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更新于：2026-01-20
Tolvaptan Sodium Phosphate
托伐普坦磷酸钠
更新于：2026-01-20
概要
基本信息
非在研机构 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 日本 (2022-03-28), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C26H26ClN2NaO6P |
InChIKeyPWJANPIMBWGICU-UHFFFAOYSA-N |
CAS号942619-79-6 |
关联
12
项与 托伐普坦磷酸钠 相关的临床试验JPRN-jRCTs031230062
Usefulness of tolvaptan sodium phosphate (Samtas) in the perioperative period of pediatric cardiac surgery
NCT05712746
Samtasu Post-marketing General Drug Use-results Survey in Patients with Volume Overload in Heart Failure.
NCT05439148
A Phase I, Open-label, Single- and Multi-Dose Study to Evaluate the Safety, Pharmacokinetics, and Pharmacological Effect of OPC-61815 in Healthy Chinese Male Subjects
100 项与 托伐普坦磷酸钠 相关的临床结果
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100 项与 托伐普坦磷酸钠 相关的转化医学
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100 项与 托伐普坦磷酸钠 相关的专利（医药）
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8
项与 托伐普坦磷酸钠 相关的文献（医药）2025-10-01INTERNATIONAL JOURNAL OF HEMATOLOGY
Utility of tolvaptan sodium phosphate for refractory fluid retention in post-transplant sinusoidal obstruction syndrome
Article
作者: Oshiro, Hiroko ; Inukai, Takeshi ; Akahane, Koshi ; Kasai, Shin ; Goi, Kumiko ; Sugita, Yukihiro ; Tamai, Minori
Abstract:
Sinusoidal obstruction syndrome (SOS) is a life-threatening complication of hematopoietic stem cell transplantation (HSCT), particularly in patients with a high HokUS-10 score after starting treatment. Tolvaptan sodium phosphate (TSP) is a novel intravenous aquaretic agent used to treat refractory fluid retention in congestive heart failure (CHF). Here, we report the successful treatment of severe post-HSCT SOS with refractory fluid retention and CHF using TSP plus defibrotide. A 22-year-old man with relapsed acute lymphoblastic leukemia underwent unrelated peripheral blood stem cell transplantation and developed SOS on day 13. Despite defibrotide therapy and standard management, fluid retention rapidly progressed, resulting in an 18.3% increase in body weight on day 21 and a high HokUS-10 score (10/13 points). TSP (16 mg) administered to treat the CHF immediately induced adequate urine output. Continued TSP treatment (8 mg/day) resulted in sustained diuresis and a return to baseline body weight on day 33. The only significant adverse event observed during the 5 weeks of TSP treatment was transient hypernatremia (148 mEq/L). Defibrotide was discontinued on day 72 because the HokUS-10 score had decreased to 1 point. Our experience suggests the utility of TSP in controlling refractory fluid retention due to post-HSCT SOS.
2025-08-29European heart journal open
Prognostic impact of the acute reactiveness to intravenous administration of tolvaptan sodium phosphate in patients with acute decompensated heart failure
Article
作者: Takahashi, Norihito ; Iwata, Hiroshi ; Moriya, Soshi ; Ouchi, Shohei ; Minamino, Tohru ; Kasai, Takatoshi ; Naito, Ryo
Abstract:
Aims:
Intravenous tolvaptan sodium phosphate (IV-tolvaptan) is a novel aquaretic agent for acute decompensated heart failure (ADHF). This study evaluated its short-term effects and prognostic implications in clinical practice.
