Delving into the Latest Updates on Flupentixol Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Flupenthixol, Flupenthixole, Flupentixol dihydrochloride

+ [7]

Target

DRDs

Action

antagonists

Mechanism

DRDs antagonists(Dopamine receptors antagonists)

Therapeutic Areas

Nervous System Diseases

Active Indication

Schizophrenia

Inactive Indication-

Originator Organization-

Active Organization

H. Lundbeck A/S

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC23H25F3N2OS

InChIKeyNJMYODHXAKYRHW-UHFFFAOYSA-N

CAS Registry2709-56-0

View All Structures (2)

Fute (Flupentixol) combined with MARTAs (Multiple-Acting Receptor Targeted Antipsychotics) drugs has its clinical efficacy toward positive symptoms and might reduce the metabolic syndrome-related factors in patients. This study is the first clinical trial to explore the treatment of patients with flupentixol combined with MARTAs. However, due to research limitations, the number of patients who participated in the clinical trial is small, and it depends on subsequent larger-scale clinical trials for more in-depth verification.

Start Date19 Dec 2019

Sponsor / Collaborator

Taichung Veterans General Hospital

NCT02660840

/ CompletedPhase 1

Interventional, Open-label, Randomised, Crossover, Comparative Study of the Pharmacokinetics and Bioequivalence of Two Flupentixol Formulations - Film Coated Tablet (Test Treatment) - 0.5 mg, 1 mg and 5 mg (H. Lundbeck A/S, Denmark) and Coated Tablet (Fluanxol®) - 0.5 mg, 1 mg and 5 mg (H. Lundbeck A/S, Denmark) in Healthy Volunteers

To establish bioequivalence between new film-coated tablet formulations of 0.5 mg, 1 mg and 5 mg flupentixol and the marketed coated tablet formulations of 0.5 mg, 1 mg, and 5 mg flupentixol, administered as single doses

Start Date01 Jan 2016

Sponsor / Collaborator

H. Lundbeck A/S

NCT02307396

/ CompletedPhase 4IIT

Evaluation of the Necessity of Long-term Pharmacological Treatment With Antipsychotics for the Prevention of Relapse in Long-term Stabilized Schizophrenic Patients: a Randomized, Single-blind, Longitudinal Trial

The main objective of the trial is to evaluate, how long an antipsychotic relapse-prevention should be continued and to which time a patient with schizophrenia is protected enough, so that a withdrawal or reduction of the medication seems appropriate. Relapse is defined as primary outcome.

Start Date01 Feb 2015

Sponsor / Collaborator

Technische Universität München

100 Clinical Results associated with Flupentixol Hydrochloride

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100 Translational Medicine associated with Flupentixol Hydrochloride

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100 Patents (Medical) associated with Flupentixol Hydrochloride

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1,615

Literatures (Medical) associated with Flupentixol Hydrochloride

10 Mar 2025·Journal of Chemical Information and Modeling

Structure-Based Identification of Non-covalent Prolyl Oligopeptidase 80 Inhibitors Targeting Trypanosoma cruzi Cell Entry

Article

Author: dos Santos Carvalho, Alexandra Maria ; Bastos, Izabela Marques Dourado ; Charneau, Sébastien ; Mendonça de Melo, Felipe da Silva ; Motta, Flávia Nader ; Mottin, Melina ; Martins Santana, Jaime ; Costa, Vinícius Alexandre Fiaia ; Grellier, Philippe ; Neves, Bruno Junior

