A Randomized, Double-blinded, Placebo-controlled, Multicenter Study to Evaluate the Antipsychotic Efficacy and Safety of LB-102 in the Treatment of Adult Patients With Acute Schizophrenia

This is a Phase 2, randomized, double-blind, placebo-controlled, multi-center inpatient study to evaluate the efficacy and safety of LB-102 in adult patients diagnosed with acutely exacerbated schizophrenia. To determine whether LB-102 administered to patients with acutely exacerbated schizophrenia demonstrates antipsychotic efficacy, as determined by a change from Baseline on the Positive and Negative Syndrome Scale (PANSS) total score, compared to placebo at 28 days. The secondary objectives of the study are to evaluate improvement in CGI-S, safety and tolerability, and pharmacokinetics.

开始日期2023-12-04

申办/合作机构

LB Pharmaceuticals, Inc.初创企业

NCT04588129 / Completed临床1期

An Open Label Positron Emission Tomography (PET) Study to Evaluate Dopamine Receptor Occupancy of LB-102 Administered Orally to Healthy Subjects

This is an open label study in 4 cohort of 4 healthy volunteers each designed to evaluate the dopamine receptor occupancy of LB-102 at various doses and timepoints.

开始日期2021-01-05

申办/合作机构

LB Pharmaceuticals, Inc.初创企业

[+1]

NCT04187560 / Completed临床1期

A Randomized, Double-blinded, Placebo-controlled, Single and Multiple Ascending Dose Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of LB-102 Administered Orally to Healthy Subjects

A Single Ascending Dose (SAD; Part A) and Multiple Ascending Dose (MAD; Part B) Phase 1 Study of LB-102 N-Methyl amisulpride) in healthy volunteers. The primary objective is to evaluate the safety and the tolerability of a single oral dose (SAD) and multiple oral doses (MAD) of LB-102 as compared to placebo. The secondary objectives are to evaluate the pharmacokinetics (PK) and pharmacodynamics (PD) of LB-102.

开始日期2020-01-22

申办/合作机构

LB Pharmaceuticals, Inc.初创企业

100 项与 N-methyl amisulpride 相关的临床结果

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100 项与 N-methyl amisulpride 相关的转化医学

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100 项与 N-methyl amisulpride 相关的专利（医药）

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项与 N-methyl amisulpride 相关的文献（医药）

2023-11-02·Expert review of clinical pharmacology

A narrative review of non-racemic amisulpride (SEP-4199) for treatment of depressive symptoms in bipolar disorder and LB-102 for treatment of schizophrenia

Review

作者: Ho, Roger ; Rhee, Taeho Greg ; d’Andrea, Giacomo ; Teopiz, Kayla M ; Kwan, Angela TH ; Wu, Jie ; Ceban, Felicia ; McIntyre, Roger S ; Martinotti, Giovanni

INTRODUCTION:

The challenges posed by treatment-resistant schizophrenia and depressive symptoms have led to ongoing difficulties despite the availability of antipsychotics and antidepressants. This review addresses the potential of amisulpride analogs, particularly SEP-4199, in addressing these challenges through enhanced efficacy and reduced side effects.

AREAS COVERED:

This review focuses on the pharmacological profile of amisulpride analogs, exemplified by LB-102 and its derivative SEP-4199. PubMed gathered articles (up to 10 March 2023) on 'amisulpride,' 'schizophrenia,' 'bipolar disorder,' and 'major depressive disorder;' ClinicalTrials.gov tracked SEP-4199 and LB-102 trials. LB-102, a newly identified N-methylated analog of amisulpride, exhibits enhanced lipophilicity at lower doses, as demonstrated in a phase 1 study, indicating significant promise for therapeutic applications. The discovery of SEP-4199, a non-racemic analog composed of R- and S-enantiomers in an 85:15 ratio, is discussed, emphasizing its potential to enhance antidepressant effects while minimizing extrapyramidal side effects via selective D2 receptor binding. Recent phase 2 trials have demonstrated SEP-4199's efficacy in treating depressive symptoms in bipolar disorder I, capitalizing on D2-mediated anti-anhedonic and D3-mediated reward effects.

EXPERT OPINION:

The development of SEP-4199 presents a potential breakthrough for managing depressive symptoms in bipolar disorder I. Further exploration of D2 and D3 receptor-mediated effects could lead to improved treatment strategies.

