Tolvaptan phosphate

Tolvaptan phosphate
Clinical data
Trade names	Samtasu
Other names	Tolvaptan sodium phosphate; OPC-61815
Identifiers
	IUPAC name [(5R)-7-Chloro-1-[2-methyl-4-[(2-methylbenzoyl)amino]benzoyl]-2,3,4,5-tetrahydro-1-benzazepin-5-yl] dihydrogen phosphate;
CAS Number	942619-74-1 ;
PubChem CID	146035877 ;
ChemSpider	17342600 ;
UNII	Y4P6WS9QVF ;
KEGG	D11659 ;
Chemical and physical data
Formula	C26H26ClN2O6P
Molar mass	528.93 g·mol−1
3D model (JSmol)	Interactive image ;
	SMILES CC1=CC=CC=C1C(=O)NC2=CC(=C(C=C2)C(=O)N3CCCC(C4=C3C=CC(=C4)Cl)OP(=O)(O)O)C;
	InChI InChI=InChI=1S/C26H26ClN2O6P/c1-16-6-3-4-7-20(16)25(30)28-19-10-11-21(17(2)14-19)26(31)29-13-5-8-24(35-36(32,33)34)22-15-18(27)9-12-23(22)29/h3-4,6-7,9-12,14-15,24H,5,8,13H2,1-2H3,(H,28,30)(H2,32,33,34)/t24-/m1/s1; Key:XTCFGVRVASPRTK-XMMPIXPASA-N;

Last updated January 02, 2026

Tolvaptan phosphate is a drug used for the treatment of cardiac edema. It is a prodrug of tolvaptan,^[1]^[2] formulated as the salt tolvaptan sodium phosphate, for intravenous administration. Tolvaptan phosphate is converted into the active drug tolvaptan in the human body following administration.

It was developed by Otsuka Pharmaceutical Co. and was approved for use in Japan in 2022.^[3]

References

↑ Kinugawa K, Nakata E, Hirano T, Kim S (March 2022). "Tolerability of the Intravenously Administered Tolvaptan Prodrug, OPC-61815, in Patients With Congestive Heart Failure Who Have Difficulty With, or Are Incapable of, Oral Intake (TRITON-HF) - A Phase III, Multicenter, Open-Label Trial". Circulation Journal. 86 (7): 1068–1078. doi: 10.1253/circj.CJ-21-0926 . PMID 35264514. S2CID 247362001.
↑ Sato N, Uno S, Yamasaki Y, Hirano T, Kim S, et al. (OPC-61815 Investigators) (March 2022). "Pharmacokinetics, Pharmacodynamics, Efficacy, and Safety of OPC-61815, a Prodrug of Tolvaptan for Intravenous Administration, in Patients With Congestive Heart Failure - A Phase II, Multicenter, Double-Blind, Randomized, Active-Controlled Trial". Circulation Journal. 86 (4): 699–708. doi: 10.1253/circj.CJ-21-0430 . PMID 34511586. S2CID 237493273.
↑ "Otsuka Obtains Approval in Japan for SAMTASU® for I.V. Infusion, a V2 -Receptor Antagonist for the Treatment of Cardiac Edema" (Press release). Otsuka Pharmaceutical Co., Ltd. March 28, 2022. Archived from the original on November 13, 2022. Retrieved June 11, 2022.

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[1] Kinugawa K, Nakata E, Hirano T, Kim S (March 2022). "Tolerability of the Intravenously Administered Tolvaptan Prodrug, OPC-61815, in Patients With Congestive Heart Failure Who Have Difficulty With, or Are Incapable of, Oral Intake (TRITON-HF) - A Phase III, Multicenter, Open-Label Trial". Circulation Journal. 86 (7): 1068–1078. doi: 10.1253/circj.CJ-21-0926 . PMID 35264514. S2CID 247362001.

[2] Sato N, Uno S, Yamasaki Y, Hirano T, Kim S, et al. (OPC-61815 Investigators) (March 2022). "Pharmacokinetics, Pharmacodynamics, Efficacy, and Safety of OPC-61815, a Prodrug of Tolvaptan for Intravenous Administration, in Patients With Congestive Heart Failure - A Phase II, Multicenter, Double-Blind, Randomized, Active-Controlled Trial". Circulation Journal. 86 (4): 699–708. doi: 10.1253/circj.CJ-21-0430 . PMID 34511586. S2CID 237493273.

[3] "Otsuka Obtains Approval in Japan for SAMTASU® for I.V. Infusion, a V2 -Receptor Antagonist for the Treatment of Cardiac Edema" (Press release). Otsuka Pharmaceutical Co., Ltd. March 28, 2022. Archived from the original on November 13, 2022. Retrieved June 11, 2022.

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