Chagas disease remains a persistent public health challenge due to the limited efficacy and significant toxicity of current pharmacological treatments. This highlights the urgent need for novel drugs with innovative mechanisms of action, specifically targeting cell infection pathways. The prolyl oligopeptidase of Trypanosoma cruzi (POPTc80) has emerged as a promising target for developing inhibitors to block the parasite's infection process. In this study, we developed a robust structure-based virtual screening pipeline to discover potent POPTc80 inhibitors. The customized protocol integrated structural analysis of the 3D structure of POPTc80 and enrichment analysis of molecular docking and shape-based models to optimize the selection of potential inhibitors. After optimization, a large-scale virtual screening of 1.3 million compounds prioritized 19 putative hits for experimental validation. Nine of these compounds demonstrated inhibitory activity at nanomolar concentrations. The most potent inhibitors─LC-44 (K_i = 0.175 μM), LC-45 (K_i = 0.054 μM), LC-46 (K_i = 0.513 μM), LC-50 (K_i = 0.44 μM), LC-53 (K_i = 0.158 μM), and LC-55 (K_i = 0.83 μM)─demonstrated superior inhibitory activity, consistent with the competitive inhibition mechanism predicted by our computational protocol. Subsequently, a phenotypic assay confirmed their ability to effectively inhibit T. cruzi entry into host cells in a dose-dependent manner, further validating their mechanism of action. These findings establish these compounds as promising chemical scaffolds for prospective hit-to-lead optimization, offering a unique opportunity to develop novel, mechanism-driven therapeutics targeting a critical step in the parasite's infection process.

01 Feb 2025·Chromatographia

Development and Validation of Confirmatory Quantitative and Screening Methods for 63 Prohibited Substances in Horse Urine Using LC–MS/MS

Author: Goktas, Eylem Funda ; Kabil, Erol

Abstract: The number of potentially abused substances in horse racing is very large and it is not easy to analyze the full range.To facilitate the analyses of substances of abuse, a method has been developed for 63 substances in horse urine using liquid chromatog.-tandem mass spectrometry.The developed method has been validated according to the 2021/808/EC and AORC criteria.The horse urine samples were extracted after enzymic hydrolysis via a C8-BCX SPE cartridge with an automated SPE and analyzed by LC-MS/MS.According to the validation study results, the within-laboratory reproducibility CV was no more than 13.9% and the average recoveries ranged from 90.71 to 117.94% for repeatability and reproducibility.The decision limits (CCα) for quant. anal. and detection capabilities (CCβ) for qual. screening were close to the targeted limit for each substance.The results of the present study showed that the method was able to perform quant. analyses of 54 substances and screening analyses of 9 substances (total 63) in horse urine and that the results were valid and applicable.The validated method was successfully applied to five proficiency tests and three suspected samples.

02 Jan 2025·Expert Opinion on Drug Safety

Risk of drug-induced delirium in older patients- a pharmacovigilance study of FDA adverse event reporting system database

Article

Author: Cui, Yimin ; Li, Jiayu ; Zhou, Ying ; Wan, Liyan ; Jia, Boying ; Zhou, Shuang

BACKGROUNDDrug-induced delirium is known risk factors associated with increased morbidity and mortality in older patients. The objective was to evaluate the risk of drug-related delirium in older patients based on the FDA Adverse Event Reporting System (FAERS).RESEARCH DESIGN AND METHODSDelirium reports in older patients (age ≥65) extracted from the FAERS database using Open Vigil 2.1. The reported odds ratio and the proportional reported ratio were calculated to detect the adverse reaction signal of delirium. Combined with published evidence, suspected drugs were categorized as known, possible, or new potential delirium-risk-increasing drugs.RESULTSOf the 130,885 reports (including 28,850 delirium events and 1,857 drugs) analyzed for this study, 314 positive signal drugs were detected. Positive signal drugs are mainly concentrated on the drug of nervous system, cardiovascular system , alimentary tract and metabolism and anti-infectives for systemic use. Of the positive signal drugs, 26.11% (82/314) were known delirium-risk increasing drugs, 44.90% (141/314) were possible and 28.98% (91/314) were new potential.CONCLUSIONDrug-induced delirium risk is prevalent in older patients, according to the FAERS. The risk level of drug-induced delirium should be taken into account to optimize drug therapy in clinical practice.

100 Deals associated with Flupentixol Hydrochloride

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