neurons and immune cells by difelikefalin are considered mechanistically responsible for the antipruritic and anti-inflammatory effects.

Medicine classification

This medicinal substance has been classified in the anatomical therapeutic chemical (ATC) classification according to its main therapeutic use as follows:

ATC code Group title Classification
V03AX04 V Various → V03 All other therapeutic products → V03A All other therapeutic products → V03AX Other therapeutic products
Discover more medicines within V03AX04

Product monographs

Competent medicine agencies globally have authorized commercialization of this active ingredient according to these medication package inserts (MPIs):

Title Information Source Document Type  
KAPRUVIA Solution for injection European Medicines Agency (EU) MPI, EU: SmPC

Structural formula

Graphic representation of the active ingredient's molecular structure

External identifiers

CAS Substance: 1024828-77-0
DrugBank Drug: DB11938
PubChem Compound: 24794466
RxNorm Ingredient: 2569089
UNII Identifier: NA1U919MRO
DIFELIKEFALIN

Medicines

Difelikefalin is an active ingredient of these brands:

Austria (AT)

Croatia (HR)

Estonia (EE)

France (FR)

Ireland (IE)

Israel (IL)

Italy (IT)

Lithuania (LT)

Note the following: The list of brand names is continuously updated, and thus does not include the total of products circulating worldwide.

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