Retosiban(Retosiban) - 药物靶点：OXTR_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Retosiban (USAN)、GSK-221149、GSK-221149A

靶点

OXTR

作用方式

拮抗剂

作用机制

OXTR拮抗剂(催产素受体拮抗剂)

治疗领域

泌尿生殖系统疾病

在研适应症-

非在研适应症

早产早泄

原研机构

GSK Plc

在研机构-

非在研机构

GSK Plc

权益机构-

最高研发阶段终止临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C27H34N4O5

InChIKeyPLVGDGRBPMVYPB-FDUHJNRSSA-N

CAS号820957-38-8

关联

11

项与 Retosiban 相关的临床试验

NCT02377466

/ Terminated临床3期

Randomized, Double-blind, Multicenter, Phase III Study Comparing the Efficacy and Safety of Retosiban Versus Placebo for Women in Spontaneous Preterm Labor

The study's primary objective is to demonstrate the superiority of retosiban to prolong pregnancy and improve neonatal outcomes compared with placebo. It is a Phase III, randomized, double-blind, parallel-group, multicenter study and will be conducted in approximately 900 females, aged 12 to 45 years, with an uncomplicated, singleton pregnancy and intact membranes in preterm labor between 24^0/7 and 33^6/7 weeks of gestation. Eligible maternal subjects will be randomly assigned in a 1:1 ratio to receive either retosiban IV infusion or placebo IV infusion over 48 hours. If not previously administered, antenatal corticosteroid treatment should be administered as either (1) two 12-mg doses of betamethasone given intramuscularly 24 hours apart or (2) four 6-mg doses of betamethasone administered intramuscularly every 12 hours. A single rescue course of antenatal corticosteroids is permitted if the antecedent treatment was at least 7 days prior to study enrolment. Investigators have discretion to use a standardized regimen of magnesium sulphate, as well as intrapartum antibiotic prophylaxis for perinatal group B streptococcal infection. Prior to randomization, each subject will be stratified by progesterone treatment and gestational age. The progesterone strata will consist of subjects on established progesterone therapy or subjects not on established progesterone therapy at Screening. The study will comprise 6 phases: Screening, Inpatient Randomized Treatment, Post Infusion Assessment, Delivery, Maternal Post-Delivery Assessment, and Neonatal Medical Review. The duration of any subject's (maternal or neonatal) participation in the study will be variable and dependent on gestational ages (GA) at study entry and the date of delivery.

开始日期2016-02-29

申办/合作机构

GSK Plc

[+1]

NCT02292784

/ Completed临床3期

Follow-Up Study to Assess Long-Term Safety and Outcomes in Infants and Children Born to Mothers Participating in Retosiban Treatment Studies

The primary objective of this study is to assess the safety and outcomes of infants and children who were exposed to retosiban or comparator in utero in the Phase III spontaneous preterm labor (SPTL) treatment studies, to provide assurance that treatment is not associated with significant adverse outcomes in early childhood. The enrolled infants and children will be followed at pre-specified intervals until they reach 24 months chronological age. This study does not require medical interventions or study visits to an investigational site, instead, parents or legal guardians will be prompted at certain time points to complete developmental questionnaires and other data on their children's health status via an electronic device. Data collected during the infant and child follow up study will be managed by a centralized research coordinating center (RCC). Regionally based pediatricians will serve as study principal investigators (referred to as RCC-PIs) for this study. All communications the RCC-PI has with the parent/legal guardian or the child's health care provider (HCP) will occur remotely; there will be no clinic visits.

开始日期2015-06-01

申办/合作机构

GSK Plc

[+1]

NCT02292771

/ Terminated临床3期

Randomized, Double-blind, Multicenter, Phase III Study Comparing the Efficacy and Safety of Retosiban Versus Atosiban Therapy for Women in Spontaneous Preterm Labor

The primary objective of this study is to demonstrate the superiority of retosiban to prolong pregnancy in females with spontaneous preterm labor compared with atosiban. This objective is based on the hypothesis that prolonging the time to delivery in the absence of harm may benefit the newborn, particularly in women who experience spontaneous preterm labor at early gestational ages (GA). This study is designed to test this hypothesis through a direct comparison with atosiban, a mixed oxytocin vasopressin antagonist indicated for short-term use to delay imminent preterm birth in women between 24^0/7 and 33^6/7 weeks' gestation in preterm labor. This is a randomized, double-blind, double-dummy study, which consists of 6 phases: Screening, Inpatient Randomized Treatment, Post Infusion Assessment, Delivery, Maternal Post Delivery Assessment, and Neonatal Medical Review. Approximately 330 females will be randomly assigned to retosiban or atosiban treatment in a 1:1 ratio. The duration of any one subject's (maternal or neonatal) participation in the study will be variable and dependent on GA at study entry and the date of delivery.

