Delving into the Latest Updates on Flubendazole with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(5-(4-fluorobenzoyl)-1H-benzimidazole-2-yl)carbamic acid methyl ester, Flubendazole (USAN/INN), methyl 5-(p-fluorobenzoyl)-2-benzimidazolecarbamate

+ [10]

Target-

Mechanism-

Therapeutic Areas

Infectious DiseasesOther DiseasesNeoplasms+ [1]

Active Indication

AscariasisHookworm InfectionsToxocariasis+ [2]

Inactive Indication-

Originator Organization-

Active Organization

Korea University

Johnson & Johnson

Zero Point Five Therapeutics, Inc.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

RegulationOrphan Drug (US)

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Structure

Molecular FormulaC16H12FN3O3

InChIKeyCPEUVMUXAHMANV-UHFFFAOYSA-N

CAS Registry31430-15-6

A Phase 3, Multi-center, Prospective, Randomized, Double-blind, Placebo- Controlled Study to Evaluate the Effectiveness and Safety of ZP5-9676 for the Treatment of Hookworm (Ancylostoma Duodenale and Necator Americanus), Ascaris Lumbricoides, and Trichuris Trichiura in Pediatric and Adult Participants

This is a Phase 3, multi-center, prospective, randomized, double-blind, placebo-controlled study to evaluate the effectiveness, safety, and tolerability of ZP5-9676 compared to placebo for the treatment of STH infections. Approximately 300 participants will be enrolled, randomized at the Baseline visit (Day 1) to one of the following treatments in a 1:1 ratio of active and placebo.

Start Date01 Oct 2024

Sponsor / Collaborator

Zero Point Five Therapeutics, Inc.

PACTR202404505131714 / SuspendedPhase 3

A Phase 3, multi-center, prospective, randomized, double-blind, placebo- controlled study to evaluate the effectiveness and safety of ZP5-9676 for the treatment of Hookworm (Ancylostoma duodenale and Necator americanus), Ascaris lumbricoides, and Trichuris trichiura in pediatric and adult Participants

Start Date17 Jun 2024

Sponsor / Collaborator

Zero Point Five Therapeutics, Inc.

100 Clinical Results associated with Flubendazole

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100 Translational Medicine associated with Flubendazole

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100 Patents (Medical) associated with Flubendazole

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392

Literatures (Medical) associated with Flubendazole

06 Dec 2024·Journal of Biomolecular Structure and Dynamics

Network pharmacology and molecular docking study-based approach to explore mechanism of benzimidazole-based anthelmintics for the treatment of lung cancer

Article

Author: Nidhi ; Khan, Imran A. ; Khan, Mohd Ashif ; Reeta ; Garg, Aakriti ; Karhana, Sonali ; Bano, Aysha

Emerging studies have reported the potential anticancer activity of benzimidazole-based anthelmintics (BBA) against lung cancer (LC). However, mechanism underlying the anticancer activity of BBA is unclear. Therefore, in the current study, network pharmacology and molecular docking-based approach were used to explore the potential molecular mechanism for the treatment of LC. The potential targets for BBA were obtained from multiple databases including SwissTargetPrediction, Drug Bank, Therapeutic Target Database, and Comparative Toxicogenomics Database while LC targets were collected from DisGeNet gene discovery platform, Integrated Genomic Database of NSCLC, Catalogue of Somatic Mutations in Cancer and Online Mendelian Inheritance in Man database. Protein-protein interaction (PPI) diagram of common targets was constructed using STRING online platform. Topological analysis was performed using Cytoscape and gene enrichment analysis was conducted using FunRich software. Highest degree targets were then confirmed using molecular docking and molecular dynamics simulations. The BBA were prioritized according to their S scores, with ricobendazole ranking highest followed by flubendazole, fenbendazole, mebendazole, triclabendazole, albendazole, oxibendazole, parbendazole, thiabendazole and oxfendazole. The potential targets of BBA identified using topological analysis and molecular docking were found to be CCND1 (cyclin D1), EGFR (Epidermal Growth Factor Receptor), ERBB2 (Erb-B2 Receptor Tyrosine Kinase 2/CD340), PTGS2 (Prostaglandin-endoperoxide synthase 2), and SRC (Proto-oncogene tyrosine-protein kinase). Furthermore, molecular dynamics confirmed that CCND1 and EGFR are the potential targets of ricobendazole for the treatment of LC. BBA can be further explored as a therapeutic strategy for the treatment of lung cancer under in vitro and in vivo studies.Communicated by Ramaswamy H. Sarma.

