LIVIVO - Search results -

Search results

Result 1 - 10 of total 43

Search options

Article ; Online: Novel drugs for the treatment of chronic pruritus.

Pereira, Manuel P / Ständer, Sonja

2018 Volume 27, Issue 12, Page(s) 981–988

Abstract: Introduction: Chronic pruritus (CP) is a multidimensional condition severely affecting the quality ... of the pathophysiology of CP is leading to the development of novel antipruritic drugs.: Areas covered: This paper ... safety of novel drugs, but further studies are necessary to enhance our understanding of the different ...

Abstract	Introduction: Chronic pruritus (CP) is a multidimensional condition severely affecting the quality of life of those affected. Although a multitude of topical and systemic agents are recommended for CP of different origins, the condition often remains refractory to treatment. However, a deeper understanding of the pathophysiology of CP is leading to the development of novel antipruritic drugs. Areas covered: This paper reviews antipruritic therapies in development by gathering data from recently published articles and clinical trials databases. Interleukin-31 antibodies and other biologics, neurokinin-1 receptor antagonists, opioid-receptor agonists/antagonists, TrkA-antagonists, and ileal bile acid transporter inhibitors are discussed. Expert opinion: Clinical trials have rendered promising data on the antipruritic efficacy and safety of novel drugs, but further studies are necessary to enhance our understanding of the different conditions associated with CP. High-quality clinical trial data is necessary for these agents to be approved for the treatment. Basic research should be intensified to identify pathways relevant for CP and to further the development of new specific antipruritic drugs.
MeSH term(s)	Antipruritics/adverse effects ; Antipruritics/pharmacology ; Antipruritics/therapeutic use ; Chronic Disease ; Drug Design ; Humans ; Pruritus/drug therapy ; Pruritus/etiology ; Pruritus/physiopathology ; Quality of Life
Chemical Substances	Antipruritics
Language	English
Publishing date	2018-11-19
Publishing country	England
Document type	Journal Article ; Review
ZDB-ID	1182884-5
ISSN	1744-7658 ; 0967-8298 ; 1354-3784
ISSN (online)	1744-7658
ISSN	0967-8298 ; 1354-3784
DOI	10.1080/13543784.2018.1548606
Database	MEDical Literature Analysis and Retrieval System OnLINE

Full text online

Accessible to users with ZB MED library card

In stock of ZB MED Cologne/Königswinter

Zs.A 3739: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
Jg. 1995 - 2021: Lesesall (2.OG)
ab Jg. 2022: Lesesaal (EG)

Order via subito

This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

Details ▾

Article: Odevixibat: A Novel Bile Salt Inhibitor Treatment for Pruritus in Progressive Familial Intrahepatic Cholestasis.

Flattmann, Farrah E / Mohiuddin, Farhan S / Singh, Anjuni / Tandon, Anamika / Lockett, Stewart J / Hirsch, Jon D / Mosieri, Chizoba N / Kaye, Adam M / Varrassi, Giustino / Ahmadzadeh, Shahab / Shekoohi, Sahar / Kaye, Alan D

Cureus

2024 Volume 16, Issue 3, Page(s) e56886

Abstract: Chronic pruritus is defined as an itch lasting greater than six weeks. It can manifest from a wide ... bile acids play a major role in chronic pruritus. The itching in cholestatic liver disease is worsened ... in some cases, depression. One such disease that results from chronic pruritus is progressive familial ...

Abstract	Chronic pruritus is defined as an itch lasting greater than six weeks. It can manifest from a wide variety of etiologies, as many different substances can act as pruritogens, such as steroids, histamine, progesterone, endogenous opioids, and serotonin. In the setting of cholestatic liver disease, increased bile acids play a major role in chronic pruritus. The itching in cholestatic liver disease is worsened in intensity at night and localized frequently to the palms, soles, knees, and other pressure sites. It can be hard to manage, affecting the quality of sleep and causing irritability, poor attention, and, in some cases, depression. One such disease that results from chronic pruritus is progressive familial intrahepatic cholestasis (PFIC), a group of uncommon hereditary disorders that affects the formation of bile and its outflow from the liver. Previously, the drug ursodeoxycholic acid was used to help manage pruritus or surgical procedures, e.g., partial external biliary diversion or partial internal biliary diversion, to help control complications of the disease. This literature review will discuss three clinical studies covering the effectiveness of odevixibat in treating pruritus in patients with PFIC. Odevixibat (Bylvay) is an oral drug that has been FDA-approved to treat pruritus in patients three months of age and older with PFIC. Odevixibat prevents the reabsorption of bile salts in the intestines, resulting in decreased levels of bile salts via their excretion in stool. Several studies have determined that the drug is well tolerated and provides a nonsurgical, pharmacological treatment alternative for those with PFIC.
Language	English
Publishing date	2024-03-25
Publishing country	United States
Document type	Journal Article ; Review
ZDB-ID	2747273-5
ISSN	2168-8184
ISSN	2168-8184
DOI	10.7759/cureus.56886
Database	MEDical Literature Analysis and Retrieval System OnLINE

