5-HT7 receptor antagonists(Serotonin 7 (5-HT7) receptor antagonists), D2 receptor antagonists(Dopamine D2 receptor antagonists), D3 receptor antagonists(Dopamine D3 receptor antagonists)

Therapeutic Areas

Other Diseases

Active Indication

Acute schizophrenia

Inactive Indication-

Originator Organization

LB Pharmaceuticals, Inc.Startup

Active Organization

LB Pharmaceuticals, Inc.Startup

Inactive Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

Structure

Molecular FormulaC17H26N2O6

InChIKeyQJMAFHBXQNFFKL-UHFFFAOYSA-N

CAS Registry1047659-23-3

Clinical Trials associated with N-methyl amisulpride

NCT06179108 / Active, not recruitingPhase 2

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.

Start Date04 Dec 2023

Sponsor / Collaborator

LB Pharmaceuticals, Inc.Startup

NCT04588129 / CompletedPhase 1

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.

Start Date05 Jan 2021

Sponsor / Collaborator

LB Pharmaceuticals, Inc.Startup

[+1]

NCT04187560 / CompletedPhase 1

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.

Start Date22 Jan 2020

Sponsor / Collaborator

LB Pharmaceuticals, Inc.Startup

100 Clinical Results associated with N-methyl amisulpride

100 Translational Medicine associated with N-methyl amisulpride

100 Patents (Medical) associated with N-methyl amisulpride

Literatures (Medical) associated with N-methyl amisulpride

02 Nov 2023·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

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

INTRODUCTIONThe 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 COVEREDThis 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 OPINIONThe 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.

01 Dec 2022·Chemosphere

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

Article

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

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.

01 Sep 2022·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

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

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.

News (Medical) associated with N-methyl amisulpride

20 Jul 2022

·www.biospace.com

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.

Clinical Result

26 Apr 2021

·www.biospace.com

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

02 Feb 2021

·www.biospace.com

LB Pharmaceuticals Announces the Initiation of Patient Dosing in Open Label Phase 1b Imaging 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 the administration of the first dose of LB-102 in a Phase 1b clinical trial (Clinical Trials Identifier NCT04588129). This clinical study is designed to evaluate the dopamine receptor occupancy of LB-102 in healthy subjects using positron emission tomography (PET). LB-102, a more lipophilic version of amisulpride, was designed to improve on amisulpride’s notoriously poor membrane (BBB) permeability while matching amisulpride’s binding affinity to the D 2 /D 3 and 5HT 7 receptors (critical to the treatment of schizophrenia). Amisulpride, which is not available in the US, is used for the treatment of schizophrenia and is widely prescribed in over 50 countries, including the EU. Furthermore, amisulpride has been shown to be both effective and well tolerated, as demonstrated by the low all-cause discontinuation rate (a key indicator of patient compliance) compared to 31 other antipsychotics (Huhn et al., 2019). “The early clinical safety and tolerability profile of LB-102 as seen in last year’s Phase 1 first-in-human study suggests that we are on the right path”, stated Zachary Prensky, President and CEO. “The goal of this Phase 1b study is both to confirm dopamine target engagement and assist in dose selection for our upcoming Phase 2 study in acute schizophrenia patients. We are excited to build on the encouraging clinical data generated to date, and are hopeful to be able to provide doctors and patients with a differentiated and effective treatment option for schizophrenia.” The American Psychological Association states that less than half of schizophrenia patients treated with current antipsychotics exhibit significant improvements, illustrating the serious unmet medical need that currently exists in the treatment of schizophrenia. With amisulpride unavailable in the US for the treatment of schizophrenia, if approved, LB-102 would become the first benzamide treatment available in the US to treat schizophrenia. About LB-102 LB-102, or N-methyl amisulpride, is a patented benzamide designed to be an improved version of amisulpride, a dopamine/5-HT 7 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. 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. More information about LB-102 and LB Pharmaceuticals may be found on our corporate website located at View source version on businesswire.com:

100 Deals associated with N-methyl amisulpride

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acute schizophrenia	Phase 2	US	LB Pharmaceuticals, Inc.Startup	04 Dec 2023

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04187560 (Pubmed) Manual	Phase 1	Schizophrenia	64	LB-102 (SAD portion)	(xcenkqotsk) = 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 hizzzlbdri (pcqhgnuvgz )	Positive	16 Jul 2022
NCT04187560 (Pubmed) Manual	Phase 1	Schizophrenia	64	LB-102 (MAD portion)		Positive	16 Jul 2022
NCT04187560 (BusinessWire) Manual	Phase 1	-	64	LB-102	(raymbsawkd) = consistent with dopamine antagonists and included transient increases in QT interval and prolactin levels, though these did not result in clinical observations ktgueorbva (wcivaydqqm ) View more	Positive	14 Sep 2020

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