Delving into the Latest Updates on Diroleuton with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(8Z,11Z,14Z)-Icosatrienoic acid, (Z,Z,Z)-8,11,14-Eicosatrienoic acid, (Z,Z,Z)-8,11,14-Icosatrienoate

+ [27]

Target

IL-10

Mechanism

IL-10 inhibitors(Interleukin-10 inhibitors)

Therapeutic Areas

Skin and Musculoskeletal Diseases

Active Indication

Acne Vulgaris

Inactive Indication

Alzheimer DiseaseMild Atopic DermatitisModerate Atopic Dermatitis+ [3]

Originator Organization

Suntory Beverage & Food Ltd.

Active Organization

Suntory Beverage & Food Ltd.

Inactive Organization

Dignity Sciences Ltd.

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC20H34O2

InChIKeyHOBAELRKJCKHQD-QNEBEIHSSA-N

CAS Registry1783-84-2

The purpose of this study is to determine whether orally administered DS107 (1g and 2g doses) is effective in the treatment of moderate to severe atopic dermatitis.
Oral DS107 capsules will be administered for 8 weeks and will be compared against placebo.
The study will enroll approximately 300 subjects.

Start Date01 Jan 2017

Sponsor / Collaborator

Dignity Sciences Ltd.

100 Clinical Results associated with Diroleuton

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100 Translational Medicine associated with Diroleuton

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100 Patents (Medical) associated with Diroleuton

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1,264

Literatures (Medical) associated with Diroleuton

30 Sep 2024·Journal of Pharmacopuncture

Antimicrobial and Anti-Inflammatory Potential of Euphorbia paralias (L.): a bioprospecting study with phytoconstituents analysis

Article

Author: Youssef, Ahmed Mohamed Mohamed ; Gaber, Yasser ; Maaty, Doaa Ahmed Mohamed ; Althneibat, Thabet Hasan Ahmad

ObjectivesThe phytochemicals in the aerial parts of Euphorbia paralias (also known as Sea Spurge) and their anti-inflammatory and antimicrobial activities were investigated.MethodsThe methanolic extract was characterized using GC-MS and HPLC techniques. The anti-inflammatory feature was estimated through a Human Red Blood Cell (HRBC) membrane stabilization technique, while the antimicrobial feature was evaluated by the disc diffusion agar technique, minimum bactericidal concentration, and minimum inhibitory concentration (MIC) via micro-broth dilution method.ResultsThe GC/MS results demonstrated the existence of various phytochemicals, such as n-hexadecenoic acid, cis-11-eicosenoic acid, and methyl stearate, recognized for their anti-inflammatory and antibacterial features. The similarity of the phytochemical composition with other Euphorbia species emphasizes the genus-wide similarity. The anti-inflammatory activity exhibited a noteworthy inhibitory effect comparable to the reference drug indomethacin. The extract's antimicrobial potential was tested against a range of microorganisms, demonstrating significant action against Gram-positive bacteria and Candida albicans. The quantification of total phenolics and flavonoids further supported the therapeutic potential of the extract.ConclusionThe methanolic extract from E. paralias emerges as a successful natural source of important active constituents with potential applications as anti-inflammatory and antimicrobial agents. This research provides a first step to valorize Euphorbia paralias insights as a source of worthwhile phytochemicals that have potential applications in the pharmaceutical industry.

01 Sep 2024·Experimental Eye Research

Targeted metabolomic analysis of serum free fatty acids: Lipidomics disturbance in patients with superior limbic keratoconjunctivitis

Article

Author: Wu, Kaili ; Zong, Yan ; Liu, Sihao ; Liu, Xiuping ; Lin, Liping ; Yu, Yubin ; Cheng, Chao

This study aimed to identify and quantify free fatty acids (FFAs), secretory phospholipase A2 group IIa (sPLA2-IIa) and cytosolic phospholipase A2 (cPLA2) in serum of superior limbic keratoconjunctivitis (SLK) patients and explored the association between FFAs, sPLA2-IIa and cPLA2 variations and SLK. Targeted metabolomic analysis of FFAs in serum was performed by gas chromatography tandem mass spectrometry (GC-MS/MS) analysis on 16 SLK patients (43.88 ± 7.88 years; female: 62.50%) and 25 healthy controls (43.12 ± 7.88 years; female: 64.00%). Qualitative and absolute quantitative results of FFAs were obtained and classified according to gender and thyroid tests. Differential lipid metabolites, metabolomic pathways and biomarkers were further evaluated. The serum sPLA2-IIa and cPLA2 were determined by enzyme linked immunosorbent assay (ELISA). Among 40 FFAs identified, 6 FFAs showed significant changes (P < 0.05) in SLK patients, including 4 decreased and 2 increased. They were mainly related to unsaturated fatty acid biosynthesis, α-linolenic acid and linoleic acid metabolism, and fatty acid biosynthesis. When dividing the data by gender or abnormal thyroid tests, some comparable FFAs alterations displayed in SLK patients. The ROC analysis revealed that the AUC values of linoleic acid, γ-linolenic acid, cis-8,11,14-eicosatrienoic acid, stearic acid, and palmitic acid, were all greater than 0.8. The serum concentrations of sPLA2-IIa and cPLA2 in patients with SLK were significantly higher than that in healthy controls. Lipidomics disturbance might be the potential mechanism of SLK. Serum FFA biomarkers associated with SLK have potential for the diagnosis and treatment of the disease.

19 Jul 2024·Alternative therapies in health and medicine

The Mechanism of Jinkui Wenjing Tang in the Treatment of Anovulatory Dysfunctional Uterine Bleeding was Explored Through Network Pharmacology and Molecular Docking Technology.

