Samtasu (tolvaptan sodium phosphate) / Otsuka - LARVOL DELTA

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. (PubMed, J Chromatogr B Analyt Technol Biomed Life Sci) - "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."

Journal • Cardiovascular • Congestive Heart Failure • Heart Failure

Samtasu Post-marketing General Drug Use-results Survey in Patients With Volume Overload in Heart Failure. (clinicaltrials.gov) - P=N/A | N=1600 | Recruiting | Sponsor: Otsuka Pharmaceutical Co., Ltd. | Not yet recruiting ➔ Recruiting

Enrollment open • Cardiovascular • Congestive Heart Failure • Heart Failure

OPC-61815 in Healthy Chinese Male Subjects (clinicaltrials.gov) - P1 | N=18 | Completed | Sponsor: Otsuka Beijing Research Institute | Recruiting ➔ Completed

Trial completion

Samtasu Post-marketing General Drug Use-results Survey in Patients With Volume Overload in Heart Failure. (clinicaltrials.gov) - P=N/A | N=1600 | Not yet recruiting | Sponsor: Otsuka Pharmaceutical Co., Ltd.

New trial • Cardiovascular • Congestive Heart Failure • Heart Failure

OPC-61815 in Healthy Chinese Male Subjects (clinicaltrials.gov) - P1 | N=18 | Recruiting | Sponsor: Otsuka Beijing Research Institute | Trial completion date: Sep 2022 ➔ Dec 2022

Trial completion date

In vitro and in vivo pharmacological profile of OPC-61815, a water-soluble phosphate ester pro-drug of tolvaptan. (PubMed, J Pharmacol Sci) - "OPC-61815 exerted dose-dependent aquaretic action in rats and dogs and a corresponding anti-edematous action in rat edema models. These results suggest that OPC-61815, a water-soluble phosphate ester pro-drug of tolvaptan, is an effective aquaretic by converting to tolvaptan after intravenous administration."

Journal • Preclinical

Efficacy and safety of intravenous OPC-61815 compared with oral tolvaptan in patients with congestive heart failure. (PubMed, ESC Heart Fail) - "OPC-61815 (16-mg injection) was confirmed as non-inferior to oral tolvaptan (15-mg tablet) in patients with congestive heart failure and inadequate response to diuretics; no new safety concerns were observed."

Journal • Cardiovascular • Congestive Heart Failure • Heart Failure • Xerostomia

OPC-61815 in Healthy Chinese Male Subjects (clinicaltrials.gov) - P1 | N=18 | Recruiting | Sponsor: Otsuka Beijing Research Institute | Not yet recruiting ➔ Recruiting | Trial completion date: Dec 2022 ➔ Sep 2022 | Trial primary completion date: Jun 2022 ➔ Sep 2022

Enrollment open • Trial completion date • Trial primary completion date

OPC-61815 in Healthy Chinese Male Subjects (clinicaltrials.gov) - P1 | N=18 | Not yet recruiting | Sponsor: Otsuka Beijing Research Institute

New P1 trial

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. (PubMed, Circ J) - "The tolerability of once daily (up to 5 days) intravenous OPC-61815 (8 mg or 16 mg) was confirmed in patients with CHF who had difficulty with, or were incapable of, oral intake."

Journal • P3 data • Cardiovascular • Congestive Heart Failure • Heart Failure • Pulmonary Disease

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. (PubMed, Circ J) - "In this first study of OPC-61815 in patients with CHF, exposure following a single IV administration of OPC-61815 16 mg was comparable with a single oral administration of tolvaptan 15 mg, with no safety concerns."

Clinical • Journal • P2 data • PK/PD data • Cardiovascular • Congestive Heart Failure • Heart Failure

A Phase I, Open-Label Trial to Assess the Absorption, Metabolism, and Excretion of (14C)-OPC-61815 in Healthy Male Japanese Subjects (clinicaltrials.gov) - P1; N=8; Completed; Sponsor: Otsuka Pharmaceutical Co., Ltd.; Recruiting ➔ Completed

Clinical • Trial completion

Efficacy and Safety Trial of OPC-61815 Injection Compared With Tolvaptan 15-mg Tablet in Patients With Congestive Heart Failure (clinicaltrials.gov) - P3; N=294; Completed; Sponsor: Otsuka Pharmaceutical Co., Ltd.; Active, not recruiting ➔ Completed; Trial completion date: Nov 2020 ➔ Jul 2020; Trial primary completion date: Nov 2020 ➔ Jul 2020

Clinical • Head-to-Head • Trial completion • Trial completion date • Trial primary completion date • Cardiovascular • Congestive Heart Failure • Heart Failure

Safety Trial of OPC-61815 Injection in Patients With Congestive Heart Failure Who Have Difficulty With or Are Incapable of Oral Intake (clinicaltrials.gov) - P3; N=45; Completed; Sponsor: Otsuka Pharmaceutical Co., Ltd.; Recruiting ➔ Completed

Clinical • Trial completion • Cardiovascular • Congestive Heart Failure • Heart Failure

Clinical Pharmacology Trial to Investigate the Dose of OPC-61815 Injection Equivalent to Tolvaptan 15-mg Tablet in Patients With Congestive Heart Failure (clinicaltrials.gov) - P=N/A; N=61; Completed; Sponsor: Otsuka Pharmaceutical Co., Ltd.; Active, not recruiting ➔ Completed

Clinical • Trial completion • Cardiovascular • Congestive Heart Failure • Heart Failure

Efficacy and Safety Trial of OPC-61815 Injection Compared With Tolvaptan 15-mg Tablet in Patients With Congestive Heart Failure (clinicaltrials.gov) - P3; N=288; Active, not recruiting; Sponsor: Otsuka Pharmaceutical Co., Ltd.; Recruiting ➔ Active, not recruiting; Trial completion date: Jul 2020 ➔ Nov 2020; Trial primary completion date: Jul 2020 ➔ Nov 2020

Clinical • Enrollment closed • Head-to-Head • Trial completion date • Trial primary completion date • Cardiovascular • Congestive Heart Failure • Heart Failure

A Phase I, Open-Label Trial to Assess the Absorption, Metabolism, and Excretion of (14C)-OPC-61815 in Healthy Male Japanese Subjects (clinicaltrials.gov) - P1; N=6; Recruiting; Sponsor: Otsuka Pharmaceutical Co., Ltd.

Clinical • New P1 trial