开始日期2015-03-16

申办/合作机构

GSK Plc

[+1]

100 项与 Retosiban 相关的临床结果

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100 项与 Retosiban 相关的转化医学

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100 项与 Retosiban 相关的专利（医药）

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30

项与 Retosiban 相关的文献（医药）

2023-07-01·American journal of perinatology4区 · 医学

Safety and Outcomes in Infants Born to Mothers Participating in Retosiban Treatment Trials: ARIOS Follow-up Study

4区 · 医学

Article

作者: Pimenta, Jeanne M. ; Beach, Kathleen J. ; Saade, George R. ; Correa, Erika Ochoa ; Powell, Marcy ; Scott, Rhona ; Thornton, Steve ; Haque, Nazneen ; Snidow, Jerry ; Miller, Diane

Objective Retosiban, an oxytocin receptor antagonist, was developed for treating spontaneous preterm labor (sPTL) in women with intact membranes. This ARIOS follow-up study aimed to characterize clinical safety, morbidity, and mortality of infants exposed to retosiban or comparator over 2 years. Study Design ARIOS prospectively assessed outcomes in infants whose mothers received at least one dose of retosiban or comparator (placebo/atosiban) in two Phase 3 sPTL trials. Both trials were terminated prematurely owing to poor enrolment. Infants could be enrolled into ARIOS from 28 days after estimated due date until hospital discharge or up to 9 months (corrected age). An internally developed questionnaire detailing medical conditions, mortality and resource use (Child Health Inventory; CHI), Ages and Stages Questionnaire-3 (ASQ-3), Modified Checklist for Autism in Toddlers–Revised with Follow-Up, and Child Behavior Checklist for Ages 1.5 to 5 were completed remotely by parents or legal guardians at prespecified intervals. Serious adverse events (SAEs) were primarily captured via CHI. No comparative statistical analysis was conducted between treatment arms. Results A total of 49 (86%) infants who had received retosiban and 49 (78%) infants who had received a comparator were enrolled in ARIOS. No deaths occurred during the study. Nine infants experienced SAEs: 6/49 (12.2%) infants in the comparators group and 3/49 (6.1%) in the retosiban group. Of the nine SAEs, seven were due to infections, three, and four in the retosiban and comparators groups, respectively. Based on ASQ-3 score, the incidence of neurodevelopmental delay at 18 and 24 months were 0/18 (0%) and 2/25 (8%) with retosiban and 7/22 (31.8%) and 3/21 (14.3%) with comparator, respectively. Conclusion The current study showed no unexpected adverse outcome or impairment with retosiban based on safety monitoring and neurodevelopment assessments. No further follow-up is intended owing to the discontinuation of clinical development of retosiban. Key Points

2021-09-02·Current medical research and opinion4区 · 医学

Novel oxytocin receptor antagonists for tocolysis: a systematic review and meta-analysis of the available data on the efficacy, safety, and tolerability of retosiban

4区 · 医学

Review

作者: Ulibarri, Hollie ; Marchand, Greg ; Ware, Kelly ; Cieminski, Kaitlynne ; King, Alexa ; Ruuska, Alexandra D. ; Blumrick, Richard ; Masoud, Ahmed Taher ; Sainz, Katelyn ; Calteux, Nicolas ; Ruther, Stacy ; Brazil, Giovanna

OBJECTIVE:

To assess the efficacy, safety, and tolerability of retosiban-a novel tocolytic unavailable in the US-in the management of preterm labor.

METHODS:

We searched ClinicalTrials.Gov, MEDLINE, PubMed, SCOPUS, Web of Science, and the Cochrane Library for relevant clinical trials using the terms "retosiban" and "preterm labor" through 09/2020. We included all published randomized clinical trials (three) that compared retosiban to placebo for preterm labor, excluding conferences, books, reviews, posters, case reports, and animal studies. We analyzed homogeneous data under the fixed-effects model and heterogeneous data under the random-effects model.

RESULTS:

We included all randomized clinical trials addressing this topic, which ultimately resulted in three trials with a total of 116 patients. There were no significant differences between retosiban and placebo in births at term (RR = 0.41, p = .02), births ≤7 days from the first study treatment (RR = 0.59, p = .23), or administration of rescue tocolytic (RR = 0.36, p = .07); the maternal adverse events of headache, anemia, constipation, or urinary tract infection (p > .05); or neonatal outcomes of Apgar score at 1 min (p = .88) or 5 min (p = .69), weight (p = .23), head circumference (p = .55), malnutrition (p = .27), hyperbilirubinemia (RR = 0.56, p = .21), jaundice (RR = 1.21, p = .84), respiratory distress (RR = 0.53, p = .49), or tachypnea (RR = 0.40, p = .42).

CONCLUSION:

With the limited high quality evidence available, retosiban demonstrates no clear benefit over placebo in the management of preterm labor. Nevertheless, its favorable safety profile, oral bioavailability, and novel mechanism of action and the limited number of studies available for review warrant further analysis.

2021-08-01·American journal of perinatology4区 · 医学

Erratum: Randomized Trials of Retosiban versus Placebo or Atosiban in Spontaneous Preterm Labor

4区 · 医学

Article

作者: Powell, Marcy ; Saade, George ; Shennan, Andrew ; Beach, Kathleen J. ; Parilla, Barbara V. ; Komatsu, Yosuke ; Thornton, Steven ; McKain, Laura ; Liu, Feng ; Hadar, Eran ; Snidow, Jerry ; Montague, Timothy H.

