User:Mr. Ibrahem/Vorapaxar

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Mr. Ibrahem/Vorapaxar
Clinical data
Trade namesZontivity
Other namesSCH-530348
License data
Routes of
administration		By mouth
Legal status
Legal status
Pharmacokinetic data
Bioavailability~100%[1]
Protein binding≥99%
MetabolismLiver (CYP3A4 and CYP2J2)
Elimination half-life5–13 days
ExcretionFeces (58%), urine (25%)
Identifiers
  • Ethyl N-[(3R,3aS,4S,4aR,7R,8aR,9aR)-4-[(E)-2-[5-(3-fluorophenyl)-2-pyridyl]vinyl]-3-methyl-1-oxo-3a,4,4a,5,6,7,8,8a,9,9a-decahydro-3H-benzo[f]isobenzofuran-7-yl]carbamate
Chemical and physical data
FormulaC29H33FN2O4
Molar mass492.591 g·mol−1
3D model (JSmol)
Melting point278 °C (532 °F)
  • Fc1cccc(c1)c2ccc(nc2)\C=C\[C@H]4[C@H]3[C@@H](C[C@H](NC(=O)OCC)CC3)C[C@H]5C(=O)O[C@@H]([C@@H]45)C
  • InChI=1S/C29H33FN2O4/c1-3-35-29(34)32-23-10-11-24-20(14-23)15-26-27(17(2)36-28(26)33)25(24)12-9-22-8-7-19(16-31-22)18-5-4-6-21(30)13-18/h4-9,12-13,16-17,20,23-27H,3,10-11,14-15H2,1-2H3,(H,32,34)/b12-9+/t17-,20+,23-,24-,25+,26-,27+/m1/s1 ☒N
  • Key:ZBGXUVOIWDMMJE-QHNZEKIYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Vorapaxar, sold under the brand name Zontivity, is a medication used to decrease the risk of heart attacks and stroke in those with atherosclerosis.[2] Overall benefits; however, remain unclear as of 2021.[2] It is taken by mouth.[2]

Common side effects include bleeding, which may include intracranial bleeding.[2] It is a thrombin receptor (protease-activated receptor, PAR-1) blocker based on the natural product himbacine.[3] It works by blocking platelet aggregation.[2]

Vorapaxar was approved for medical use in the United States in 2014.[2] While it was approved for use in Europe in 2015, this approval was withdrawn in 2017.[4][5] In the United States it costs about 370 USD per month as of 2021.[6]

References[edit]

  1. ^ "ZONTIVITY™ (vorapaxar) Tablets 2.08 mg, for oral use. Full Prescribing Information" (PDF). Merck & Co., Inc. Initial U.S. Approval: 05/2014. Archived (PDF) from the original on 17 June 2014. Retrieved 17 June 2014.
  2. ^ a b c d e f g h i "Vorapaxar Monograph for Professionals". Drugs.com. Archived from the original on 24 January 2021. Retrieved 16 September 2021.
  3. ^ Chackalamannil, S; Wang, Y; Greenlee, WJ; Hu, Z; Xia, Y; Ahn, HS; Boykow, G; Hsieh, Y; Palamanda, J; Agans-Fantuzzi, J; Kurowski, S; Graziano, M; Chintala, M (12 June 2008). "Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity". Journal of medicinal chemistry. 51 (11): 3061–4. doi:10.1021/jm800180e. PMID 18447380.
  4. ^ "Zontivity". Archived from the original on 28 November 2020. Retrieved 16 September 2021.
  5. ^ "Zontivity Withdrawal of the marketing authorisation in the European Union" (PDF). Archived (PDF) from the original on 3 June 2019. Retrieved 16 September 2021.
  6. ^ "Zontivity Prices, Coupons & Savings Tips - GoodRx". GoodRx. Archived from the original on 9 August 2016. Retrieved 16 September 2021.
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