[Translation] A single-center, randomized, open-label, two-dose, two-period, two-sequence, single-dose, double-crossover bioequivalence study of rebamipide tablets (trade name: Mucosta®) produced by Zhejiang Otsuka Pharmaceutical Co., Ltd. and the original drug rebamipide tablets (trade name: Mucosta®) in healthy Chinese subjects in the fasting and fed state

（1）主要目的：以瑞巴派特的主要药代动力学参数（AUC和Cmax）为生物等效性的评价指标，在中国健康受试者空腹和餐后状态下评估受试制剂（浙江大冢制药有限公司生产的瑞巴派特片，规格：0.1g；商品名：膜固思达®）和参比制剂（OTSUKA PHARMACEUTICAL Co.,Ltd.持证的瑞巴派特片，规格：0.1g；商品名：Mucosta®）的生物等效性。（2）次要目的：观察空腹和餐后状态下受试制剂和参比制剂的安全性。

[Translation]

(1) Primary objective: To evaluate the bioequivalence of the test formulation (rebamipide tablets produced by Zhejiang Otsuka Pharmaceutical Co., Ltd., specification: 0.1g; trade name: Mucosta®) and the reference formulation (rebamipide tablets certified by OTSUKA PHARMACEUTICAL Co., Ltd., specification: 0.1g; trade name: Mucosta®) in Chinese healthy subjects under fasting and fed conditions, using the main pharmacokinetic parameters (AUC and Cmax) of rebamipide as bioequivalence evaluation indicators. (2) Secondary objective: To observe the safety of the test formulation and the reference formulation under fasting and fed conditions.

Start Date22 Jan 2024

Sponsor / Collaborator

Otsuka Beijing Research Institute

CTR20233084 / RecruitingPhase 1/2

一项在中国骨髓增生异常综合征受试者中口服ASTX727和注射用地西他滨的开放、交叉、药代动力学和疗效桥接研究

[Translation] An open-label, crossover, pharmacokinetic, and efficacy bridging study of oral ASTX727 and injectable decitabine in Chinese subjects with myelodysplastic syndrome

主要目的： 1.评估中国骨髓增生异常综合征（MDS）受试者接受ASTX727治疗的有效性[完全缓解率（CR率）]； 2.评估口服ASTX727与注射用地西他滨治疗5天后的主要药代动力学（PK）参数（地西他滨5天总暴露）；次要目的： 1.评估中国骨髓增生异常综合征受试者接受ASTX727治疗有效性的其他终点指标； 2.评估中国骨髓增生异常综合征受试者接受ASTX727治疗的安全性； 3.评估中国骨髓增生异常综合征受试者接受ASTX727与注射用地西他滨后的地西他滨、E7727和E7727-差向异构体PK参数。

[Translation]

Primary objectives: 1. To evaluate the efficacy of ASTX727 in Chinese subjects with myelodysplastic syndrome (MDS) [complete remission rate (CR rate)]; 2. To evaluate the main pharmacokinetic (PK) parameters (total 5-day exposure of decitabine) after 5 days of oral ASTX727 and decitabine injection; Secondary objectives: 1. To evaluate other endpoints of the efficacy of ASTX727 in Chinese subjects with myelodysplastic syndrome; 2. To evaluate the safety of ASTX727 in Chinese subjects with myelodysplastic syndrome; 3. To evaluate the PK parameters of decitabine, E7727 and E7727-diamer after ASTX727 and decitabine injection in Chinese subjects with myelodysplastic syndrome.

Start Date20 Oct 2023

Sponsor / Collaborator

BSP Pharmaceuticals SpA

[+2]

NCT06091267 / RecruitingPhase 1/2

An Open-label, Crossover, Pharmacokinetic and Efficacy Bridging Study of Oral ASTX727 Versus IV Decitabine in Chinese Subjects With Myelodysplastic Syndromes

This is an Open-Label, Crossover, Pharmacokinetic and Efficacy Bridging Study of Oral ASTX727 versus IV Decitabine in Chinese Subjects with Myelodysplastic Syndromes

Start Date16 Oct 2023

Sponsor / Collaborator

Otsuka Beijing Research Institute

100 Clinical Results associated with Otsuka Beijing Research Institute

0 Patents (Medical) associated with Otsuka Beijing Research Institute

Literatures (Medical) associated with Otsuka Beijing Research Institute

01 Jan 2022·PsychopharmacologyQ3 · MEDICINE

Efficacy and safety of aripiprazole once-monthly versus oral aripiprazole in Chinese patients with acute schizophrenia: a multicenter, randomized, double-blind, non-inferiority study