Order via subito

Article ; Online: Identification of Dihydrobenzofuran Neolignans as Novel PDE4 Inhibitors and Evaluation of Antiatopic Dermatitis Efficacy in DNCB-Induced Mice Model.

Gu, Chenming / Liu, Jiayuan / Qian, Fei / Yu, Wenchao / Huang, Doudou / Shen, Jingshan / Feng, Chenguo / Chen, Kaixian / Li, Yiming / Jiang, Xiangrui / Xu, Yechun / Zhang, Liuqiang

Journal of medicinal chemistry

2024 Volume 67, Issue 6, Page(s) 4855–4869

Abstract: Atopic dermatitis is a chronic relapsing skin disease characterized by recurrent, pruritic ...

Abstract	Atopic dermatitis is a chronic relapsing skin disease characterized by recurrent, pruritic, localized eczema, while PDE4 inhibitors have been reported to be effective as antiatopic dermatitis agents. 3',4-
MeSH term(s)	Mice ; Animals ; Dermatitis, Atopic/chemically induced ; Dermatitis, Atopic/drug therapy ; Phosphodiesterase 4 Inhibitors/pharmacology ; Phosphodiesterase 4 Inhibitors/therapeutic use ; Dinitrochlorobenzene/pharmacology ; Dinitrochlorobenzene/therapeutic use ; Lignans/pharmacology ; Lignans/therapeutic use ; Tumor Necrosis Factor Inhibitors/pharmacology ; Tumor Necrosis Factor Inhibitors/therapeutic use ; Cytokines/pharmacology ; Skin
Chemical Substances	Phosphodiesterase 4 Inhibitors ; Dinitrochlorobenzene ; Lignans ; Tumor Necrosis Factor Inhibitors ; Cytokines
Language	English
Publishing date	2024-03-15
Publishing country	United States
Document type	Journal Article
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.3c02424
Database	MEDical Literature Analysis and Retrieval System OnLINE

In stock of ZB MED Cologne/Königswinter

Zs.B 151: Show issues			Location: Je nach Verfügbarkeit (siehe Angabe bei Bestand) bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular ab Jg. 2022: Lesesaal (EG)
Zs.MB 1: Show issues

Order via subito

Details ▾
- See ZB MED holdings
- Order with fees

Article ; Online: Characterization of the effects on pruritus by novel treatments for atopic dermatitis.

Bonnekoh, Hanna / Butze, Monique / Metz, Martin

Journal der Deutschen Dermatologischen Gesellschaft = Journal of the German Society of Dermatology : JDDG

2021 Volume 20, Issue 2, Page(s) 150–156

Abstract: ... signaling pathways. Novel drugs target these pathways and have shown rapid and sustained reduction of pruritus ... Each of the novel drugs shows very good effects on pruritus. These data offer hope for an even better and possibly ... contributes to impairment of quality of life. Effective treatment of pruritus should therefore be one ...