2022-12-01·Chemosphere

Persistence of N-oxides transformation products of tertiary amine drugs at lab and field studies.

Article

作者: Perez, S ; Tadić, D ; Chiron, S ; Gomez, O ; Manasfi, R

This work aimed at studying the formation and persistence of N-oxides transformation products (TPs) of tertiary amine drugs by combining laboratory and field studies relevant for surface water. A monitoring study using passive samplers was first achieved for assessing attenuation of selected pharmaceuticals and their related N-oxides and N-, O-dealkylated TPs (i.e., venlafaxine, tramadol, amisulpride and sulpiride) along a 1.7 km river stretch between two sampling sites. This study revealed the stability of tramadol-N-oxide, amisulpride-N-oxide and the fast dissipation of O-desmethylvenlafaxine-N-oxide, as well as the significance of N-oxidized TPs in comparison to N-dealkylated TPs and parent compounds in river. Lab-scale experiments were then implemented for a better understanding of their mechanisms of formation and degradation under aerobic water/sediment testing and under simulated solar photochemistry. N-oxidation reactions were always a minor transformation pathway under both degradation conditions with respect to N-and O-dealkylation reactions. The amount of generated N-oxides were similar for venlafaxine, tramadol and sulpiride and peaked in the 8.4-12.8% and <4% of their initial concentration (100 μg/L), during photodegradation and biodegradation experiments, respectively. Other transformation pathways such as hydroxylation and α-C-hydroxylation followed by oxidation to amide or dehydration were also identified. Investigated N-oxides TPs (except O-desmethylvenlafaxine-N-oxide) were found stable under solar photolysis and aerobic biodegradation with a very slight reverse reaction to parent compound observed for tramadol-N-oxide and amisulpride-N-oxide. Lab-scale degradation experiments were not able to anticipate the high occurrence levels of N-oxide compounds in the environment. This was most likely due to faster degradation kinetics and/or higher sorption to sediment of parent compounds and dealkylated TPs over N-oxide TPs, resulting in higher relative accumulation of the latter.

2022-09-01·Psychopharmacology

A randomized, double-blind, placebo controlled, phase 1 study of the safety, tolerability, pharmacokinetics, and pharmacodynamics of LB-102, a selective dopamine D2/3/5-HT7 inhibitor

Article

作者: Grattan, Vincent T ; Prensky, Zachary ; Biernat, Lukasz ; Vaino, Andrew R ; Hixon, Mark S

LB-102 is an N-methylated analogue of amisulpride under development to treat schizophrenia. LB-102 was evaluated in a Phase 1, double-blind, placebo-controlled, clinical study to evaluate safety and pharmacokinetics. This was a first-in-human study examining single and multiple doses of LB-102 administered orally in 64 healthy volunteers. Dosing in the single ascending dose (SAD) portion of the study was initially planned to be 50, 100, 200, and 400 mg, with doses in the multiple ascending dose (MAD) portion to be determined based on observations in the SAD portion. As a result of two cases of EPS (acute dystonia) at 200 mg in the MAD portion of the study, dosing of that arm was discontinued and doses for the remaining cohort were decreased to 150 mg/day. Dose escalation was guided by safety and plasma concentrations of LB-102 compared to a translational model. LB-102 was generally safe and well-tolerated, and clinical lab values were unremarkable at all doses, save for prolactin which was transiently elevated in the majority of subjects treated with LB-102; there were no clinical observations associated with the increases in prolactin elevation. There was evidence of transient QT interval prolongation at the 200 mg dose, none of which resulted in clinical observation or triggered stopping criteria. There were four instances of EPS (acute dystonia), typically associated with dopamine receptor occupancy in excess of 80%, one at 100 mg QD, one at 75 mg BID, and two at 100 mg BID. A phase 2 clinical study of LB-102 in schizophrenia patients with PANSS as primary endpoint is being planned.

