Delving into the Latest Updates on Enecadin Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Enecadin

+ [2]

Target

Calpain1/2 x SCNA x VDCCs

Mechanism

Calpain1/2 inhibitors(Calpain1/2 inhibitors), SCNA blockers(Sodium channel alpha subunit blockers), VDCCs blockers(Voltage-gated calcium channel blockers)

Therapeutic Areas

Nervous System DiseasesCardiovascular Diseases

Active Indication-

Inactive Indication

Acute Ischemic StrokeNervous System Diseases

Originator Organization

Nippon Shinyaku Co., Ltd.

Active Organization-

Inactive Organization

Paion Deutschland GmbH

Nippon Shinyaku Co., Ltd.

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC21H28FN3O

InChIKeySZSHJTJCJOWMHM-UHFFFAOYSA-N

CAS Registry259525-01-4

View All Structures (2)

The main objective of this study is to investigate the tolerability of enecadin in patients with acute ischemic stroke. Furthermore, the pharmacokinetics of enecadin in both male and female patients with acute ischemic stroke will be assessed. Efficacy trends will be evaluated up to day 30 post stroke.

Start Date01 May 2006

Sponsor / Collaborator

Paion Deutschland GmbH

100 Clinical Results associated with Enecadin Hydrochloride

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100 Translational Medicine associated with Enecadin Hydrochloride

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100 Patents (Medical) associated with Enecadin Hydrochloride

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34

Literatures (Medical) associated with Enecadin Hydrochloride

26 Sep 2023·Antibiotics (Basel, Switzerland)

Naturally Derived Malabaricone B as a Promising Bactericidal Candidate Targeting Multidrug-Resistant Staphylococcus aureus also Possess Synergistic Interactions with Clinical Antibiotics.

Article

Author: Govind, Murugan Govindakurup ; Kaul, Grace ; Akhir, Abdul ; Dan, Mathew ; Shukla, Manjulika ; Chopra, Sidharth ; Sivadas, Neethu ; Radhakrishnan, Kokkuvayil Vasu

The emergence of multidrug-resistant (MDR) superbugs underlines the urgent need for innovative treatment options to tackle resistant bacterial infections. The clinical efficacy of natural products directed our efforts towards developing new antibacterial leads from naturally abundant known chemical structures. The present study aimed to explore an unusual class of phenylacylphenols (malabaricones) from Myristicamalabarica as antibacterial agents. In vitro antibacterial activity was determined via broth microdilution, cell viability, time-kill kinetics, biofilm eradication, intracellular killing, and checkerboard assays. The efficacy was evaluated in vivo in murine neutropenic thigh and skin infection models. Confocal and SEM analyses were used for mechanistic studies. Among the tested isolates, malabaricone B (NS-7) demonstrated the best activity against S. aureus with a favorable selectivity index and concentration-dependent, rapid bactericidal killing kinetics. It displayed equal efficacy against MDR clinical isolates of S. aureus and Enterococci, efficiently clearing S. aureus in intracellular and biofilm tests, with no detectable resistance. In addition, NS-7 synergized with daptomycin and gentamicin. In vivo, NS-7 exhibited significant efficacy against S. aureus infection. Mechanistically, NS-7 damaged S. aureus membrane integrity, resulting in the release of extracellular ATP. The results indicated that NS-7 can act as a naturally derived bactericidal drug lead for anti-staphylococcal therapy.

28 Mar 2023·Scientific reports

Aerobic biodegradation of untreated polyester-polyether urethanes by newly isolated yeast strains Exophilia sp. NS-7 and Rhodotorula sp. NS-12.

Article

Author: Moghimi, Hamid ; Giyahchi, Minoo

Polyester-urethanes as the most widely used polyurethanes (PUs) are among the most recalcitrant plastics in natural conditions. Among existing approaches for managing and reducing plastic waste, biodegradation as a promising approach to reduce plastic waste pollution has drawn scientific society's attention in recent years. In this study, two polyester-polyether urethane degrading yeasts were isolated and identified as two new strains of Exophilia sp. NS-7 and Rhodotorula sp. NS-12. The results showed that Exophilia sp. NS-7 is esterase, protease, and urease positive, and Rhodotorula sp. NS-12 can produce esterase and urease. Both strains can degrade Impranil^® as the sole carbon source with the highest growth rate in 4-6 and 8-12 days, respectively. SEM micrograph revealed PU degradation ability in both strains by showing so many pits and holes in treated films. The Sturm test showed that these two isolates can mineralize PU to CO₂, and significant decreases in N-H stretching, C-H stretching, C=O stretching, and N-H/C=O bending absorption in the molecular structure of PU were revealed by the FT-IR spectrum. The detection of the deshielding effect in chemical shifts of the H-NMR spectrum after the treatment also confirmed the destructive effects of both strains on PU films.

01 May 2022·Annals of clinical case reports

Tocotrienols: Exciting Biological and Pharmacological Properties of Tocotrienols and other Naturally Occurring Compounds, Part I.

Article

Author: Qureshi, A A

Inflammation has been implicated in cardiovascular disease and tocotrienols are potent hypocholesterolemic agents that reduce β-hydroxy-β-methyl-glutaryl coenzyme A reductase activity, which is degraded via the ubiquitin-proteasome pathway. Impact of various tocotrienols (α-, γ-, or δ-tocotrienol) treatments inhibit the chymotrypsin-like activity of 20S rabbit muscle proteasome (>50%) in RAW 264.7 cells and BALB/c mice. Moreover, the effect of various tocotrienols (α-, γ-, or δ-tocotrienol), α-tocopherol, quercetin, riboflavin, (-) Corey lactone, amiloride, dexamethasone supplemented diets fed to chickens (4-weeks) resulted in reduction of total cholesterol, LDL-cholesterol, and triglycerides. This trend was also observed in macrophages from RAW 264.7 cells, in LPS-induced thioglycolate-elicited peritoneal macrophages derived from C57BL/6, BALB/c, LMP7/MECL-1^-/-, and PPAR-α^-/- knockout mice from young (4-week-old) and senescent (42-week-old) mice, resulting in significant inhibition of TNF-α and nitric oxide levels (30% to 70%), blocked degradation of P-IκB protein, and decreased activation of NF-κB, followed gene suppression of mRNA levels of TNF-α, IL-1β, IL-6, and iNOS. In human study, normal or hypercholesterolemic subjects administered two capsules/d of NS-7 or NS-6 (4-weeks) showed decrease in serum CRP, NO, γ-GT, total cholesterol, LDL-cholesterol, and triglycerides levels in normal as compared to hypercholesterolemic subjects (12% to 39%). In second study, hypercholesterolemic subjects were given increasing doses of δ-tocotrienol (125 mg, 250 mg, 500 mg, and 750 mg/day) plus AHA Step-1 diet (4-weeks). The most effective dose of tocotrienols (250 mg/day) may be used to lower serum NO (40%), CRP (40%), MDA (34%), γ-GT (22 %), and inflammatory cytokines IL-1α, IL-12, IFN-γ by 15% to 17%, and increase TAS levels by 22%.

100 Deals associated with Enecadin Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Enecadin Hydrochloride	-	DB13032

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acute Ischemic Stroke	Phase 2	BE	Paion Deutschland GmbH	01 May 2006
Acute Ischemic Stroke	Phase 2	AT	Paion Deutschland GmbH	01 May 2006
Acute Ischemic Stroke	Phase 2	DE	Paion Deutschland GmbH	01 May 2006
Nervous System Diseases	Phase 2	JP	Nippon Shinyaku Co., Ltd.	-