User:Mr. Ibrahem/Upadacitinib

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Mr. Ibrahem/Upadacitinib
Clinical data
Trade namesRinvoq
Other namesABT-494
AHFS/Drugs.comMonograph
MedlinePlusa619051
License data
Pregnancy
category
  • AU: D
  • Not recommended[1]
Routes of
administration		By mouth
Drug classJanus kinase (JAK) inhibitor[2]
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)[3]
  • US: ℞-only[4]
  • EU: Rx-only[5]
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Protein binding52%
MetabolismHepatic (CYP3A major, CYP2D6 minor)[7]
MetabolitesM4, an acyl glucuronide
Elimination half-life9–14[6] (6–15[7]) hours
ExcretionMainly unchanged in feces (38%) and urine (24%)[6]
Identifiers
  • (3S,4R)-3-Ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide
Chemical and physical data
FormulaC17H19F3N6O
Molar mass380.375 g·mol−1
3D model (JSmol)
  • CCC1CN(CC1C2=CN=C3N2C4=C(NC=C4)N=C3)C(=O)NCC(F)(F)F
  • InChI=1S/C17H19F3N6O/c1-2-10-7-25(16(27)24-9-17(18,19)20)8-11(10)13-5-22-14-6-23-15-12(26(13)14)3-4-21-15/h3-6,10-11,21H,2,7-9H2,1H3,(H,24,27)/t10-,11+/m1/s1 checkY
  • Key:WYQFJHHDOKWSHR-MNOVXSKESA-N checkY

Upadacitinib, sold under the brand name Rinvoq, is a medication used to treat moderate to severe rheumatoid arthritis (RA) where methotrexate was not sufficiently effective.[2] While it may be used together with conventional RA medication, use with immunosuppressive agent is not recommended.[2] It is taken by mouth.[2]

Common side effects include upper respiratory tract infections (such as the common cold), nausea, cough, and fever.[8][2] Other side effects may include serious infections, blood clots, and cancer.[2] Use during pregnancy may harm the baby.[2] Use in those with active tuberculosis is not recommended.[9] Upadacitinib works by blocking the action of enzymes called Janus kinases, which results in decreased inflammation.[2][8]

Upadacitinib was approved for medical use in Europe and the United States in 2019.[8][2] Per year, in Canada it costs about 18,000 CAD as of 2019, in the United States it costs about 67,000 USD, while in the United Kingdom this amount costs the NHS about £10,500 as of 2021.[10][11][9]

References[edit]

  1. ^ a b "Upadacitinib (Rinvoq) Use During Pregnancy". Drugs.com. 23 September 2019. Archived from the original on 18 March 2020. Retrieved 17 March 2020.
  2. ^ a b c d e f g h i j k l "Upadacitinib Monograph for Professionals". Drugs.com. Archived from the original on 22 August 2021. Retrieved 13 September 2021.
  3. ^ "Rinvoq 15 mg prolonged-release tablets - Summary of Product Characteristics (SmPC)". (emc). 1 March 2020. Archived from the original on 27 August 2021. Retrieved 22 August 2020.
  4. ^ "Rinvoq- upadacitinib tablet, extended release". DailyMed. 1 March 2020. Archived from the original on 27 August 2021. Retrieved 29 April 2020.
  5. ^ "Rinvoq EPAR". European Medicines Agency (EMA). 16 October 2019. Archived from the original on 20 October 2020. Retrieved 29 April 2020.
  6. ^ a b "Rinvoq: EPAR – Public assessment report" (PDF). European Medicines Agency. 2020-03-05. Archived (PDF) from the original on 2020-07-21. Retrieved 2021-06-05.
  7. ^ a b Mohamed MF, Camp HS, Jiang P, Padley RJ, Asatryan A, Othman AA (December 2016). "Pharmacokinetics, Safety and Tolerability of ABT-494, a Novel Selective JAK 1 Inhibitor, in Healthy Volunteers and Participants with Rheumatoid Arthritis". Clinical Pharmacokinetics. 55 (12): 1547–1558. doi:10.1007/s40262-016-0419-y. PMID 27272171. S2CID 39036534.
  8. ^ a b c "Rinvoq". Archived from the original on 20 October 2020. Retrieved 13 September 2021.
  9. ^ a b BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 1169. ISBN 978-0-85711-369-6.{{cite book}}: CS1 maint: date format (link)
  10. ^ Pharmacoeconomic Review Report: Upadacitinib (Rinvoq): (AbbVie): Indication: For the treatment of adults with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to methotrexate. Canadian Agency for Drugs and Technologies in Health. 2020. Archived from the original on 23 September 2021. Retrieved 13 September 2021.
  11. ^ "Rinvoq Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 16 January 2021. Retrieved 13 September 2021.
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