项与 N-methyl amisulpride 相关的新闻（医药）

2023-09-25

·药明康德

速递 | 助力经典精神分裂症药物创新升级，新锐完成新一轮融资

▎药明康德内容团队编辑日前，根据LB Pharmaceuticals近日提交给美国证券交易委员会（SEC）的文件，该公司已完成了新一轮的融资，预计本轮融资总额将达到4000万美元。加上此前已完成的融资，LB Pharmaceuticals的总融资额已高达7500万美元。这些资金将用于推进一种有着几十年历史治疗精神分裂症药物的优化版本的开发测试。LB Pharmaceuticals是一家专注于中枢神经系统的生命科学公司，致力于将在其他国家或地区已成功应用、但在美国尚未上市的改良型中枢神经系统疾病治疗药物进行商业化。该公司的先导化合物LB-102是一种新型多巴胺/7型五羟色胺受体拮抗剂，它以氨磺必利（amisulpride）为基础。根据今年6月发布的一份投资者报告，LB Pharmaceuticals计划对氨磺必利的一种化学差异版本进行2期试验。需要指出的是，氨磺必利是一种多巴胺D2和D3受体拮抗剂，已在欧洲和50多个国家及地区上市数十年。LB-102是LB Pharmaceuticals开发的氨磺必利的甲基化版本。这种改良使得该药物通过血脑屏障的通透性得到增强，从而可能在较低剂量下达到更佳的治疗效果。LB Pharmaceuticals计划在25个地点招募约350名受试者，利用常用的精神分裂症临床试验指标PANSS（阳性和阴性症状量表）来测试三种不同剂量下，该药物的效果是否优于安慰剂。该公司表示，这一研究将主要针对住院患者，并持续四周。如果中期试验成功，LB Pharmaceuticals有望在2025年开展LB-102的多个3期试验，并计划在2028年提交新药申请（NDA）。而在精神分裂症治疗方面取得的进展仅为公司的第一步，他们还计划针对抑郁症、双相抑郁症和其他疾病进行进一步研究。Zachary Prensky先生是LB Pharmaceuticals的现任首席执行官，并且也是该公司的联合创始人。他在投资和企业管理方面拥有丰富的经验。大家都在看▲欲了解更多前沿技术在生物医药产业中的应用，请长按扫描上方二维码，即可访问“药明直播间”，观看相关话题的直播讨论与精彩回放参考资料：[1] LB Pharmaceuticals raising $75M for schizophrenia drug as Karuna looks to change the field，Retrieved Sep 25, 2023, from https://endpts.com/nyc-biotech-lb-pharmaceuticals-eyes-75m-for-new-take-on-decades-old-schizophrenia-drug/[2] UNITED STATES SECURITIES AND EXCHANGE COMMISSION. Retrieved September 25, 2023 from https://www.sec.gov/Archives/edgar/data/1691082/000169108223000004/xslFormDX01/primary_doc.xml免责声明：药明康德内容团队专注介绍全球生物医药健康研究进展。本文仅作信息交流之目的，文中观点不代表药明康德立场，亦不代表药明康德支持或反对文中观点。本文也不是治疗方案推荐。如需获得治疗方案指导，请前往正规医院就诊。版权说明：本文来自药明康德内容团队，欢迎个人转发至朋友圈，谢绝媒体或机构未经授权以任何形式转载至其他平台。转载授权请在「药明康德」微信公众号回复“转载”，获取转载须知。分享，点赞，在看，聚焦全球生物医药健康创新

临床2期临床3期

2022-07-20

·BioSpace

LB Announces Publication of Phase 1 Clinical Study of LB-102

NEW YORK--(BUSINESS WIRE)-- LB Pharmaceuticals Inc (LB), a biotechnology company focused on developing and commercializing novel and improved versions of successful CNS treatments, announced today that details from its first Phase 1 clinical trial of LB-102 (NCT04187560) have been published. The article, titled "A randomized, double-blind, placebo controlled, phase 1 study of the safety, tolerability, pharmacokinetics, and pharmacodynamics of LB-102, a selective dopamine D2/3/5-HT7 inhibitor" (Biernat et al. 2022), was published online in Psychopharmacology. LB-102 is being developed by LB as a potential treatment for schizophrenia and other psychiatric disorders. A copy of the publication is available on the Company’s website at www.LBPharma.us. This clinical study enrolled 64 healthy volunteers and was the first time LB-102 had been dosed in humans. The study consisted of 8 arms (each of 8 subjects randomized 3:1 LB-102: placebo), 5 single dose and 3 multiple doses (BID dosing) arms. The primary endpoint of this dose-finding study was safety, with pharmacokinetics as a secondary endpoint. The study demonstrated that LB-102 was safe and well-tolerated. The pharmacokinetic properties of LB-102 were amenable to once-a-day dosing, with a half-life of ~13 hours. Plasma concentrations of LB-102 were nearly perfectly dose-linear. Based on these encouraging data, as well as data from a subsequent clinical study of dopamine receptor occupancy using positron emission tomography, LB is planning a Phase 2 clinical study of LB-102 in patients with acute exacerbated schizophrenia. This will be a double-blind, placebo-controlled study of two single daily doses of less than 100 mg LB-102 versus placebo. The primary endpoint of the study will be change in PANSS from baseline at 4 weeks. About LB Pharmaceuticals LB is a development stage CNS-focused life science company devoted to commercializing novel and improved versions of successful CNS treatments used overseas but unavailable in the United States. LB’s lead compound, LB-102 (N-methyl amisulpride) is a novel dopamine/5-HT7 antagonist based on amisulpride, a drug successfully used to treat schizophrenia and other psychiatric disorders in Europe for decades. More information about LB-102 and LB Pharmaceuticals may be found on our website located at www.LBPharma.us.

