Delving into the Latest Updates on Tirilazad Mesylate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Tirilazad mesylate (USAN), Tirilazad mesylate hydrate

+ [4]

Target-

Action

inhibitors

Mechanism

Lipid peroxidation inhibitors

Therapeutic Areas

Other Diseases

Active Indication

Soft Tissue Injuries

Inactive Indication-

Originator Organization-

Active Organization-

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC38H52N6O2

InChIKeyRBKASMJPSJDQKY-RBFSKHHSSA-N

CAS Registry110101-66-1

View All Structures (2)

BACKGROUNDReperfusion serves as a mainstay therapy in almost all ischemic vascular diseases (IVD), but reperfusion may enhance cell damage after an ischemic period time. Increased ROS and inflammatory markers, decreasing organ function parameters, along with systemic inflammatory response and multi-organ damage may occur in ischemic reperfusion injury (IRI). Unfortunately, this series of events is unpredictable and sudden, causing high mortality in patients with IRI. Due to the significant role of inflammation in IRI, how is the effectiveness of anti-inflammatory agents administered before reperfusion therapy to prevent IRI? To know the efficacy of anti-inflammatory agents administered before reperfusion therapy to prevent IRI.METHODSA systematic search was conducted in databases (Pubmed, EMBASE, Scopus) and was later selected according to predetermined inclusion and exclusion criteria. Studies included later critically appraised using the CEBM Oxford questionnaire for randomized control trials and systematic review.RESULTSSeven studies were included among 1072 studies found in early searching. Six of the studies are randomized control trials, and one is a meta-analysis of randomized control trials. Methylprednisolone, pexelizumab, tirilazad mesylate, and N-acetylcysteine are known anti-inflammatory agents applicable in humans. The highest effectiveness of anti-inflammatory agents is methylprednisolone, with a relative risk reduction (RRR) of 75-85%. Besides that, pexelizumab also had an RRR of 27%, and tirilazad-mesylate had an RRR of 18%. N-acetylcysteine is not effective in preventing IRI. IL-6 levels postoperatively also decreased significantly in patients given anti-inflammatory agents before reperfusion therapy. There are no side effects of the intervention reported.CONCLUSIONAnti-inflammatory agent administration before reperfusion therapy effectively prevents IRI. The choices of anti-inflammatory agents recommended are methylprednisolone, pexelizumab, and tirilazad-mesylate. Anti-inflammatory agent administration before reperfusion therapy is recommended.

01 Jan 2025·Current Microbiology

Evaluation of Tridax procumbens Secondary Metabolites Anti-Tuberculosis Activity by In Vitro and In Silico Methods

Article

Author: Seetharaman, Jayashri ; Muthuraj, M ; Philip, Reya Rene ; Sankari, D ; Priya, R Akshaya

Mycobacterium tuberculosis is a human pathogen that causes Tuberculosis (TB) disease. Researchers have reported the activity of traditional medicinal plants against human pathogens. However, antimycobacterial studies of medicinal plants against M. tuberculosis remain limited. Thus, the purpose of this study is to characterize the phytochemical profile, antibacterial and antimycobacterial activity of Tridax procumbens towards H37Rv. The antibacterial activity was elucidated by the inhibitory zone formed around the disc by performing disk diffusion method. Tridax antimycobacterial activity measured by Microplate Alamar Blue Assay (MABA) infers the sample is sensitive to H37Rv at MIC (minimum inhibitory concentration) 600 µg/mL. BACTEC MGIT 960 DST identifies the sample is susceptible to H37Rv and Rifampicin resistant (RR). Antiproliferative, functional group determination and mechanism of action of secondary metabolites were performed by MTT, Fourier transform infrared spectroscopy (FTIR) and Gas Chromatography-mass spectrometry (GC-MS). The phytocompounds antimycobacterial efficacy is further supported by molecular docking data. The binding interactions of ligands with gyrA gene revealed (S,Z)-Heptadeca-1,9-dien-4,6-diyn-3-ol molecule as a prominent phytocompound with a binding affinity of -6.6 kcal/mol.

01 Sep 2024·Neural Regeneration Research

Nrf2 as a potential target for the treatment of epilepsy

Article

Author: Shekh-Ahmad, Tawfeeq ; Singh, Prince Kumar

A review.In conclusion, the vulnerability of the brain to oxidative stress (OS) holds a pivotal significance in acute neurol. injuries as well as in the initiation and progression of epilepsy conditions.Seizures can induce OS, while chronic OS can contribute to neuronal excitability, inflammation, and neuronal cell loss, all of which contribute to epilepsy.However, the current evidence on the use of antioxidants for epilepsy treatment is limited and has produced mixed results.Clin. trials of vitamin E, N-acetylcysteine, ebselen, and tirilazad have primarily focused on symptomatic treatment of epilepsy rather than investigating their potential for modifying the disease.To achieve significant clin. benefits in chronic and progressive neurol. conditions, such as epilepsy, it is necessary to administer antioxidant therapy at an early stage for a prolonged duration.Nonetheless, another significant challenge in utilizing antioxidants efficiently is their short life and limited BBB permeability.Our previous report suggested that the antioxidant defense system is not homogeneously activated throughout the brain but possibly has a region-specific antioxidant defense, suggesting that most antioxidant-based therapies failed to exhibit prolonged effects in preclin. and clin. investigations.Thus, targeting the Keap1-Nrf2 pathway, a master regulator of antioxidant and anti-inflammatory responses, is a promising therapeutic approach, as revealed in various preclin. investigations.The activation of Nrf2 enhances antioxidant and anti-inflammatory responses and provides neuroprotection.Collectively, these therapeutic strategies for targeting OS via activation of Nrf2 to orchestrate antioxidant and anti-inflammatory responses in epilepsy show exciting avenues, however, further research and strategic clin. trials are required to fully comprehend the relationship between OS and epilepsy to understand and mitigate disease development and progression by validating efficacy and safety to achieve maximum clin. benefits.

100 Deals associated with Tirilazad Mesylate

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External Link

KEGG	Wiki	ATC	Drug Bank
D06168	Tirilazad Mesylate	N07XX01	DB13050

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Soft Tissue Injuries	-	-	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


Pubmed \| Mater Sci Eng C Mater Biol Appl	Not Applicable	-	-	CNSI-DOX	tsmgrqibgk(luumimcjzp) = ggcsqdqxrb nqqjgtgjse (lluftvkpfs )	-	01 Nov 2018
				Free DOX	tsmgrqibgk(luumimcjzp) = wrewjrlljy nqqjgtgjse (lluftvkpfs )