Delving into the Latest Updates on Fenoterol Hydrobromide with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

1-(3,5-dihydroxyphenyl)-1-hydroxy-2-((4-hydroxyphenyl)isopropylamino)ethane, 1-(p-hydroxyphenyl)-2-((β-hydroxy-β-(3',5'-dihydroxyphenyl))ethyl)aminopropane, 3,5-dihydroxy-α-(((p-hydroxy-α-methylphenethyl)amino)methyl)benzyl alcohol

+ [13]

Target

β2-adrenergic receptor

Action

agonists

Mechanism

β2-adrenergic receptor agonists(Beta-2 adrenergic receptor agonists)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesRespiratory Diseases+ [1]

Active Indication

Bronchitis, ChronicPneumoconiosisPulmonary Emphysema+ [2]

Inactive Indication

Chronic lung disease

Originator Organization-

Active Organization

Nippon Boehringer Ingelheim Co., Ltd.

Inactive Organization

University Medical Center Göttingen

Boehringer Ingelheim GmbH

Drug Highest PhaseApproved

First Approval Date

(01 Jan 1971),

AsthmaPulmonary Disease, Chronic Obstructive

Regulation-

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Structure/Sequence

Molecular FormulaC17H21NO4

InChIKeyLSLYOANBFKQKPT-UHFFFAOYSA-N

CAS Registry13392-18-2

View All Structures (2)

The aims of this study is :
to assess the bronchodilator (DUOVENT HFA) response of parameters measured by the forced oscillations (FOT) and in particular the reactance parameters related to the presence of a limitation of expiratory flows
to compare the response of the reactance parameters to bronchodilators with the conventional spirometric parameters (FEV1) and inspiratory capacity (IC), and according to the severity of the disease
to assess and compare the relationship between the response to bronchodilators in terms of IC on the one hand and on the other hand in terms of FEV1, reactance parameters (measured by FOT), resistance parameters (measured by plethysmography and FOT)
Assess and compare the relationship between dyspnea intensity assessed by various scales and conventional respiratory function parameters (spirometry, plethysmography, diffusion indices) and parameters measured by FOT

Start Date23 Apr 2019

Sponsor / Collaborator-

100 Clinical Results associated with Fenoterol Hydrobromide

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100 Translational Medicine associated with Fenoterol Hydrobromide

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100 Patents (Medical) associated with Fenoterol Hydrobromide

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2,706

Literatures (Medical) associated with Fenoterol Hydrobromide

01 Mar 2025·Journal of Pharmaceutical and Biomedical Analysis

Plasma metabolomic signatures after oral administration of ritonavir in COVID-19 treatment via chemometrics-assisted UPLC/Q-TOF/MS/MS

Article

Author: Gundogdu, Gulsah ; Demir, Sema Nur ; Kadioglu, Yucel ; Abd El-Aty, A M ; Yuksel, Busra ; Bayrak, Burak ; Demirkaya Miloglu, Fatma

Understanding the pharmacodynamics of ritonavir through metabolomics offers insights into its side effects and helps in the development of safer therapies. This study aimed to investigate the effects of ritonavir treatment on the metabolic profiles of rabbits via a metabolomics approach, with the objective of elucidating its impact on various biochemical pathways and identifying relevant biomarkers. The rabbits were divided into control and ritonavir-treated groups, and their plasma samples were analyzed via ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC/Q-TOF/MS/MS). Metabolites were identified on the basis of the masscharge ratio (m/z) and validated via XCMS software. Metabolites with a fold change ≥ 1.5 and P ≤ 0.01 were analyzed via principal component analysis (PCA) and orthogonal partial least squares discrimination analysis (OPLS-DA) to distinguish between the groups. MetaboAnalyst 6.0 was used for pathway analysis to identify metabolic pathways affected by ritonavir. The PCA and OPLS-DA models revealed clear separation between the control and ritonavir-treated groups, with high R² and Q² values indicating robust model performance. Pathway analysis revealed that ritonavir treatment significantly affected several metabolic pathways, including those related to ether lipid, phenylalanine, sphingolipid, and glycerophospholipid metabolism. Particularly significant changes were observed in metabolites related to lipid metabolism, oxidative stress responses and cellular signaling. Ritonavir significantly impacts metabolic pathways, particularly those involved in lipid metabolism, and oxidative stress responses, which may influence immune responses and drug interactions. This study also highlights the potential of integrating metabolomics with personalized medicine approaches to optimize ritonavir treatment strategies and reduce adverse effects. These findings indicate that ritonavir significantly influences cellular homeostasis and metabolic processes in addition to its antiviral properties. This highlights the necessity of comprehending the metabolic effects of ritonavir to enhance its clinical application, especially in the management of COVID-19. Further research is warranted to explore these alterations and their implications for therapeutic strategies.