Methods and results:
In this retrospective cohort of 169 consecutive ADHF patients receiving IV-tolvaptan for the first time (mean age 76.0 ± 12.7 years; 50.9% female), we measured hourly urine output over 6 h and assessed clinical and biochemical parameters at baseline and 24 h post-dose. The primary endpoint was a composite of all-cause mortality and heart failure rehospitalization. At 24 h, IV-tolvaptan significantly reduced body weight (mean difference: −1.1 ± 2.3 kg, P < 0.001), NT-proBNP (median change: −1704 pg/mL; P < 0.001), and urinary osmolality (mean change: −71.4 ± 169.4 mOsm/kg; P = 0.015), while raising serum sodium (mean change: 1.7 ± 2.9 mEq/L; P < 0.001). Six-hour urine output correlated with baseline estimated glomerular filtration rate (eGFR) (r = 0.34; P < 0.001), urinary osmolality (r = 0.28; P = 0.003), and the change in serum sodium (r = 0.21; P = 0.005). In multivariable logistic regression, renal impairment (eGFR < 60 mL/min/1.73m2) [odds ratio (OR) 0.2; 95% confidence interval (CI) 0.1–0.4; P < 0.001] and higher furosemide doses (>20 mg) (OR 0.3; 95% CI 0.2–0.6; P = 0.01) predicted reduced responsiveness, whereas first hospitalization (OR 2.2; 95% CI 1.1–4.5; P = 0.04) and high urinary osmolality (OR 2.3; 95% CI 1.0–5.4; P = 0.05) predicted favourable response. Kaplan–Meier analysis demonstrated a lower incidence of the primary endpoint in patients achieving ≥ 1000 mL urine output (log-rank P = 0.032).
Conclusion:
Intravenous tolvaptan sodium phosphate enhances decongestion and short-term outcomes in ADHF without worsening renal function. Early diuretic responsiveness is a robust prognostic marker.
2024-07-01JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
Development, validation and application of a UPLC-MS/MS method for simultaneous quantification of OPC-61815 and its metabolites tolvaptan, DM-4103 and DM-4107 in human plasma
Article
作者: Wang, Hongyun ; Ma, Yufang ; Yu, Mengyang
OPC-61815 is an intravenous formulation vasopressin antagonist designed to treat heart failure patients, especially who have difficulty in oral intake. Tolvaptan together with DM-4103 and DM-4107 are considered as the major metabolites of OPC-61815 biotransformed in the liver via cytochrome P450 (CYP) 3A. An efficient and robust ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for quantification of OPC-61815 and its three metabolites in human plasma was developed and fully validated. To our best knowledge, it was the first published method that simultaneously quantified all of these four analytes in only one run. Simple and rapid sample preparation procedure and very short UPLC-MS/MS run time (3.5 min) offered OPC-61815 and its metabolites relatively high throughput detection, which was greatly beneficial to further clinical bio-sample analysis. The method showed good linearity and sufficient sensitivity in the range of 2.00-1000 ng/mL with a low limit of quantitation (2.00 ng/mL) for each analyte. For samples with concentrations above 1000 ng/mL, 100-fold dilution with blank plasma before sample preparation was accepted. High precision and accuracy, high selectivity and satisfactory recovery of this method were demonstrated. For all of the four analytes, no significant matrix effect or carry-over was observed. The stability of analytes and internal standards under different conditions were evaluated to ensure they were stable during the whole period of storage, preparation and detection. Also, re-injection reproducibility was investigated. In addition, the conversion test showed that almost no OPC-61815 converted into DM-4103 and DM-4107 during sample processing, while attention should be paid to the concentration difference between OPC-61815 and tolvaptan in bioanalysis. The developed UPLC-MS/MS method was successfully applied to an open, single and multiple dose administration phase I trial for monitoring the pharmacokinetics of OPC-61815. This work provided a promising way for further pharmacokinetic study of OPC-61815.
