托伐普坦

托伐普坦
臨床資料
商品名	Samsca, Jinarc, Jynarque, others
其他名稱	OPC-41061
AHFS/Drugs.com	Monograph
MedlinePlus	a609033
核准狀況	美 DailyMed: Tolvaptan;
懷孕分級	英國：禁用;
给药途径	口服給藥
ATC碼	C03XA01 (WHO) ;
法律規範狀態
法律規範	澳：限医生处方（S4）; 歐：Rx-only; 英：处方药（℞-only） (POM); 美：处方药（℞-only）;
藥物動力學數據
血漿蛋白結合率	99%
药物代谢	Liver (CYP3A4-mediated)
生物半衰期	12 hours (terminal)
识别信息
	IUPAC命名法 N-(4-{[(5R)-7-Chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl}-3-methylphenyl)-2-methylbenzamide; ;
CAS号	150683-30-0
PubChem CID	216237;
IUPHAR/BPS	2226;
DrugBank	DB06212 ;
ChemSpider	187438 ;
UNII	21G72T1950;
KEGG	D01213;
ChEBI	CHEBI:32246;
ChEMBL	ChEMBL344159 ;
CompTox Dashboard (EPA)	DTXSID3048780 ;
ECHA InfoCard	100.219.212
化学信息
化学式	C26H25ClN2O3
摩尔质量	448.95 g·mol−1
3D模型（JSmol）	交互式图像;
	SMILES Cc1ccccc1C(=O)Nc2cc(C)c(cc2)C(=O)N3c4ccc(Cl)cc4[C@H](O)CCC3;
	InChI InChI=1S/C26H25ClN2O3/c1-16-6-3-4-7-20(16)25(31)28-19-10-11-21(17(2)14-19)26(32)29-13-5-8-24(30)22-15-18(27)9-12-23(22)29/h3-4,6-7,9-12,14-15,24,30H,5,8,13H2,1-2H3,(H,28,31) ; Key:GYHCTFXIZSNGJT-UHFFFAOYSA-N ;

Tolvaptan（暫譯：托伐普坦，台灣商品名Jinarc（佳腎康），另有Samsca等商品名），是血管加壓素受體2的选择性競爭性拮抗劑，有利尿作用，用於治疗鬱血性心衰竭、肝硬化和抗利尿激素分泌異常症候群（SIADH）相关的低血鈉症，於2009 年 5 月 19 日获得美国食品药品监督管理局(FDA) 批准^[9]^[10]。

2012 年 4 月，FDA 授予托伐普坦孤儿药资格，用于治疗體染色體顯性的多囊性腎病變^[11]。托伐普坦現為學名药^[12] ^[13]。

医疗用途

托伐普坦（商品名 Samsca）適應症為治疗高血容性低血鈉症和正常血容性低血鈉症。^[14]

托伐普坦（商品名 Jynarque）適應症為用於患有體染色體顯性多囊性腎病變而有急速惡化風險之病人，減緩其肾功能衰退^[15]。

静脉注射劑型為磷酸托伐普坦（tolvaptan phosphate），其為前体药物，在人体内转化为活性药物托伐普坦^[16]。

副作用

依據美国食品药品监督管理局规定，托伐普坦的使用时间不應超过 30 天，且因可能傷害肝臟甚至導致肝功能衰竭，不应用于已有肝病的患者。應注意，用于治疗低血钠症时，有可能因矯治低血鈉過快，造成致命性的滲透性脫髓鞘症候群。^[17]

