Wikipedia

User:Mr. Ibrahem/Difelikefalin

< User:Mr. Ibrahem
Mr. Ibrahem/Difelikefalin
Clinical data
Trade namesKorsuva, Kapruvia
Other namesCR845, FE-202845, D-Phe-D-Phe-D-Leu-D-Lys-[γ-(4-N-piperidinyl)amino carboxylic acid][1]
AHFS/Drugs.comMonograph
License data
Routes of
administration		Intravenous[2]
Drug classKappa opioid receptor agonist[2]
Legal status
Legal status
Pharmacokinetic data
Bioavailability100% (IV)[5]
MetabolismNot metabolized[5]
Elimination half-life2 hours[5]
ExcretionExcreted as unchanged
drug via bile and urine[5]
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
Chemical and physical data
FormulaC36H53N7O6
Molar mass679.863 g·mol−1
3D model (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 a medication used to in itchiness in those on hemodialysis due to chronic kidney disease.[4] It may be used in moderate to severe cases.[6] It is given by injection into a vein at the end of dialysis.[4]

Common side effects include diarrhea, dizziness, nausea, risk of falling, high potassium, headache, and sleepiness.[4] It should not be used in people with significant liver problems.[4] It is a kappa opioid receptor (KOR) agonist which binds to specific nerve and immune cells to decrease itching and inflammation.[2]

Difelikefalin was approved for medical use in the United States in 2021 and Europe in 2022.[4][2] In the United Kingdom it costs the NHS about £420 per vial as of 2022.[6] In the United States it costs about 2,000 USD per month.[7]

References edit

  1. ^ Janecka A, Perlikowska R, Gach K, Wyrebska A, Fichna J (2010). "Development of opioid peptide analogs for pain relief". Curr. Pharm. Des. 16 (9): 1126–35. doi:10.2174/138161210790963869. PMID 20030621.
  2. ^ a b c d e "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.
  3. ^ https://pdf.hres.ca/dpd_pm/00066996.PDF Archived 2022-10-01 at the Wayback Machine [bare URL PDF]
  4. ^ a b c d e f g h i "Korsuva- difelikefalin injection, solution". DailyMed. Archived from the original on 12 September 2021. Retrieved 12 September 2021.
  5. ^ a b c d Raymond S. Sinatra; Jonathan S. Jahr; J. Michael Watkins-Pitchford (14 October 2010). The Essence of Analgesia and Analgesics. Cambridge University Press. pp. 490–491. ISBN 978-1-139-49198-3.
  6. ^ a b "Difelikefalin". SPS - Specialist Pharmacy Service. 10 December 2015. Archived from the original on 24 October 2021. Retrieved 28 October 2022.
  7. ^ Watnick, Suzanne; Butler, Catherine R. (August 2022). "Difelikefalin: A Novel Therapy for Dialysis Patient Care". Kidney Medicine. 4 (8): 100519. doi:10.1016/j.xkme.2022.100519.
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