Abstract	Chronic pruritus is a common and debilitating symptom in patients with atopic dermatitis and contributes to impairment of quality of life. Effective treatment of pruritus should therefore be one of the main treatment goals in patients with atopic dermatitis. Pathophysiologically, the histamine-independent pruritogens interleukin-31, interleukin-13, and interleukin-4, have been shown to play a major role in atopic dermatitis. All three cytokines can mediate chronic pruritus via Janus kinase 1/2 signaling pathways. Novel drugs target these pathways and have shown rapid and sustained reduction of pruritus in patients with atopic dermatitis in clinical use and in phase II and III clinical trials. Here we summarize the published data on the effects of these drugs on itch parameters such as overall reduction in pruritus intensity and percent of patients with atopic dermatitis achieving a relevant reduction in itch. Each of the novel drugs shows very good effects on pruritus. These data offer hope for an even better and possibly more specific treatment of pruritus in patients with atopic dermatitis in the future. In addition, the different pharmacological approaches give us the chance to learn more about the pathophysiology of pruritus in atopic dermatitis.
MeSH term(s)	Cytokines ; Dermatitis, Atopic/complications ; Dermatitis, Atopic/drug therapy ; Eczema ; Humans ; Pruritus/drug therapy ; Pruritus/etiology ; Quality of Life
Chemical Substances	Cytokines
Language	English
Publishing date	2021-12-27
Publishing country	Germany
Document type	Journal Article ; Review
ZDB-ID	2093479-8
ISSN	1610-0387 ; 1610-0379
ISSN (online)	1610-0387
ISSN	1610-0379
DOI	10.1111/ddg.14678
Database	MEDical Literature Analysis and Retrieval System OnLINE

Full text online

Accessible to users with ZB MED library card

In stock of ZB MED Cologne/Königswinter

Zs.A 6148: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
ab Jg. 2022: Lesesaal (EG)

Order via subito

Details ▾

Article: Lichen Planopilaris Responsive to a Novel Phytoactive Botanical Treatment: A Case Series.

Umar, Sanusi / Kan, Petrina / Carter, Marissa J / Shitabata, Paul / Novosilska, Myroslava

Dermatology and therapy

2022 Volume 12, Issue 7, Page(s) 1697–1710

Abstract: ... Conclusions: Patients with treatment-refractory LPP responded to a novel botanical treatment. To the best ... treatment alternatives.: Methods: Based on our previous success in treating a patient with central ... preparation. Three patients had failed previous treatment with intralesional steroid injections, topical ...

Abstract	Introduction: Lichen planopilaris (LPP) is characterized by chronic scarring alopecia that is progressive and typically refractory to therapy. Current drug treatments are suboptimal and not applicable for long-term use because of the high potential for adverse effects, warranting safer and more effective treatment alternatives. Methods: Based on our previous success in treating a patient with central centrifugal cicatricial alopecia using a topical botanical formulation (Gashee), we reviewed records of four patients with biopsy-proven LPP treated with the topical formulation alone or in combination with its oral preparation. Three patients had failed previous treatment with intralesional steroid injections, topical minoxidil, tacrolimus, and clobetasol. Physical examination and photographic documentation were also used as outcome measures. Treatment duration with the botanical formulations ranged from 6 weeks to 9.5 months. Results: All patients showed overall improvement in surrogate indicators of LPP activity as evidenced by the disappearance of symptoms (pruritus, tenderness, scalp irritation, and hair shedding), improvement in hair growth, and reduction in redness. All reported a high satisfaction level and no adverse effects. Conclusions: Patients with treatment-refractory LPP responded to a novel botanical treatment. To the best of our knowledge, this is the first published report of LPP responding to a plant-based natural treatment. Further evaluation of this treatment in a controlled trial with a larger number of patients is warranted.
Language	English
Publishing date	2022-06-08
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2680284-3
ISSN	2190-9172 ; 2193-8210
ISSN (online)	2190-9172
ISSN	2193-8210
DOI	10.1007/s13555-022-00749-3
Database	MEDical Literature Analysis and Retrieval System OnLINE

Order via subito

Article ; Online: A Novel Method of Steroid Delivery to Improve the Efficacy of Intralesional Injection in Keloid Treatment.

Cho, Mi Yeon / Song, Ahreum / Chung, Kee Yang / Roh, Mi Ryung

Dermatologic surgery : official publication for American Society for Dermatologic Surgery [et al.

2022 Volume 48, Issue 6, Page(s) 631–635

Abstract: Background: Keloids are a chronic disease and cause pain, pruritus, and limitation of motion ... Intralesional corticosteroid injection is the first-line treatment, but its effects can be limited, even ... of the tunneling method over the conventional method for therapeutic effect and side effects in keloid treatment. ...

