Difelikefalin

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Difelikefalin
Clinical data
Trade namesKorsuva
Other namesCR845, FE-202845, D-Phe-D-Phe-D-Leu-D-Lys-[γ-(4-N-piperidinyl)amino carboxylic acid][1]
License data
Pregnancy
category
Kappa opioid receptor agonist
ATC code
Legal status
Legal status
IV)[10]
MetabolismNot metabolized[10]
Elimination half-life2 hours[10]
ExcretionExcreted as unchanged
drug via bile and urine[10]
Identifiers
  • 4-amino-1-[(2R)-6-amino-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid
JSmol)
  • CC(C)C[C@H](C(=O)N[C@H](CCCCN)C(=O)N1CCC(CC1)(C(=O)O)N)NC(=O)[C@@H](CC2=CC=CC=C2)NC(=O)[C@@H](CC3=CC=CC=C3)N

  • as salt: CC(O)=O.CC(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)=O
  • InChI=1S/C36H53N7O6/c1-24(2)21-29(32(45)40-28(15-9-10-18-37)34(47)43-19-16-36(39,17-20-43)35(48)49)42-33(46)30(23-26-13-7-4-8-14-26)41-31(44)27(38)22-25-11-5-3-6-12-25/h3-8,11-14,24,27-30H,9-10,15-23,37-39H2,1-2H3,(H,40,45)(H,41,44)(H,42,46)(H,48,49)/t27-,28-,29-,30-/m1/s1
  • Key:FWMNVWWHGCHHJJ-SKKKGAJSSA-N

  • as salt: InChI=1S/C36H53N7O6.C2H4O2/c1-24(2)21-29(32(45)40-28(15-9-10-18-37)34(47)43-19-16-36(39,17-20-43)35(48)49)42-33(46)30(23-26-13-7-4-8-14-26)41-31(44)27(38)22-25-11-5-3-6-12-25;1-2(3)4/h3-8,11-14,24,27-30H,9-10,15-23,37-39H2,1-2H3,(H,40,45)(H,41,44)(H,42,46)(H,48,49);1H3,(H,3,4)/t27-,28-,29-,30-;/m1./s1
  • Key:MZWHRPKAHCWTOI-KGURMGBCSA-N

Difelikefalin, sold under the brand name Korsuva, is an

itch. It acts as a peripherally-restricted, highly selective agonist of the κ-opioid receptor (KOR).[10][11][12][13]

Difelikefalin acts as an analgesic by activating KORs on peripheral

proinflammatory, nerve-sensitizing mediators (e.g., prostaglandins).[10]

Difelikefalin was approved for medical use in the United States in August 2021.[8][14][15] The U.S. Food and Drug Administration considers it to be a first-in-class medication.[16]

Society and culture

Legal status

On 24 February 2022, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Kapruvia, intended for treatment of moderate-to-severe pruritus associated with chronic kidney disease.[17] The applicant for this medicinal product is Vifor Fresenius Medical Care Renal Pharma France.[17] Difelikefalin was approved for medical use in the European Union in April 2022.[9][18]

Research

It is under development by

pruritus (itching).[10][11][12] Difelikefalin has completed phase II clinical trials for postoperative pain and has demonstrated significant and "robust" clinical efficacy, along with being safe and well tolerated.[11][13] It has also completed a phase III clinical trial for uremic pruritus in hemodialysis patients.[19]

References

  1. PMID 20030621
    .
  2. ^ a b "Korsuva". Therapeutic Goods Administration (TGA). 25 November 2022. Archived from the original on 5 February 2023. Retrieved 7 April 2023.
  3. ^ "Updates to the Prescribing Medicines in Pregnancy database". Therapeutic Goods Administration (TGA). 21 December 2022. Archived from the original on 3 April 2022. Retrieved 2 January 2023.
  4. ^ https://www.tga.gov.au/resources/auspar/auspar-korsuva
  5. ^ "Product monograph" (PDF). Health Canada. Archived (PDF) from the original on 1 October 2022. Retrieved 7 April 2023.
  6. ^ "Summary Basis of Decision - Korsuva". Health Canada. 23 October 2014. Archived from the original on 24 January 2023. Retrieved 24 January 2023.
  7. ^ "Details for: Korsuva". Health Canada. 6 February 2023. Archived from the original on 3 March 2024. Retrieved 3 March 2024.
  8. ^ a b "Korsuva- difelikefalin injection, solution". DailyMed. Archived from the original on 12 September 2021. Retrieved 12 September 2021.
  9. ^ a b "Kapruvia EPAR". European Medicines Agency (EMA). 22 February 2022. Archived from the original on 6 May 2022. Retrieved 28 April 2022. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  10. ^
    ISBN 978-1-139-49198-3
    .
  11. ^
    ISBN 978-0-323-29934-3
    .
  12. ^
    ISBN 978-3-662-44605-8
    .
  13. ^
    ISBN 978-1-84973-645-9
    .
  14. ^ "Korsuva: FDA-Approved Drugs". U.S. Food and Drug Administration. Archived from the original on 25 August 2021. Retrieved 24 August 2021.
  15. ^ "Vifor Pharma and Cara Therapeutics announce U.S. FDA approval of Korsuva injection for the treatment of moderate-to-severe pruritus in hemodialysis patients" (Press release). Vifor Pharma. 24 August 2021. Archived from the original on 24 August 2021. Retrieved 24 August 2021 – via Business Wire.
  16. ^ Advancing Health Through Innovation: New Drug Therapy Approvals 2021 (PDF). U.S. Food and Drug Administration (FDA) (Report). 13 May 2022. Archived from the original on 6 December 2022. Retrieved 22 January 2023. Public Domain This article incorporates text from this source, which is in the public domain.
  17. ^ a b "Kapruvia: Pending EC decision". European Medicines Agency. 24 February 2022. Archived from the original on 27 October 2022. Retrieved 26 February 2022. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  18. ^ "Kapruvia Product information". Union Register of medicinal products. Archived from the original on 4 March 2023. Retrieved 3 March 2023.
  19. PMID 31702883
    .

External links


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