Article

Author: Weng, Shuangyan ; Chen, Zhi ; Tang, Sisi ; Huang, Yu ; Hu, Renzhi

ObjectivesJinkui Wenjing Tang (JKWJT), a Traditional Chinese Medicine prescription for gynecological menstrual adjustment, is also used to treat continuous uterine bleeding and abdominal pain. However, the mechanism of action, potential targets, and active ingredients of JKWJT in the treatment of anovulatory dysfunctional uterine bleeding (ADUB) remain unknown. Therefore, it is imperative to explore the molecular mechanism of JKWJT.MethodsThe chemical composition and target of JKWJT were obtained by using the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP), and the SwissTargetPrediction website. ADUB-related targets were collected through the GeneCards database. The protein-protein interaction network was constructed from the target protein. Gene Ontology function and Kyoto Encyclopedia of Genes and Genomes pathway enrichment analysis were performed. The binding of the compounds in JKWJT and the potential therapeutic target molecules was verified by molecular docking. Finally, immunohistochemistry, Western Blotting, and qPCR were used for target expression validation within ADUB patient tissues.ResultsThe putative targets of JKWJT for the treatment of ADUB mainly involve ESR1, VEGFA, TNF, AR, OXTR, and PCNA. Functional enrichment analysis showed that the therapeutic effect of JKWJT on ADUB was correlated to response to estradiol, gland development, regulation of hormone levels as well as endocrine resistance, estrogen signaling pathway, HIF-1 signaling pathway, EGFR tyrosine kinase inhibitor resistance, MAPK signaling pathway, prolactin signaling pathway. Molecular docking showed that the target OXTR was expected to have a good binding affinity with 4 corresponding compounds (Girinimbin, icosa-11, 14, 17-trienoic acid methyl ester, Kanzonol F, and Obacunone). After treatment with JKWJT, OXTR relative protein expression and mRNA levels were significantly reduced in ADUB patients.ConclusionIn this study, the basic pharmacological effects, and mechanisms of JKWJT in the treatment of ADUB were elucidated, thus providing a clinical basis for the treatment of ADUB by JKWJT.

100 Deals associated with Diroleuton

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Diroleuton	-	DB00154

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acne Vulgaris	Phase 2	-	Suntory Beverage & Food Ltd.	-
Moderate Atopic Dermatitis	Preclinical	CA	Dignity Sciences Ltd.	01 Jan 2015
Mild Atopic Dermatitis	Discovery	ZA	Dignity Sciences Ltd.	01 Dec 2016
Moderate Atopic Dermatitis	Discovery	US	Dignity Sciences Ltd.	01 Jan 2015
Moderate Atopic Dermatitis	Discovery	CA	Dignity Sciences Ltd.	01 Jan 2015
Moderate Atopic Dermatitis	Discovery	US	Dignity Sciences Ltd.	01 Jan 2015
Severe Atopic Dermatitis	Discovery	CA	Dignity Sciences Ltd.	01 Jan 2015
Severe Atopic Dermatitis	Discovery	US	Dignity Sciences Ltd.	01 Jan 2015
Severe Atopic Dermatitis	Discovery	US	Dignity Sciences Ltd.	01 Jan 2015
Severe Atopic Dermatitis	Discovery	CA	Dignity Sciences Ltd.	01 Jan 2015

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02864498 (CTgov)	Phase 2	Moderate Atopic Dermatitis \| Severe Atopic Dermatitis	321	DS107 (1g DS107)	lxwuypovym(gjbaoplvef) = alumnxrkta euahrnarwi (idcgodsavq, jzgblojvll - biwkvvikax) View more	-	10 Oct 2022
				DS107 (2g DS107)	lxwuypovym(gjbaoplvef) = bvovpbfuqq euahrnarwi (idcgodsavq, hmtigjorpy - hrelqhuvtw) View more
NCT02925793 (CTgov)	Phase 2	Alzheimer Disease \| Moderate Atopic Dermatitis \| Mild Atopic Dermatitis	327	Vehicle cream (Vehicle Cream)	hmmxwzpuha(dryniukppg) = kxgcuoicdh poklvdaspz (cmpgudjauz, safisuyyky - ttsgtufniq) View more	-	07 Oct 2022
				DS107 (1% DS107 Cream)	hmmxwzpuha(dryniukppg) = djabchpjce poklvdaspz (cmpgudjauz, ycrqoeunrx - zpnoqnjazz) View more
NCT02211417 (CTgov)	Phase 2	Moderate Atopic Dermatitis \| Severe Atopic Dermatitis	102	Placebo (Placebo)	ggjmhhftem(zsspxvrkww) = pqsejdouua kyarwhmxgl (xqrxnjddrm, qttzthqfiq - tglvcdlsci) View more	-	07 Oct 2022
				Oral DS107 (Oral DS107 2g)	ggjmhhftem(zsspxvrkww) = dmgdtoucto kyarwhmxgl (xqrxnjddrm, zymtspwtcv - yyhgkvoohu) View more
NCT03817190 (CTgov)	Phase 2	Moderate Atopic Dermatitis \| Severe Atopic Dermatitis	219	Placebo	qjfchsoifd(pqlygwfwck) = avpkijuyis grnzcanvis (jbculakztg, zhusnxkwse - wvtvvhpnkh) View more	-	06 May 2022
ISC2020	Not Applicable	Acute Ischemic Stroke	111	Dihomo-gamma-linolenic acid (DHLA)	rbsljiwycw(xangkadfrh) = sjibhirnpm zjzmyshcjn (inbbujebtz ) View more	-	01 Feb 2020
				Control group (without DHLA)	rbsljiwycw(xangkadfrh) = wrwolspmgt zjzmyshcjn (inbbujebtz ) View more