药理與化學

托伐普坦是选择性加压素 V ₂受体拮抗剂^[18]^[19]。其為外消旋体，是兩种对映异构体的 1:1 混合物：

托伐普坦的对映异构体
（ R ）-托伐普坦 CAS编号：331947-66-1	（ S ）-托伐普坦 CAS编号：331947-44-5

参考資料

^ Tolvaptan GH (Lupin Australia Pty Limited). Therapeutic Goods Administration (TGA). 14 January 2025 [20 January 2025].
^ Samsca 15 mg tablets - Summary of Product Characteristics (SmPC). (emc). [14 December 2020].
^ Jinarc 15 mg tablets - Summary of Product Characteristics (SmPC). (emc). 21 April 2020 [14 December 2020].
^ Jynarque- tolvaptan kit Jynarque- tolvaptan tablet. DailyMed. 31 March 2020 [14 December 2020].
^ Samsca- tolvaptan tablet. DailyMed. 26 October 2020 [14 December 2020].
^ Samsca EPAR. European Medicines Agency (EMA). 17 September 2018 [14 December 2020].
^ Jinarc EPAR. European Medicines Agency (EMA). 17 September 2018 [14 December 2020].
^ Shoaf S, Elizari M, Wang Z, et al. Tolvaptan administration does not affect steady state amiodarone concentrations in patients with cardiac arrhythmias. J Cardiovasc Pharmacol Ther. 2005, 10 (3): 165–71. PMID 16211205. S2CID 39158242. doi:10.1177/107424840501000304 .
^ Drug Approval Package: Samsca (Tolvaptan) Tablets NDA #022275. U.S. Food and Drug Administration (FDA). 21 July 2009 [15 August 2020]. （原始内容存档于January 19, 2017）.
^ Drug Approval Package: Jynarque (tolvaptan). U.S. Food and Drug Administration (FDA). 8 June 2018 [15 August 2020]. （原始内容存档于March 30, 2019）.
^ Tolvaptan Orphan Drug Designations and Approvals. U.S. Food and Drug Administration (FDA). 6 April 2012 [15 August 2020]. （原始内容存档于August 29, 2021）.
^ Drugs@FDA: FDA-Approved Drugs. U.S. Food and Drug Administration (FDA). [15 August 2020]. （原始内容存档于October 20, 2020）.
^ Tolvaptan Accord: Pending EC decision. European Medicines Agency (EMA). 26 January 2023 [28 January 2023]. （原始内容存档于27 January 2023）.
^ Samsca- tolvaptan tablet. DailyMed. 28 May 2019 [15 August 2020].
^ Jynarque- tolvaptan kit Jynarque- tolvaptan tablet. DailyMed. 31 March 2020 [15 August 2020].
^ Otsuka Obtains Approval in Japan for SAMTASU® for I.V. Infusion, a V2 -Receptor Antagonist for the Treatment of Cardiac Edema (新闻稿). March 28, 2022 [June 11, 2022].
^ Goodman & Gilman's the pharmacological basis of therapeutics. Brunton, Laurence L, Knollmann, Björn C, Hilal-Dandan, Randa Thirteenth. New York. 5 December 2017. ISBN 9781259584732. OCLC 994570810.
^ DailyMed - SAMSCA- tolvaptan tablet. dailymed.nlm.nih.gov. [2025-10-15].
^ DailyMed - JYNARQUE- tolvaptan kit JYNARQUE- tolvaptan tablet. dailymed.nlm.nih.gov. [2025-10-15].

[1] Tolvaptan GH (Lupin Australia Pty Limited). Therapeutic Goods Administration (TGA). 14 January 2025 [20 January 2025].

[2] Samsca 15 mg tablets - Summary of Product Characteristics (SmPC). (emc). [14 December 2020].

[3] Jinarc 15 mg tablets - Summary of Product Characteristics (SmPC). (emc). 21 April 2020 [14 December 2020].

[4] Jynarque- tolvaptan kit Jynarque- tolvaptan tablet. DailyMed. 31 March 2020 [14 December 2020].

[5] Samsca- tolvaptan tablet. DailyMed. 26 October 2020 [14 December 2020].

[Samsca_EPAR-6] Samsca EPAR. European Medicines Agency (EMA). 17 September 2018 [14 December 2020].

[Jinarc_EPAR-7] Jinarc EPAR. European Medicines Agency (EMA). 17 September 2018 [14 December 2020].

[pk-8] Shoaf S, Elizari M, Wang Z, et al. Tolvaptan administration does not affect steady state amiodarone concentrations in patients with cardiac arrhythmias. J Cardiovasc Pharmacol Ther. 2005, 10 (3): 165–71. PMID 16211205. S2CID 39158242. doi:10.1177/107424840501000304 .

[9] Drug Approval Package: Samsca (Tolvaptan) Tablets NDA #022275. U.S. Food and Drug Administration (FDA). 21 July 2009 [15 August 2020]. （原始内容存档于January 19, 2017）.

[10] Drug Approval Package: Jynarque (tolvaptan). U.S. Food and Drug Administration (FDA). 8 June 2018 [15 August 2020]. （原始内容存档于March 30, 2019）.

[11] Tolvaptan Orphan Drug Designations and Approvals. U.S. Food and Drug Administration (FDA). 6 April 2012 [15 August 2020]. （原始内容存档于August 29, 2021）.

[12] Drugs@FDA: FDA-Approved Drugs. U.S. Food and Drug Administration (FDA). [15 August 2020]. （原始内容存档于October 20, 2020）.

[13] Tolvaptan Accord: Pending EC decision. European Medicines Agency (EMA). 26 January 2023 [28 January 2023]. （原始内容存档于27 January 2023）.

[Samsca_FDA_label-14] Samsca- tolvaptan tablet. DailyMed. 28 May 2019 [15 August 2020].

[Jynarque_FDA_label-15] Jynarque- tolvaptan kit Jynarque- tolvaptan tablet. DailyMed. 31 March 2020 [15 August 2020].

[16] Otsuka Obtains Approval in Japan for SAMTASU® for I.V. Infusion, a V2 -Receptor Antagonist for the Treatment of Cardiac Edema (新闻稿). March 28, 2022 [June 11, 2022].

[17] Goodman & Gilman's the pharmacological basis of therapeutics. Brunton, Laurence L, Knollmann, Björn C, Hilal-Dandan, Randa Thirteenth. New York. 5 December 2017. ISBN 9781259584732. OCLC 994570810.

[18] DailyMed - SAMSCA- tolvaptan tablet. dailymed.nlm.nih.gov. [2025-10-15].

[19] DailyMed - JYNARQUE- tolvaptan kit JYNARQUE- tolvaptan tablet. dailymed.nlm.nih.gov. [2025-10-15].

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