Q3 · MEDICINE

Article

Author: Zhao, Qian ; Zhang, Kerang ; Sun, Jushui ; Zhang, Hongyan ; Xian, Mingji ; Liu, Tiebang ; Wang, Gang ; Xu, Xiufeng ; Li, An-Ning ; Zhang, Wenshun ; Xie, Shiping ; Xu, Xiaojin ; Wu, Bin ; Li, Keqing ; Xiao, Le ; Zhang, Ruiling ; Uki, Motomichi ; Tan, Yunlong ; Wang, Lina ; Zhang, Honggeng ; Guan, Nianhong

OBJECTIVEThe present study aimed to evaluate the efficacy and safety of aripiprazole once-monthly (AOM) compared to oral aripiprazole in treating acute schizophrenia.METHODSThis randomized, double-blind, non-inferiority study recruited patients from 15 trial sites across China from May 2017 to April 2019. Patients with an acute psychotic episode received AOM at 400 mg or oral aripiprazole at 10-20 mg for 12 weeks. The primary and secondary efficacy endpoints were the difference in scores from baseline to week 10, as assessed on the Positive and Negative Syndrome Scale (PANSS) and Clinical Global Impressions-Severity (CGI-S) scores, respectively.RESULTSA total of 436 patients were randomized. Among them, 159/218 (72.9%) and 165/218 (75.7%) in the AOM and oral aripiprazole groups completed 10 weeks of treatment, respectively. The least-squares (LS) mean changes from baseline to endpoint (week 10) in PANSS were - 33.6 for the AOM group and - 34.8 in the oral aripiprazole group, respectively, with a difference of - 1.2 (95% CI: - 4.1, 1.7). The non-inferiority margin of AOM to oral aripiprazole was - 4.1, which was above the lower limit of the pre-defined margin. The altered CGI-S score was - 2.2 and - 2.3 in the AOM and oral aripiprazole groups, respectively. The incidence of treatment-emergent adverse events (TEAEs) was similar in both groups. The rate of discontinuation due to TEAEs was 2.3% and 3.2% in the AOM and oral aripiprazole groups, respectively.CONCLUSIONSThis study confirmed the efficacy and safety of AOM for the treatment of Chinese patients with acute schizophrenia. The non-inferiority of AOM to oral aripiprazole was established, with comparable efficacy and tolerability. These findings suggested that AOM could be used as a treatment option for patients experiencing an acute episode of schizophrenia.TRIAL REGISTRATIONClinicalTrials.gov identifier: NCT03172871.

01 May 2015·Annals of OncologyQ1 · MEDICINE

Phase I and biomarker study of OPB-51602, a novel signal transducer and activator of transcription (STAT) 3 inhibitor, in patients with refractory solid malignancies

Q1 · MEDICINE

Article

Author: B.R. Asuncion ; M. Motoyama ; Y.J. Lee ; M.T. Cordero ; J.S. Lim ; P.C. Marban ; A.L. Wong ; S. Pervaiz ; W.L. Thuya ; R.A. Soo ; B. Pang ; L.Z. Wang ; W.W. Xu ; R. Soong ; T.M. Chin ; S.C. Lee ; T. Yamauchi ; D.S. Tan ; J.L. Hirpara ; A. Sinha ; M. Yuasa ; M.Q. Yee ; L.R. Kong ; T. Tsunoda ; B.C. Goh

