Tolvaptan Explained

Tolvaptan, sold under the brand name Samsca among others, is an aquaretic drug that functions as a selective, competitive vasopressin receptor 2 (V2) antagonist used to treat hyponatremia (low blood sodium levels) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH). Tolvaptan was approved by the U.S. Food and Drug Administration (FDA) on May 19, 2009, and is sold by Otsuka Pharmaceutical Co. under the trade name Samsca.[1] Tolvaptan, as Jynarque, was granted approval for medical use in the United States in April 2018.[2]

The U.S. Food and Drug Administration (FDA) granted tolvaptan a fast track designation for clinical trials investigating its use for the treatment of polycystic kidney disease.[3] The FDA granted Jynarque an orphan drug designation in April 2012, for the treatment of autosomal dominant polycystic kidney disease.[4]

Tolvaptan is available as a generic medication.[5] [6]

Medical uses

Tolvaptan (Samsca) is indicated for the treatment of clinically significant hypervolemic and euvolemic hyponatremia.[7]

Tolvaptan (Jynarque) is indicated for slow kidney-function decline in adults at risk of rapidly progressing autosomal dominant polycystic kidney disease (ADPKD).[8]

Tolvaptan phosphate is a prodrug of tolvaptan, developed for intravenous administration. Tolvaptan phosphate is converted into the active drug tolvaptan in the human body following administration.[9]

Side effects

The FDA has determined that tolvaptan should not be used for longer than 30 days and should not be used in patients with underlying liver disease because it can cause liver injury, potentially leading to liver failure.[10] When using to treat hyponatremia, it may cause too rapid correction of hyponatremia resulting in fatal osmotic demyelination syndrome.[11]

Pharmacology

Tolvaptan is a selective vasopressin V2 receptor antagonist.

Chemistry

Tolvaptan is a racemate, a 1:1 mixture of the following two enantiomers:[12]

Further reading

External links

Notes and References

  1. Web site: Drug Approval Package: Samsca (Tolvaptan) Tablets NDA #022275 . U.S. Food and Drug Administration (FDA) . 21 July 2009 . 15 August 2020.
  2. Web site: Drug Approval Package: Jynarque (tolvaptan) . U.S. Food and Drug Administration (FDA) . 8 June 2018 . 15 August 2020.
  3. Web site: Otsuka Maryland Research Institute, Inc. Granted Fast Track Designation For Tolvaptan In PKD . Medical News Today . Healthline Media UK Ltd . 6 December 2018 .
  4. Web site: Tolvaptan Orphan Drug Designations and Approvals . U.S. Food and Drug Administration (FDA) . 6 April 2012 . 15 August 2020.
  5. Web site: Drugs@FDA: FDA-Approved Drugs . U.S. Food and Drug Administration (FDA) . 15 August 2020.
  6. Web site: Tolvaptan Accord: Pending EC decision . European Medicines Agency (EMA) . 26 January 2023 . 28 January 2023.
  7. Web site: Samsca- tolvaptan tablet . DailyMed . 28 May 2019 . 15 August 2020.
  8. Web site: Jynarque- tolvaptan kit Jynarque- tolvaptan tablet . DailyMed . 31 March 2020 . 15 August 2020.
  9. Otsuka Obtains Approval in Japan for SAMTASU® for I.V. Infusion, a V2 -Receptor Antagonist for the Treatment of Cardiac Edema . March 28, 2022 . June 11, 2022.
  10. "U.S. Food and Drug Administration." Samsca (Tolvaptan): Drug Safety Communication. N.p., 30 Apr. 2013. Web. 1 June 2014.
  11. Book: Goodman & Gilman's the pharmacological basis of therapeutics. Brunton, Laurence L, Knollmann, Björn C, Hilal-Dandan, Randa. 5 December 2017. 9781259584732. Thirteenth. New York. 994570810.
  12. Rote Liste Service GmbH (Hrsg.): Rote Liste 2017 - Arzneimittelverzeichnis für Deutschland (einschließlich EU-Zulassungen und bestimmter Medizinprodukte). Rote Liste Service GmbH, Frankfurt/Main, 2017, Aufl. 57,, S. 222.

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