01 Nov 2024·Journal of Cellular and Molecular Medicine

Repurposing flubendazole for glioblastoma ferroptosis by affecting xCT and TFRC proteins

Article

Author: Cen, Wu ; Liu, Jian ; Teng, Wei ; Zhang, Hongzhi ; Chu, Liangzhao ; Zhou, Xingwang ; Jiang, Lishi ; Long, Niya ; Ling, Yuanguo

AbstractNew uses of old drugs hold great promise for clinical translation. Flubendazole, an FDA‐approved antiparasitic drug, has been shown to target p53 and promote apoptosis in glioblastoma (GBM) cells. However, its damaging mechanism in GBM remains elusive. Herein, we explored the ferroptosis‐inducing ability of flubendazole on GBM cells. After treating glioma cell lines U251 and LN229 with the flubendazole (DMSO <1‰), cell viability was inhibited in a concentration‐dependent manner (IC50 for LN229 = 0.5331 μM, IC50 for U251 = 0.6809 μM), attributed to the induction of ferroptosis, as evidenced by increased MDA levels, accumulation of ROS and lipid peroxides, change in mitochondrial membrane potential and structure. Protein analysis related to ferroptosis showed upregulation of TFRC, DMT1 and p53, alongside downregulation of xCT, FHC and GPX4 (p < 0.05). All‐atom docking studies demonstrated that flubendazole bound closely with xCT, and TFRC, validating its role in inducing glioma ferroptosis via modulation of these proteins. Notably, flubendazole could damage the glioblastoma stem cells (GSC) that are typically resistant to other therapies, thereby possessing advantages in stopping glioma recurrence. This study delved into the mechanisms of flubendazole‐induced ferroptosis in glioma, broadening its application and providing new ideas for new uses of other old drugs.

01 Jul 2024·Environmental Monitoring and Assessment

Surface water monitoring of chemicals associated with animal husbandry in an agricultural region in the Netherlands using passive sampling

Article

Author: Roex, Erwin ; Beeltje, Henry ; Rakonjac, Nikola

AbstractCompounds originating from animal husbandry can pollute surface water through the application of manure to soil. Typically, grab sampling is employed to detect these residues, which only provides information on the concentration at the time of sampling. To better understand the emission patterns of these compounds, we utilized passive samplers in surface water to collect data at eight locations in a Dutch agricultural region, during different time intervals. As a passive sampler, we chose the integrative-based Speedisk® hydrophilic DVB. In total, we targeted 46 compounds, among which 25 antibiotics, three hormones, nine antiparasitics, and nine disinfectants. From these 46 compounds, 22 compounds accumulated in passive samplers in amounts above the limit of quantification in at least one sampling location. Over the 12-week deployment period, a time integrative uptake pattern was identified in 53% of the examined cases, with the remaining 47% not displaying this behavior. The occurrences without this behavior were primarily associated with specific location, particularly the most upstream location, or specific compounds. Our findings suggest that the proposed use of passive samplers, when compared in this limited context to traditional grab sampling, may provide enhanced efficiency and potentially enable the detection of a wider array of compounds. In fact, a number of compounds originating from animal husbandry activities were quantified for the first time in Dutch surface waters, such as flubendazole, florfenicol, and tilmicosine. The set-up of the sampling campaign also allowed to distinguish between different pollution levels during sampling intervals on the same location. This aspect gains particular significance when considering the utilization of different compounds on various occasions, hence, it has the potential to strengthen ongoing monitoring and mitigation efforts.

100 Deals associated with Flubendazole

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External Link

KEGG	Wiki	ATC	Drug Bank
D04200	Flubendazole	P02CA05	DB08974

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Ascariasis	-	Johnson & Johnson	-
Hookworm Infections	-	Johnson & Johnson	-
Toxocariasis	-	Johnson & Johnson	-

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Ascariasis	Phase 3	GH	Zero Point Five Therapeutics, Inc.	01 Oct 2024
Ascariasis	Phase 3	BR	Zero Point Five Therapeutics, Inc.	01 Oct 2024
Hookworm Infections	Phase 3	BR	Zero Point Five Therapeutics, Inc.	01 Oct 2024
Hookworm Infections	Phase 3	GH	Zero Point Five Therapeutics, Inc.	01 Oct 2024
Trichuriasis	Phase 3	BR	Zero Point Five Therapeutics, Inc.	01 Oct 2024
Trichuriasis	Phase 3	GH	Zero Point Five Therapeutics, Inc.	01 Oct 2024
HER2 Positive Breast Cancer	Preclinical	KR	Korea University	01 Jul 2017