Abstract	Background: Keloids are a chronic disease and cause pain, pruritus, and limitation of motion. Intralesional corticosteroid injection is the first-line treatment, but its effects can be limited, even with repeated injections. Objective: To investigate the efficacy and safety of a tunneling method of corticosteroid injection compared with conventional intralesional injection. Materials and methods: A retrospective review was conducted of keloid patients treated with intralesional corticosteroid injection by conventional and tunneling methods. Results: A total of 119 cases of keloid were included in the study. Among 78 patients treated with 20 mg/mL triamcinolone, the Investigators' Global Assessment effectiveness score and Observer Scar Assessment Scale (OSAS) score were significantly higher in the tunneling group than the conventional group at 1 month. At 6 months, the tunneling group showed significantly higher effectiveness in the OSAS score than the conventional group. In the tunneling group, the interval between treatments was significantly longer than in the conventional group. The occurrence of side effects was lower in the tunneling method group than in the conventional method group. Conclusion: This study reveals the benefits of the tunneling method over the conventional method for therapeutic effect and side effects in keloid treatment.
MeSH term(s)	Adrenal Cortex Hormones ; Humans ; Injections, Intralesional ; Keloid/surgery ; Sleep Apnea, Obstructive/drug therapy ; Steroids/therapeutic use ; Triamcinolone Acetonide
Chemical Substances	Adrenal Cortex Hormones ; Steroids ; Triamcinolone Acetonide (F446C597KA)
Language	English
Publishing date	2022-03-23
Publishing country	United States
Document type	Journal Article
ZDB-ID	1227586-4
ISSN	1524-4725 ; 1076-0512
ISSN (online)	1524-4725
ISSN	1076-0512
DOI	10.1097/DSS.0000000000003432
Database	MEDical Literature Analysis and Retrieval System OnLINE

In stock of ZB MED Cologne/Königswinter

Zs.A 1212: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
Jg. 1995 - 2021: Lesesall (1.OG)
ab Jg. 2022: Lesesaal (EG)

Order via subito

Details ▾
- See ZB MED holdings
- Order with fees

Article ; Online: Atopic dermatitis: pathomechanisms and lessons learned from novel systemic therapeutic options.

Bieber, T / Paller, A S / Kabashima, K / Feely, M / Rueda, M J / Ross Terres, J A / Wollenberg, A

Journal of the European Academy of Dermatology and Venereology : JEADV

2022 Volume 36, Issue 9, Page(s) 1432–1449

Abstract: ... has allowed treatment strategies to evolve from broad-acting systemic immunosuppressive therapies ... of the pathophysiological mechanisms underlying AD and holds promise for individualized treatment strategies tailored ... Atopic dermatitis (AD) is a chronic, heterogenous, inflammatory skin disorder associated ...

Abstract	Atopic dermatitis (AD) is a chronic, heterogenous, inflammatory skin disorder associated with a high skin-related health burden, typically starting in childhood and often persisting into adulthood. AD is characterized by a wide range of clinical phenotypes, reflecting multiple underlying pathophysiological mechanisms and interactions between genetics, immune system dysregulation and environmental factors. In this review, we describe the diverse cellular and molecular mechanisms involved in AD, including the critical role of T-cell-driven inflammation, primarily via T helper (Th) 2- and Th17-derived cytokines, many of which are mediated by the Janus kinase (JAK) signaling pathway. These local inflammatory processes interact with sensory neuronal pathways, contributing to the clinical manifestations of AD, including itch, pain and sleep disturbance. The recent elucidation of the molecular pathways involved in AD has allowed treatment strategies to evolve from broad-acting systemic immunosuppressive therapies to more targeted agents, including JAK inhibitors and cytokine-specific biologic agents. Evidence from the clinical development of these targeted therapies has reinforced and expanded our understanding of the pathophysiological mechanisms underlying AD and holds promise for individualized treatment strategies tailored to specific AD subtypes.
MeSH term(s)	Cytokines/metabolism ; Dermatitis, Atopic/drug therapy ; Humans ; Immunotherapy ; Pruritus/metabolism ; Skin/metabolism
Chemical Substances	Cytokines
Language	English
Publishing date	2022-05-21
Publishing country	England
Document type	Journal Article ; Review
ZDB-ID	1128828-0
ISSN	1468-3083 ; 0926-9959
ISSN (online)	1468-3083
ISSN	0926-9959
DOI	10.1111/jdv.18225
Database	MEDical Literature Analysis and Retrieval System OnLINE

Full text online

Accessible to users with ZB MED library card

In stock of ZB MED Cologne/Königswinter

Zs.A 3492: Show issues			Location: Je nach Verfügbarkeit (siehe Angabe bei Bestand) bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular Jg. 1995 - 2021: Lesesall (2.OG) ab Jg. 2022: Lesesaal (EG)
Zs.MO 413: Show issues

Order via subito

Details ▾

Article ; Online: Alterations in Brain Neural Network and Stress System in Atopic Dermatitis: Novel Therapeutic Interventions.