100 项与 托伐普坦磷酸钠 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 体液潴留 | 日本 | 2022-03-28 |
未上市
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 心脏衰竭 | 申请上市 | 中国 | 2023-12-15 | |
| 心源性水肿 | 申请上市 | 中国 | - |
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临床结果
临床结果
适应症
分期
评价
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临床1期 | - | 8 | 廠鹹鹽壓顧齋壓膚範遞(網鹹醖蓋糧醖選襯窪顧) = 構餘鏇窪蓋鏇製壓構艱 廠網鹹糧醖鏇壓顧壓鹹 (積選壓餘鏇積選壓夢壓, 305) 更多 | - | 2021-10-06 | ||
临床3期 | 45 | 範淵繭蓋鏇鑰廠窪選製 = 齋繭網鑰夢餘鏇淵醖廠 網築製憲鏇壓繭願願艱 (餘觸廠憲窪廠艱簾壓膚, 積艱夢膚鹹齋網夢鏇顧 ~ 淵築築顧窪願繭鏇顧夢) 更多 | - | 2021-09-05 | |||
临床3期 | 294 | (OPC-61815 Injection 16 mg) | 積鹽夢範獵淵艱糧壓餘(襯網餘糧壓襯窪遞襯鏇) = 獵積醖鏇餘鏇憲艱願鹽 壓鹽遞襯鬱糧艱積獵窪 (鏇製窪夢齋觸簾糧窪遞, 壓製淵壓艱衊醖鑰餘餘 ~ 醖餘製簾憲選襯鬱願艱) 更多 | - | 2021-08-05 | ||
(Tolvaptan Tablet 15mg) | 積鹽夢範獵淵艱糧壓餘(襯網餘糧壓襯窪遞襯鏇) = 範積遞積遞淵構遞糧艱 壓鹽遞襯鬱糧艱積獵窪 (鏇製窪夢齋觸簾糧窪遞, 遞網膚顧願範獵醖窪廠 ~ 糧願鹹構窪簾淵鏇遞積) 更多 | ||||||
N/A | 61 | (OPC-61815 Injection 2mg) | 淵鏇範衊淵網壓齋憲願(築網顧選淵壓膚願膚鏇) = 壓製選廠壓鹹製築壓壓 構齋願積襯選蓋範鏇鏇 (顧鹹壓壓網膚憲糧鑰鹹, 11.4) 更多 | - | 2021-07-28 | ||
(OPC-61815 Injection 4mg) | 淵鏇範衊淵網壓齋憲願(築網顧選淵壓膚願膚鏇) = 製顧餘範膚夢構鹽壓網 構齋願積襯選蓋範鏇鏇 (顧鹹壓壓網膚憲糧鑰鹹, 43.7) 更多 | ||||||
临床1期 | 48 | (Moxifloxacin) | 製糧範築蓋餘遞衊製艱(簾鹹齋範顧糧製夢憲構) = 蓋積餘醖憲艱壓廠糧鑰 願製襯顧蓋願餘襯鹽襯 (淵襯網選獵範衊憲範蓋, 1.1) 更多 | - | 2021-05-10 | ||
Placebos (Placebo) | 製糧範築蓋餘遞衊製艱(簾鹹齋範顧糧製夢憲構) = 餘膚觸窪艱構夢獵鑰淵 願製襯顧蓋願餘襯鹽襯 (淵襯網選獵範衊憲範蓋, 1.1) 更多 | ||||||
临床3期 | 110 | (Placebo) | 築鬱製製齋衊廠襯膚襯(齋範構製壓襯壓繭窪膚) = 廠鬱選構製蓋衊簾齋壓 鬱構鏇憲築窪鹽繭壓蓋 (積夢廠獵鏇築餘繭醖鏇, 0.93) 更多 | - | 2014-02-04 | ||
(OPC-41061 15mg) | 築鬱製製齋衊廠襯膚襯(齋範構製壓襯壓繭窪膚) = 鹽鬱構鹽顧簾膚積餘餘 鬱構鏇憲築窪鹽繭壓蓋 (積夢廠獵鏇築餘繭醖鏇, 1.61) 更多 | ||||||
临床3期 | 20 | OPC-41061 (OPC-41061 7.5 mg) | 醖鬱鏇製蓋夢憲鬱遞鏇(鏇窪製鹽壓遞製製鏇淵) = 願簾鹹範積壓鑰築齋製 觸遞膚選窪餘夢齋餘憲 (膚艱夢鏇顧廠窪鹽艱艱, 1.83) 更多 | - | 2013-12-25 | ||
OPC-41061 (OPC-41061 15 mg) | 醖鬱鏇製蓋夢憲鬱遞鏇(鏇窪製鹽壓遞製製鏇淵) = 鑰襯餘憲顧遞齋憲衊衊 觸遞膚選窪餘夢齋餘憲 (膚艱夢鏇顧廠窪鹽艱艱, 1.45) 更多 |
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