Last update 21 Nov 2024

Dilevalol

Last update 21 Nov 2024

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Dilevalon, Levadil

+ [2]

Target

β-adrenoceptors

Mechanism

β-adrenoceptors antagonists(Beta adrenergic receptors antagonists)

Therapeutic Areas-

Active Indication-

Inactive Indication-

Originator Organization

Schering-Plough Corp.

Active Organization-

Inactive Organization-

Drug Highest Phase-

First Approval Date-

Regulation-

Structure

Molecular FormulaC19H24N2O3

InChIKeySGUAFYQXFOLMHL-ACJLOTCBSA-N

CAS Registry75659-07-3

100 Clinical Results associated with Dilevalol

100 Translational Medicine associated with Dilevalol

100 Patents (Medical) associated with Dilevalol

139

Literatures (Medical) associated with Dilevalol

01 May 2019·Journal of Pharmaceutical and Biomedical AnalysisQ3 · MEDICINE

Development of an integrated chromatographic system for ω-transaminase-IMER characterization useful for flow-chemistry applications

Q3 · MEDICINE

Article

Author: Marrubini, G ; Massolini, G ; Corti, M ; Kupfer, T ; Calleri, E ; Ferrandi, E E ; Rinaldi, F ; Terreni, M ; Conti, P ; Monti, D ; Tripodo, G ; Temporini, C

An integrated chromatographic system was developed to rapidly investigate the biocatalytic properties of ω-transaminases useful for the synthesis of chiral amines. ATA-117, an (R)-selective ω-transaminase was selected as a proof of concept. The enzyme was purified and covalently immobilized on an epoxy monolithic silica support to create an immobilized enzyme reactor (IMER). Reactor efficiency was evaluated in the conversion of a model substrate. The IMER was coupled through a switching valve to an achiral analytical column for separation and quantitation of the transamination products. The best conditions of the transaminase-catalyzed bioconversion were optimized by a design of experiments (DoE) approach. The production of (R)-1-(4-methoxyphenyl)propan-2-amine and (R)-1-methyl-3-phenylpropylamine, intermediates for the synthesis of the bronchodilator formoterol and the antihypertensive dilevalol respectively, was achieved in the presence of different amino donors. The enantiomeric excess (ee) was determined off-line by developing a derivatization procedure using Nα-(2,4-dinitro-5-fluorophenyl)-L-alaninamide reagent. The most satisfactory conversion yields were 60% for (R)-1-(4-methoxyphenyl)propan-2-amine and 29% for (R)-1-methyl-3-phenylpropylamine, using isopropylamine as amino donor. The enantiomeric excess of the reactions were 84%_R and 99%_R, respectively.

10 Nov 2017·Oncotarget

Prediction on the risk population of idiosyncratic adverse reactions based on molecular docking with mutant proteins

Article

Author: Xie, Hongbo ; Chen, Xiujie ; Ke, Kehui ; Jin, Qing ; Hu, Ming ; Zeng, Diheng ; Huo, Diwei ; Zhang, Denan ; Liu, Lei

Idiosyncratic adverse drug reactions are drug reactions that occur rarely and unpredictably among the population. These reactions often occur after a drug is marketed, which means that they are strongly related to the genotype of the population. The prediction of such adverse reactions is a major challenge because of the lack of appropriate test models during the drug development process. In this study, we chose withdrawn drugs because the reasons why they were withdrawn and from which countries or regions is easily obtained. We selected Dilevalol and its chiral drug (Labetalol) as the investigatory drugs, as they have been withdrawn from a European market (Britain) because of serious hepatotoxicity. First, we searched for and obtained the Dilevalol-induced- liver-injury related protein, multidrug resistance protein 1 (MDR1), from the Comparative Toxicogenomics Database (CTD). Then, we searched and extracted 477 non-synonymous single nucleotide polymorphisms (nsSNP) on MDR1 in the dbSNP database. Second, we used the VarMod tool to predict the functional changes of MDR1 induced by these nsSNPs, from which we extracted the nsSNPs that significantly change the functions of this protein. Third, we built the three-dimensional structures of those variant proteins and used AutoDock to perform a docking study, choosing the best model to determine the sites of nsSNPs. Finally, we used the data from the 1000 Genomes Project to verify the dominant population distribution of the risk SNP. We applied the same strategy to the post-marketing drug-induced liver injury drugs to further test the feasibility of our method.

01 Sep 2017·Journal of HypertensionQ2 · MEDICINE

The effect of vasodilator β-blockers on renal function in hypertensive patients

Q2 · MEDICINE

Article

Author: Wats, Karan ; Kwon, Lawrence H. ; Rosendorff, Clive

BACKGROUNDNot only is there a limited number of studies on the effects of vasodilator β-blocker (VBB) therapy on kidney function - specifically, glomerular filtration rate (GFR), serum creatinine (sCr) and proteinuria - but of those that have been reported, the results are mixed. This meta-analysis seeks to assess the efficacy of VBBs on selected renal parameters in hypertensive patients.METHODSWe conducted a meta-analysis of any prospective trial that provided both baseline and follow-up of at least 4 weeks of VBB therapy - carvedilol, labetalol, dilevalol, nebivolol and celiprolol in patients with hypertension. We used Ovid MEDLINE, EMBASE and PubMed, all without date restrictions. We included 39 studies totaling 3987 patients.RESULTSAlthough VBBs did not significantly change GFR or sCr levels after at least 4 weeks of therapy, they did significantly decrease protein excretion by -0.12 SD units [95% confidence interval (CI) -0.19 to -0.04; P < 0.01]. VBBs did not alter renal blood or plasma flow, but renal vascular resistance (RVR) decreased by -20.03 mmHg min/l (95% CI -28.92 to -11.15; P < 0.01). In the analysis which compared VBBs with non-VBBs, the only significant difference was the greater decrease in RVR in the VBB group by -38.44 mmHg min/l (95% CI -60.57 to -16.31; P < 0.01).CONCLUSIONVBBs do not affect GFR or sCr levels, but decrease protein excretion. This class of β-blockers, however, is not superior to non-VBBs in reducing proteinuria. VBBs decrease RVR significantly more than non-VBBs.

100 Deals associated with Dilevalol

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Dilevalol

Overview

Basic Info

Structure

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R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Regulation