Difelikefalin is a kappa opioid receptor agonist used in the treatment of pruritus associated with chronic kidney disease in patients undergoing hemodialysis. KORs were first associated with itching in 1984.
- Mechanism
- Curator reviewed · 3 references
Difelikefalin is a synthetic peptide and agonist of kappa opioid receptors (KORs), which have long been known to be involved with the itching sensation (in addition to playing some role in addiction). Endogenous KOR agonists - called dynorphins - have a neuroinhibitory effect on the itching sensation at the spinal cord level and mouse models have shown KOR agonist antipruritic activity when used to treat itching induced by different pruritogens.
Although the specifics of the mechanism have yet to be elucidated, the administration of KOR agonists, like difelikefalin, in patients with uremic pruritus has proven an effective means to suppress scratching and improve their quality of life.
- Primary indication
- Difelikefalin is indicated for the treatment of moderate-to-severe pruritus associated with chronic kidney disease (CKD-aP; uremic pruritus) in adults undergoing hemodialysis.Curator reviewed · 1 structured indication
- Formula / weight
- C36H53N7O6 · 679.863 g/mol (avg)
- First approval
- Canada, 2022 · United States, 2021 · European Union, 2022
- Code names
- CR-845 · FE202845 · MR-13A9
- Brand names
Resolves to
FWMNVWWHGCHHJJ-SKKKGAJSSA-NSMILESCC(C)C[C@@H](NC(=O)[C@@H](CC1=CC=CC=C1)NC(=O)[C@H](N)CC1=CC=CC=C1)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=OWhat you can answer from here — as of September 23, 2026
Which drugs share a target with Difelikefalin, and which of those have an active Phase 3 trial?
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