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Difelikefalin

Difelikefalin structure

CAS No:
1024828-77-0
Formula:
C36H53N7O6
Chemical Name:
Difelikefalin
Synonyms:
Difelikefalin (CR845);Difelikefalin(CR-845, FE-202845);CKD-943;CKD-943; CR 845; FE 202845; KORSUVA; MR13A9;DIFELIKEFALIN;CR845;CR 845;FE 202845;KORSUVA;MR13A9
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Difelikefalin has been used in trials studying the treatment of Acute Pain and Postoperative Pain.

Difelikefalin, a novel drug discovered by Cara Therapeutics and developed by Vifor Pharma, was approved by the USFDA and the European Medicines Agency (EMA) in 2021 for the treatment of moderate to severe pruritus (pruritus). It is a highly selective κ-type opioid receptor agonist administered as an intravenous injection. difelikefalin restricts its action to the peripheral nervous system, which reduces central nervous system side effects such as sedation, anxiety and hallucinations. This peripheral restriction makes difelikefalin potentially advantageous in the treatment of pruritus, especially in patients who experience refractory pruritus due to renal failure or other conditions.

Difelikefalin Basic Attributes

Molecular Weight：

679.85

Exact Mass：

679.40573244

UNII：

NA1U919MRO

Color/Form：

White to off-white

Characteristics

Density：

1.214±0.06 g/cm3(Predicted)

Boiling Point：

1005.5±65.0 °C(Predicted)

PKA：

2.05±0.20(Predicted)

Drug Information

Drug Indication：

Treatment of chronic kidney disease associated pruritus

MeSH Entry Terms：

4-Piperidinecarboxylic acid, 4-amino-1-((2R)-6-amino-2-(((2R)-2-(((2R)-2-(((2R)-2-amino-1-oxo-3-phenylpropyl)amino)-1-oxo-3-phenylpropyl)amino)-4-methyl-1-oxopentyl)amino)-1-oxohexyl)-

Difelikefalin Use and Manufacturing

Uses

Difelikefalin is used in the formation of oral formulations of kappa opioid receptor agonists for the treatment of variety of kappa opioid receptor-assocd. diseases and conditions such as pain, pruritus and inflammation.

Use Classification：

Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

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