100 项与 Retosiban 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D08986	Retosiban	-	DB11818

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
早产	临床3期	比利时	GSK Plc	2015-03-16
早产	临床3期	德国	GSK Plc	2015-03-16
早产	临床3期	以色列	GSK Plc	2015-03-16
早产	临床3期	意大利	GSK Plc	2015-03-16
早产	临床3期	墨西哥	GSK Plc	2015-03-16
早产	临床3期	韩国	GSK Plc	2015-03-16
早产	临床3期	西班牙	GSK Plc	2015-03-16
早产	临床3期	瑞典	GSK Plc	2015-03-16
早产	临床3期	英国	GSK Plc	2015-03-16
早泄	临床1期	美国	GSK Plc	2007-03-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT02292784 (ARIOS, Pubmed \| Am J Perinatol)	临床3期	-	-	Comparator (Placebo/Atosiban)	獵艱積遞繭簾衊獵齋構(簾簾製廠憲淵鑰襯顧選) = 鏇鬱顧鑰襯鹹鏇觸構簾鏇憲膚憲膚襯顧餘簾顧 (膚衊繭選膚齋選鑰觸獵 )	-	2021-08-05
NCT02292784 (ARIOS, CTgov)	临床3期	早产	98	Placebo (Placebo (200719 Study))	艱簾積廠鬱積蓋壓遞淵 = 構選觸範網憲範構窪襯鏇淵艱夢膚願製範簾願 (範衊壓窪顧淵築膚構糧, 鏇選築觸遞繭壓構鹽窪 ~ 繭鹹衊鹽鏇膚築淵艱選) 更多	-	2020-07-09
				Atosiban (Atosiban (200721 Study))	艱簾積廠鬱積蓋壓遞淵 = 網衊獵簾衊鬱繭鹽膚築鏇淵艱夢膚願製範簾願 (範衊壓窪顧淵築膚構糧, 鹹鏇鏇衊蓋蓋餘願鏇鏇 ~ 鬱壓膚觸齋鹹製顧鹹鹽) 更多
NCT02292771 (CTgov)	临床3期	早产	97	Retosiban (Retosiban)	艱鏇鏇憲蓋廠鹽鬱鹹構(積醖夢衊窪艱製膚窪遞) = 選蓋鑰積鏇鹽簾製積鬱壓糧艱鏇餘襯選鑰齋襯 (膚艱窪構淵觸醖範構齋, 2.990) 更多	-	2018-09-10
				Atosiban (Atosiban)	艱鏇鏇憲蓋廠鹽鬱鹹構(積醖夢衊窪艱製膚窪遞) = 壓窪糧選築夢願窪觸廠壓糧艱鏇餘襯選鑰齋襯 (膚艱窪構淵觸醖範構齋, 2.531) 更多
NCT02377466 (NEWBORN-1, CTgov)	临床3期	早产	25	Placebo IV infusion (Placebo)	繭築鏇簾繭繭獵構淵選(簾餘顧簾鏇淵鹹衊膚鹹) = 遞顧艱糧鑰遞蓋獵顧獵衊積壓襯製獵鬱鬱鹹觸 (構築範獵製鬱齋簾憲獵, 14.987) 更多	-	2018-07-19
				Retosiban IV infusion (Retosiban)	繭築鏇簾繭繭獵構淵選(簾餘顧簾鏇淵鹹衊膚鹹) = 憲積鬱廠糧窪範窪膚鑰衊積壓襯製獵鬱鬱鹹觸 (構築範獵製鬱齋簾憲獵, 22.993) 更多
NCT00404768 (Pubmed \| Br J Clin Pharmacol) 人工标引	临床2期	早产	64	retosiban	積淵襯淵糧繭膚艱鏇鏇(積鏇選糧願襯夢衊廠衊) = 範鏇淵夢壓齋鑰選齋鏇衊憲簾繭積鹹積遞窪簾 (糧醖鑰壓顧鏇廠積憲觸 ) 更多	积极	2015-10-01
				Placebo	積淵襯淵糧繭膚艱鏇鏇(積鏇選糧願襯夢衊廠衊) = 衊襯壓鬱鏇衊膚蓋夢鏇衊憲簾繭積鹹積遞窪簾 (糧醖鑰壓顧鏇廠積憲觸 ) 更多
NCT01702376 (Pubmed \| Clin Ther)	临床1期	-	52	Retosiban 100 mg	衊蓋憲艱鑰範鏇鹽餘鏇(鹽選鹹艱鏇壓範鑰壓築) = 鑰鹽夢鬱觸膚鑰範蓋獵膚繭憲齋衊製顧醖壓鑰 (壓觸鬱顧繭鬱製淵範鏇 )	-	2015-07-01
				Retosiban 800 mg	衊蓋憲艱鑰範鏇鹽餘鏇(鹽選鹹艱鏇壓範鑰壓築) = 製廠艱齋獵衊壓鑰糧糧膚繭憲齋衊製顧醖壓鑰 (壓觸鬱顧繭鬱製淵範鏇 )