Nakagawa, Yutaka / Yamada, Shizuo

The Journal of pharmacology and experimental therapeutics

2023 Volume 385, Issue 2, Page(s) 78–87

Abstract: ... as with some psychiatric disorders and chronic pain. The proposed mechanistic model could lead to development of novel ... may be effective as interventions in the treatment of this condition. ... Atopic dermatitis is a common chronic inflammatory skin disease, with most cases experiencing skin ...

Abstract	Atopic dermatitis is a common chronic inflammatory skin disease, with most cases experiencing skin barrier dysfunction and enhanced allergen entry, accompanied by cytokine production which evokes predominantly type-2-skewed immune responses, itch, and scratching behavior. Although intense itch and excessive scratching behavior affect progression of skin lesions, it is unclear what causes them. Data suggest that scratching behavior stimulates brain dopaminergic reward and habit learning systems, strengthening habitual scratching behavior, while nocturnal scratching behavior presumably increases locus coeruleus-noradrenergic system activity, prompting sleep disturbances. At the early stage of atopic dermatitis, increased cortisol levels, due to hypothalamic-pituitary-adrenal axis overactivation caused by such system stimulation, can induce dorsolateral prefrontal cortex disturbance with reinforcement of habitual scratching behavior and may aggravate type-2-skewed immune responses in the skin. During the later phases, whereas blunted hypothalamic-pituitary-adrenal axis function and the shift of type-2-dominated to type-1-co-dominated inflammation are induced, noradrenergic system overactivation-associated dorsolateral prefrontal cortex disruption is ongoing and responsible for itch cognitive distortion to catastrophize about itch, which leads to a vicious spiral along with habitual scratching behavior and skin lesions. Data are presented in this review indicating that while skin immune system dysfunction initiates pathologic changes in atopic dermatitis, brain neural network and stress system alterations can promote the progression of this condition. It is also suggested that cognitive distortion contributes to pathology in atopic dermatitis as with some psychiatric disorders and chronic pain. The proposed mechanistic model could lead to development of novel medications for slowing or terminating the relentless progression of this disorder. SIGNIFICANCE STATEMENT: Although conventional pharmacological interventions focusing on skin homeostasis and itch occurrence significantly attenuate clinical signs in atopic dermatitis patients, achievement of 100% improvement is less than 40% in several double-blind, randomized, placebo-controlled trials. Our model predicts that itch cognitive distortion, due to dorsolateral prefrontal cortex disturbance, can significantly contribute to the progression of atopic dermatitis and that agents capable of improving brain neural network, stress system, and skin homeostasis may be effective as interventions in the treatment of this condition.
MeSH term(s)	Humans ; Dermatitis, Atopic/drug therapy ; Hypothalamo-Hypophyseal System/pathology ; Pituitary-Adrenal System/pathology ; Pruritus/etiology ; Brain/pathology ; Randomized Controlled Trials as Topic
Language	English
Publishing date	2023-02-24
Publishing country	United States
Document type	Journal Article ; Review
ZDB-ID	3106-9
ISSN	1521-0103 ; 0022-3565
ISSN (online)	1521-0103
ISSN	0022-3565
DOI	10.1124/jpet.122.001482
Database	MEDical Literature Analysis and Retrieval System OnLINE

In stock of ZB MED Cologne/Königswinter

Uf I Zs.40: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
ab Jg. 2022: Lesesaal (EG)

Order via subito

Details ▾
- See ZB MED holdings
- Order with fees

Article: Individual Article: A Novel 3-Step Over-the-Counter Eczema Regimen Improves Eczema Severity, Itch, and Life Quality: Randomized Study.

Hawley, Kristi / Lio, Peter / Nguyen, Thu / Qureshi, Aamir / Emesiani, Christine / Meckfessel, Matthew

Journal of drugs in dermatology : JDD

2023 Volume 22, Issue 10, Page(s) SF388641s21–SF388641s26

Abstract: ... with unpredictable flares of erythema, rash, and pruritus. AD arises from a combination of immune system ... Additionally, mean ItchyQuant scores showed that pruritus was significantly improved from 5.4 at baseline to 2 ... a reduced number of flares, and improved quality of life. J Drugs Dermatol. 2023;22:10(Suppl 2):s21-26. ...

