User:Mr. Ibrahem/Macitentan

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Mr. Ibrahem/Macitentan
Clinical data
Trade namesOpsumit
Other namesACT-064992
AHFS/Drugs.comMonograph
MedlinePlusa615033
License data
Pregnancy
category
  • AU: X (High risk)
Routes of
administration		By mouth
Drug classEndothelin receptor antagonist (ERA)[1]
Legal status
Legal status
Pharmacokinetic data
MetabolismHydrolysis, oxidation (CYP3A4)
Excretion2/3 urine, 1/3 faeces
Identifiers
  • N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide
Chemical and physical data
FormulaC19H20Br2N6O4S
Molar mass588.28 g·mol−1
3D model (JSmol)
  • Brc1ccc(cc1)c3c(ncnc3OCCOc2ncc(Br)cn2)NS(=O)(=O)NCCC
  • InChI=1S/C19H20Br2N6O4S/c1-2-7-26-32(28,29)27-17-16(13-3-5-14(20)6-4-13)18(25-12-24-17)30-8-9-31-19-22-10-15(21)11-23-19/h3-6,10-12,26H,2,7-9H2,1H3,(H,24,25,27)
  • Key:JGCMEBMXRHSZKX-UHFFFAOYSA-N

Macitentan, sold under the brand name Opsumit, is a medication used to treat pulmonary arterial hypertension (PAH).[3] It may be used alone or with PDE5 inhibitors or prostanoids.[3] It is taken by mouth.[3]

Common side effects include low red blood cells, headache, and sore throat.[1] Other side effects include liver problems, infertility, and pulmonary edema.[3] Use in pregnancy may harm the baby.[3] It is an endothelin receptor antagonist (ERA) which help widen widen the arteries in the lungs.[1]

Macitentan was approved for medical use in the United States and Europe in 2013.[1][3] Approval for a generic version was granted in 2021.[5] In the United Kingdom a month of medication costs the NHS about £2,300 as of 2021.[4] In the United States this amount costs about 11,000 USD.[6]

References

  1. ^ a b c d e "Opsumit". Archived from the original on 21 June 2021. Retrieved 13 November 2021.
  2. ^ "Opsumit- macitentan tablet, film coated". DailyMed. 22 September 2020. Archived from the original on 27 October 2020. Retrieved 24 October 2020.
  3. ^ a b c d e f g "Macitentan Monograph for Professionals". Drugs.com. Archived from the original on 28 October 2020. Retrieved 13 November 2021.
  4. ^ a b BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 198. ISBN 978-0857114105.
  5. ^ "Macitentan: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Archived from the original on 24 June 2021. Retrieved 19 June 2021.
  6. ^ "Opsumit Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 18 April 2021. Retrieved 13 November 2021.
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