BACKGROUNDThe aim of this study was to determine the maximum-tolerated dose (MTD), safety, pharmacokinetics, and pharmacodynamics of OPB-51602, an oral, direct signal transduction activator of transcription 3 (STAT3) inhibitor, in patients with refractory solid tumors.PATIENTS AND METHODSThree cohorts were studied: cohort A, a sequential dose escalation of OPB-51602 administered intermittently (days 1-14 every 21 days); cohort B, an expansion cohort evaluating the dose lower than the MTD; cohort C, evaluating continuous daily dosing.RESULTSFifty-one patients were studied at 2, 4, and 5 mg per day dosing. The MTD was 5 mg; first-cycle dose-limiting toxicities (DLTs) were grade 3 hyponatremia in one patient, and grade 3 dehydration in another. Intermittent dosing of both 2 and 4 mg doses were tolerable, and the recommended phase II dose was 4 mg. Cohort B investigated 4 mg intermittently, whereas cohort C investigated 4 mg continuously. Common toxicities included fatigue, nausea/vomiting, diarrhea, anorexia, and early-onset peripheral neuropathy. Drug-induced pneumonitis occurred in two patients in cohort C. Continuous dosing was associated with a higher incidence of peripheral neuropathy and a lower mean relative dose intensity, compared with intermittent dosing. Steady-state pharmacokinetics was characterized by high oral clearance, mean elimination half-life ranging from 44 to 61 h, and a large terminal-phase volume of distribution. An active metabolite, OPB-51822, accumulated to a greater extent than OPB-51602. Flow cytometry of peripheral blood mononuclear cells demonstrated pSTAT3 (Tyr(705)) inhibition following exposure. Two patients achieved partial responses at 5 mg intermittently and 4 mg continuously; both had epidermal growth factor receptor (EGFR) mutation-positive non-small-cell lung cancer (NSCLC) with prior EGFR tyrosine kinase inhibitor exposure.CONCLUSIONOPB-51602 demonstrates promising antitumor activity, particularly in NSCLC. Its long half-life and poorer tolerability of continuous dosing, compared with intermittent dosing, suggest that less frequent dosing should be explored.CLINICALTRIALSGOV IDENTIFIERNCT01184807.

20 May 2012·Journal of Clinical Oncology

Phase I study of OPB51602, a small molecule inhibitor of STAT3 phosphorylation, in patients with refractory solid malignancies.

Author: Wong, Andrea LA ; Soo, Ross A. ; Goh, Boon C. ; Zhu, Qian ; Chuah, Benjamin ; Mikami, Tomomi ; Yong, Wei-Peng ; Lwin, Thuya Win ; Kong, Li-Ren ; Yuasa, Miyuki ; Marban, Patrick ; Zee, Ying Kiat ; Lee, Soo-Chin

3002 Background: STAT3 is constitutively activated by growth signaling pathways in many malignancies; in many cell lines inhibition of STAT3 leads to cell death. OPB51602 is a small molecule inhibitor of STAT3 phosphorylation (Tyr705) and activation. Methods: A phase I study of OPB51602 administered for 2 weeks every 3 weeks was initiated to determine the maximum tolerable dose (MTD), evaluate pharmacokinetics (PK), and assess pharmacodynamics effects on STAT3 in peripheral blood mononuclear cells (PBMCs). The starting dose was 2mg/day, and dose escalations to 5mg/d, 10mg/d, 20mg/d, were planned. Single dose PK was done on the first day of administration for 4 days. Dose escalation was based on the “3+3” design, MTD was defined as the dose with at least 2/6 dose limiting toxicities (DLTs) in the first cycle and toxicities were graded by NCICTCv4.0. Results: 32 patients (pt) were treated at doses of 2mg/d (n=7), 4mg/d (n=18), 5mg/d (n=7). The main toxicities observed included nausea/vomiting, diarrhea, peripheral neuropathy and fatigue. 5 mg/d was the MTD, where cycle 1 DLTs of grade 3 diarrhea/dehydration and hyponatremia occurred in 1 patient respectively. One pt developed grade 3 peripheral neuropathy at 4mg/d cohort. PK showed maximal drug levels 2-3 hours after administration, bi-exponential decay, with mean oral clearance of 316.5 +/- 638.9 L/h and long terminal mean half-life of 61.8 +/- 15.9 h on day 17. STAT3 phosphorylation in PBMCs assessed in 6 pts receiving 4mg/d was reduced from 67.4 +/- 17.4% at baseline to 53.0 +/- 18.1% (p=0.001) after administration on day 1. Interestingly, reduction in tumor metabolism by PET CT on day 15 was observed in 4/8 pts receiving 4mg/d. A pt with heavily pretreated adenocarcinoma of lung at 5mg/d dose had partial response; another pt with metastatic endometrial cancer at 4mg/d dose experienced stable disease for 6 cycles. Conclusions: OPB51602 has an MTD of 5mg/d on this schedule, demonstrates inhibition of STAT3 phosphorylation, and evidence of clinical activity. Further proof of concept studies of OPB51602 are warranted.

100 Deals associated with Otsuka Beijing Research Institute

100 Translational Medicine associated with Otsuka Beijing Research Institute

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