Tolvaptan phosphate explained

Tradename:	Samtasu
Synonyms:	Tolvaptan sodium phosphate; OPC-61815
Cas Number:	942619-74-1
Pubchem:	146035877
Kegg:	D11659
Chemspiderid:	17342600
Unii:	Y4P6WS9QVF
Iupac Name:	[(5''R'')-7-Chloro-1-[2-methyl-4-[(2-methylbenzoyl)amino]benzoyl]-2,3,4,5-tetrahydro-1-benzazepin-5-yl] dihydrogen phosphate
C:	26
H:	26
Cl:	1
N:	2
O:	6
P:	1
Smiles:	CC1=CC=CC=C1C(=O)NC2=CC(=C(C=C2)C(=O)N3CCCC(C4=C3C=CC(=C4)Cl)OP(=O)(O)O)C
Stdinchi:	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
Stdinchikey:	XTCFGVRVASPRTK-XMMPIXPASA-N

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]

Notes and References

Kinugawa K, Nakata E, Hirano T, Kim S . 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 . March 2022 . 86 . 7 . 1068–1078 . 35264514 . 10.1253/circj.CJ-21-0926 . 247362001 . free .
Sato N, Uno S, Yamasaki Y, Hirano T, Kim S . 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 . March 2022 . 34511586 . 10.1253/circj.CJ-21-0430 . 237493273 . OPC-61815 Investigators . free .
Otsuka Pharmaceutical Co., Ltd. . 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.