01 Feb 2025·Journal of Biological Chemistry

Substrate-specific effects point to the important role of Y361 as part of the YER motif in closing the binding pocket of OCT1

Article

Author: Neumann, Anna ; Lazzarin, Erika ; Stockner, Thomas ; Lindemann, Erik ; Meyer-Tönnies, Marleen J ; Tzvetkov, Mladen V ; Römer, Sarah

Organic cation transporter 1 (OCT1) is located in the sinusoidal membrane of human hepatocytes. It mediates the uptake of hydrophilic organic cationic drugs in hepatocytes and thus determine their systemic concentrations. OCT1 has a broad spectrum of structurally diverse substrates like metformin, sumatriptan, trospium, and fenoterol. Recent cryo-EM data suggested that Y361, E386, and R439, referred to as the YER motif, could be important for transport. Building on this, we used extensive functional analyses to investigate the general function, and the substrate-specific effects of the YER motif. We determined the activity of the Y361A, E386A, and R439A mutants for fifteen OCT1 substrates. Extended mutagenesis revealed the negative charge of E386 and the positive charge of R439 as essential for the transport of all substrates tested. Charge reversal mutants, E386R-R439E, did not restore transport activity, suggesting that at least one of the two amino acids is involved in additional interactions essential for transport. Y361 exhibited substrate-specific effects. The Y361A mutant transported fenoterol, but not pirbuterol or other beta₂-adrenergic drugs with only one aromatic ring. MD simulations suggested that substrates with aromatic or lipophilic characteristics may compensate for the missing aromatic ring at position 361. Only tryptophan at codon 361 efficiently rescued the transport of the Y361A mutant supporting hydrogen bound interaction with E386 and R439. Our study confirms that the YER motif is essential for OCT1 transport and points to Y361 as a lever that interacts with E386 and R439 to trigger the closing of the binding pocket of human OCT1.

01 Feb 2025·Analytical and Bioanalytical Chemistry

LC-HRMS screening procedure for the detection of 11 different classes of prohibited substances in dried urine spots for doping control purposes

Article

Author: Tsivou, Maria ; Pizzolato, Francesca ; Honesová, Lenka ; Gmeiner, Günter ; Mazzarino, Monica ; Van Eenoo, Peter

Dried urine spots have recently been proposed as an alternative matrix in the anti-doping field. Drying urine may open the opportunity to limit microbial and thermal degradation of the prohibited substances during transportation to the anti-doping laboratories without the need for refrigeration or freezing. In this study, a multi-targeted initial testing procedure was developed for the determination of 237 prohibited drugs/metabolites from 11 different classes in dried urine spots. The comparability between two different microsampling techniques (i.e., Whatman^® FTA DMPK-C cards and Mitra^® tips) was evaluated. The developed method was then used to evaluate the stability of the target compounds in urine for 7 days under different environmental conditions to simulate the transportation of the urine samples from the collection sites to anti-doping laboratories. Sample preparation consists of (i) extraction of the analytes from the collection device using a mixture of acetonitrile/methanol (1/1) for 30 min at 40 °C, (ii) enzymatic hydrolysis, and (iii) sample concentration by solid-phase extraction. Analysis was performed using liquid chromatography coupled to high-resolution mass spectrometry. The entire workflow was validated in terms of specificity (analytes were distinguishable from the matrix interferences), sensitivity (only with the Mitra^® tips the limits of detection comply with the World Anti-Doping Agency's requirements for the majority of the target compounds), carry-over (no signals in the negative urine injected after the positive urine), matrix effect (16-28% for Mitra^® tips and 22-35% for DMPK-C cards), and extraction yield (Mitra^® tips: 51-88%; DMPK-C cards: 40-76%). As proof of concept, authentic urine samples were analyzed: results obtained in dried urine were compared with those of fluid urine, providing good agreement. Stability studies showed that the target compounds were stable for the whole duration of the study (7 days) at -20 and 4 °C in both fluid and dried urine. At 50 °C or at 20-25 °C, several thiazide-based compounds were completely degraded to their degradation product in the first 24 h or after 3-4 days in fluid urine, whereas in dried urine the compounds were detectable for the entire duration of the study.

100 Deals associated with Fenoterol Hydrobromide

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External Link

KEGG	Wiki	ATC	Drug Bank
D01428	Fenoterol Hydrobromide	R03AC04 G02CA03 R03CC04	DB01288

R&D Status

Approved

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Indication	Country/Location	Organization	Date
Bronchitis, Chronic	Japan	Nippon Boehringer Ingelheim Co., Ltd.	15 Mar 1999
Pneumoconiosis	Japan	Nippon Boehringer Ingelheim Co., Ltd.	15 Mar 1999
Pulmonary Emphysema	Japan	Nippon Boehringer Ingelheim Co., Ltd.	15 Mar 1999
Asthma	-	-	01 Jan 1971
Pulmonary Disease, Chronic Obstructive	-	-	01 Jan 1971

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Asthma	Phase 2	-	Boehringer Ingelheim GmbH	01 Feb 1990
Chronic lung disease	Phase 1	Netherlands	Boehringer Ingelheim GmbH	01 Oct 2002
Pulmonary Disease, Chronic Obstructive	Phase 1	Netherlands	Boehringer Ingelheim GmbH	01 Oct 2002

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ERS2014	Not Applicable	Lung Diseases, Obstructive	42	Fenoterol	(esokxopxck) = ehvohqdsbg lqgkkeybio (xllewteorj )	Positive	01 Sep 2014
				Ipratropium	(esokxopxck) = rairrvmcam lqgkkeybio (xllewteorj )
NCT00274066 (Pubmed \| Chest)	Phase 3	Pulmonary Disease, Chronic Obstructive Maintenance \| Add-on	60	Ipratropium bromide	mbamddnogt(adyvuzxlvz) = lnqcxoevec egiroiygnq (ktskscdwzq )	-	01 Nov 2007
				Fenoterol	mbamddnogt(adyvuzxlvz) = yvniizsgal egiroiygnq (ktskscdwzq )