Tolvaptan phosphate

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.

Tolvaptan phosphate
Clinical data
Trade namesSamtasu
Other namesTolvaptan sodium phosphate; OPC-61815
Identifiers
  • [(5R)-7-Chloro-1-[2-methyl-4-[(2-methylbenzoyl)amino]benzoyl]-2,3,4,5-tetrahydro-1-benzazepin-5-yl] dihydrogen phosphate
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC26H26ClN2O6P
Molar mass528.93 g·mol−1
3D model (JSmol)
  • 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=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

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

References
  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 (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. Retrieved June 11, 2022.
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