临床结果

2021-04-26

·BioSpace

LB Pharmaceuticals To Participate in the B. Riley Securities’ Neuroscience Conference

April 26, 2021 15:09 UTC NEW YORK--(BUSINESS WIRE)-- LB Pharmaceuticals Inc, (“LB”) a biotechnology company focused on developing and commercializing novel and improved versions of successful CNS treatments, announced today that Zachary Prensky, President and Chief Executive Officer, will present at the 2021 B. Riley Securities’ Neuroscience Conference, to be held virtually on April 28-29, 2021. LB’s presentation will take place on Thursday, April 29th at 9:30am ET and will be live webcast to registered attendees at . Following the presentation, Mr. Prensky will participate in a question-and-answer session. After completion of the event, a replay of the presentation will be publicly available on the LB website at . About LB Pharmaceuticals LB is a development stage CNS-focused life science company devoted to commercializing novel and improved versions of successful CNS treatments used extensively overseas but never developed, approved, or marketed, in the United States. Our approach is to create a research-focused organization dedicated to generating novel intellectual property around improved versions of these former best-selling drugs. We have a low-risk, high-reward drug development business plan: Invest in bringing to the US market patented, branded, first-to-market versions of standard-of-care CNS therapies currently in use worldwide. LB’s lead compound, LB-102, or N-methyl amisulpride, is a patented benzamide designed to be an improved version of amisulpride, a dopamine/5-HT7 antagonist successfully used to treat schizophrenia in Europe for decades. LB-102 was designed to improve on amisulpride’s low permeability across the blood brain barrier. LB-102 has the potential to offer schizophrenia patients the benefits of amisulpride at a lower dose than amisulpride. A first-in-human, double-blind placebo-controlled Phase 1 study designed to test the safety and pharmacokinetics of LB-102 was completed over the summer of 2020. A Phase 2 clinical trial in acute schizophrenia patients is expected to commence in the fourth quarter of 2021. More information about LB-102 and LB Pharmaceuticals may be found on our corporate website located at

100 项与 N-methyl amisulpride 相关的药物交易

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适应症	最高研发状态	国家/地区	公司	日期
急性精神分裂症	临床2期	美国	LB Pharmaceuticals, Inc.初创企业	2023-12-04

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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


NCT04187560 (Pubmed) 人工标引	临床1期	精神分裂症	64	LB-102 (SAD portion)	壓襯鏇憲膚衊衊淵糧積(繭願範餘遞窪簾壓醖繭) = LB-102 was generally safe and well-tolerated, and clinical lab values were unremarkable at all doses, save for prolactin which was transiently elevated in the majority of subjects treated with LB-102 襯齋鹹繭糧鏇顧觸選簾 (衊夢觸廠獵鏇衊壓夢製 )	积极	2022-07-16
NCT04187560 (Pubmed) 人工标引	临床1期	精神分裂症	64	LB-102 (MAD portion)		积极	2022-07-16
NCT04187560 (BusinessWire) 人工标引	临床1期	-	64	LB-102	鬱範衊醖鹽艱鏇獵範築(構遞鏇齋選願衊壓衊繭) = consistent with dopamine antagonists and included transient increases in QT interval and prolactin levels, though these did not result in clinical observations 遞艱鏇糧淵糧膚壓膚範 (壓繭鏇膚夢蓋鏇願構簾 ) 更多	积极	2020-09-14