Mr. Ibrahem/Icatibant
Clinical data
Trade namesFirazyr
Other namesHoe 140, JE 049[1]
AHFS/Drugs.comMonograph
License data
Pregnancy
category
  • AU: C
Routes of
administration
Subcutaneous
Drug classBradykinin B2 receptors inhibitor[2]
Legal status
Legal status
  • AU: S4 (Prescription only)
  • US: ℞-only[2]
  • EU: Rx-only[3]
  • In general: ℞ (Prescription only)
Identifiers
  • (2S)-2-[[(3aS,7aS)-1-[2-[(2S)-2-[[(2S)-
    2-[[2-[[(4R)-1-[1-[2-[[(2R)-2-amino-5-(diaminomethylideneamino)
    pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-
    2-carbonyl]-4-hydroxypyrrolidine-2-carbonyl]amino]acetyl]amino]-
    3-thiophen-2-ylpropanoyl]amino]-3-hydroxypropanoyl]
    3,4-dihydro-1H-isoquinoline-3-carbonyl]
    2,3,3a,4,5,6,7,7a-octahydroindole-2-carbonyl]amino]-
    5-(diaminomethylideneamino)pentanoic acid
Chemical and physical data
FormulaC59H89N19O13S
Molar mass1304.54 g·mol−1
3D model (JSmol)
  • C1CC[C@H]2[C@@H](C1)CC(N2C(=O)C3CC4=CC=CC=C4CN3C(=O)[C@H](CO)NC(=O)[C@H](CC5=CC=CS5)NC(=O)CNC(=O)C6C[C@H](CN6C(=O)C7CCCN7C(=O)C(CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)N)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O
  • InChI=1S/C59H89N19O13S/c60-37(14-5-19-67-57(61)62)48(82)72-38(15-6-20-68-58(63)64)52(86)75-22-8-18-43(75)54(88)77-30-35(80)26-44(77)50(84)70-28-47(81)71-40(27-36-13-9-23-92-36)49(83)74-41(31-79)53(87)76-29-34-12-2-1-10-32(34)24-46(76)55(89)78-42-17-4-3-11-33(42)25-45(78)51(85)73-39(56(90)91)16-7-21-69-59(65)66/h1-2,9-10,12-13,23,33,35,37-46,79-80H,3-8,11,14-22,24-31,60H2,(H,70,84)(H,71,81)(H,72,82)(H,73,85)(H,74,83)(H,90,91)(H4,61,62,67)(H4,63,64,68)(H4,65,66,69)/t33-,35+,37+,38-,39-,40-,41-,42-,43-,44-,45?,46+/m0/s1 checkY
  • Key:QURWXBZNHXJZBE-OVZQYVDUSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Icatibant, sold under the brand name Firazyr, is a medication used to treat attacks of hereditary angioedema (HAE) in people with insufficient C1-esterase inhibitor.[2][3] It does not appear effective for angioedema due to ACE inhibitors.[4][5] It is given by injection under the skin.[3]

Common side effects include redness, itching, and pain at the site of injection.[3] Other side effects may include fever, headache, and nausea.[6] Safety in pregnancy is unclear.[7] It is a bradykinin B2 receptors inhibitor.[2]

Icatibant was approved for medical use in Europe in 2008 and the United States in 2011.[3][8] In the United Kingdom it costs the NHS about £1,400 per dose.[6] In the United States this amount costs about 3,600 USD.[9]

References edit

  1. ^ "Icatibant: HOE 140, JE 049, JE049". Drugs in R&D. 5 (6): 343–8. 2004. doi:10.2165/00126839-200405060-00006. PMID 15563238.
  2. ^ a b c d e f "Firazyr- icatibant acetate injection, solution". DailyMed. 16 December 2019. Archived from the original on 3 August 2020. Retrieved 17 April 2020.
  3. ^ a b c d e f "Firazyr EPAR". European Medicines Agency (EMA). Archived from the original on 12 April 2020. Retrieved 17 April 2020.
  4. ^ Jeon, J; Lee, YJ; Lee, SY (October 2019). "Effect of icatibant on angiotensin-converting enzyme inhibitor-induced angioedema: A meta-analysis of randomized controlled trials". Journal of clinical pharmacy and therapeutics. 44 (5): 685–692. doi:10.1111/jcpt.12997. PMID 31290163.
  5. ^ Sinert R, Levy P, Bernstein JA, Body R, Sivilotti ML, Moellman J, et al. (September–October 2017). "Randomized Trial of Icatibant for Angiotensin-Converting Enzyme Inhibitor-Induced Upper Airway Angioedema". The Journal of Allergy and Clinical Immunology. In Practice. 5 (5): 1402–1409.e3. doi:10.1016/j.jaip.2017.03.003. PMID 28552382.
  6. ^ a b BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 306. ISBN 978-0857114105.
  7. ^ "Icatibant (Firazyr) Use During Pregnancy". Drugs.com. Archived from the original on 4 December 2020. Retrieved 25 November 2021.
  8. ^ "Icatibant Monograph for Professionals". Drugs.com. Archived from the original on 23 January 2021. Retrieved 25 November 2021.
  9. ^ "Icatibant Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 24 January 2021. Retrieved 25 November 2021.