Tolvaptan
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| Trade names | Samsca, Jinarc, Jynarque, others |
| Other names | OPC-41061 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a609033 |
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| Routes of administration | By mouth |
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| Pharmacokinetic data | |
| Protein binding | 99% |
| Metabolism | Liver (CYP3A4-mediated)[8] |
| Elimination half-life | 12 hours (terminal) |
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| ECHA InfoCard | 100.219.212 |
| Chemical and physical data | |
| Formula | C26H25ClN2O3 |
| Molar mass | 448.95 g·mol−1 |
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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.[9] Tolvaptan, as Jynarque, was granted approval for medical use in the United States in April 2018.[10]
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.[11] The FDA granted Jynarque an orphan drug designation in April 2012, for the treatment of autosomal dominant polycystic kidney disease.[12]
Tolvaptan is available as a generic medication.[13][14]
- ^ "Tolvaptan GH (Lupin Australia Pty Limited)". Therapeutic Goods Administration (TGA). 14 January 2025. Retrieved 20 January 2025.
- ^ "Samsca 15 mg tablets - Summary of Product Characteristics (SmPC)". (emc). Retrieved 14 December 2020.
- ^ "Jinarc 15 mg tablets - Summary of Product Characteristics (SmPC)". (emc). 21 April 2020. Retrieved 14 December 2020.
- ^ "Jynarque- tolvaptan kit Jynarque- tolvaptan tablet". DailyMed. 31 March 2020. Retrieved 14 December 2020.
- ^ "Samsca- tolvaptan tablet". DailyMed. 26 October 2020. Retrieved 14 December 2020.
- ^ "Samsca EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 14 December 2020.
- ^ "Jinarc EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 14 December 2020.
- ^ Shoaf S, Elizari M, Wang Z, et al. (2005). "Tolvaptan administration does not affect steady state amiodarone concentrations in patients with cardiac arrhythmias". J Cardiovasc Pharmacol Ther. 10 (3): 165–71. doi:10.1177/107424840501000304. PMID 16211205. S2CID 39158242.
- ^ "Drug Approval Package: Samsca (Tolvaptan) Tablets NDA #022275". U.S. Food and Drug Administration (FDA). 21 July 2009. Archived from the original on January 19, 2017. Retrieved 15 August 2020.
- ^ "Drug Approval Package: Jynarque (tolvaptan)". U.S. Food and Drug Administration (FDA). 8 June 2018. Archived from the original on March 30, 2019. Retrieved 15 August 2020.
- ^ "Otsuka Maryland Research Institute, Inc. Granted Fast Track Designation For Tolvaptan In PKD". Medical News Today. Healthline Media UK Ltd. Retrieved 6 December 2018.
- ^ "Tolvaptan Orphan Drug Designations and Approvals". U.S. Food and Drug Administration (FDA). 6 April 2012. Archived from the original on August 29, 2021. Retrieved 15 August 2020.
- ^ "Drugs@FDA: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Archived from the original on October 20, 2020. Retrieved 15 August 2020.
- ^ "Tolvaptan Accord: Pending EC decision". European Medicines Agency (EMA). 26 January 2023. Archived from the original on 27 January 2023. Retrieved 28 January 2023.