Abstract	Background: Eczema, or atopic dermatitis (AD), is a chronic relapsing skin disease associated with unpredictable flares of erythema, rash, and pruritus. AD arises from a combination of immune system dysregulation and abnormal skin barrier function. Skin barrier support with proper skincare regimens have a central role in management. Methods: This was a multi-center, 12-week in-use study of a skincare regimen in children and adults with mild-to-moderate eczema (6-16) on the Patient-Oriented Eczema Measure (POEM), and ≥2 flares within 3 months prior to screening. The regimen included Itch Relief Gel, Eczema Soothing Lotion, and Flare Relief Cream. Efficacy assessments included POEM, ItchyQuant, Eczema Area and Severity Index (EASI), Quality of Life and digital photography, along with gathering of adverse events and cutaneous tolerability. Results: 34 subjects completed the study. In 12 weeks, mean POEM scores improved from 9.7 to 5.3, and EASI scores improved by 17.9% (P<0.05 vs baseline). Additionally, mean ItchyQuant scores showed that pruritus was significantly improved from 5.4 at baseline to 2.7 at week 12 (P<0.05). The number of flares decreased from 4.2 to 3.2 after 12 weeks of regimen application (P<0.05 vs 12 weeks before baseline). Quality-of-life measures also showed improvement in both children and adults from baseline (P<0.05). There were no related adverse events, the regimen was well tolerated, and participants had positive perceptions of the regimen. Conclusions: 12-week use of this OTC skincare regimen resulted in significant improvements in EASI, POEM, and ItchyQuant scores, a reduced number of flares, and improved quality of life. J Drugs Dermatol. 2023;22:10(Suppl 2):s21-26.
MeSH term(s)	Child ; Adult ; Humans ; Eczema/diagnosis ; Eczema/drug therapy ; Quality of Life ; Pruritus/diagnosis ; Pruritus/drug therapy ; Pruritus/etiology ; Dermatitis, Atopic/diagnosis ; Dermatitis, Atopic/drug therapy ; Dermatitis, Atopic/complications ; Skin ; Emollients ; Nonprescription Drugs ; Severity of Illness Index ; Treatment Outcome
Chemical Substances	Emollients ; Nonprescription Drugs
Language	English
Publishing date	2023-10-06
Publishing country	United States
Document type	Randomized Controlled Trial ; Journal Article
ZDB-ID	2145090-0
ISSN	1545-9616
ISSN	1545-9616
DOI	10.36849/JDD.8641
Database	MEDical Literature Analysis and Retrieval System OnLINE

In stock of ZB MED Cologne/Königswinter

Zs.A 5931: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
Jg. 1995 - 2021: Lesesall (2.OG)
ab Jg. 2022: Lesesaal (EG)

Order via subito

Details ▾
- See ZB MED holdings
- Order with fees

Article ; Online: ME3183, a novel phosphodiesterase-4 inhibitor, exhibits potent anti-inflammatory effects and is well tolerated in a non-clinical study.

Kubota-Ishida, Natsuki / Kaji, Chizuko / Matsumoto, Shogo / Wakabayashi, Tsubasa / Matsuhira, Takashi / Okura, Iori / Cho, Naoki / Isshiki, Satoshi / Kumura, Ko / Tabata, Yuji

European journal of pharmacology

2023 Volume 962, Page(s) 176202

Abstract: ... in a substance P-induced mouse pruritus model. In these in vitro and in vivo studies, ME3183 also significantly ... suppressed skin inflammation in a chronic oxazolone-induced dermatitis model and showed antipruritic effects ... These wide margins demonstrate the effectiveness of ME3183 in treating many inflammatory diseases ...

Abstract	Phosphodiesterase 4 (PDE4) inhibitors are expected to exhibit efficacy against inflammatory diseases due to their broad pharmacological activity. The launched PDE4 inhibitors apremilast, crisaborole, and roflumilast have not exhibited sufficient inhibitory potential due to poor margins of effectiveness and tolerability. In this report, we describe the non-clinical efficacy, brain translocation, and vomit-inducing effects of ME3183 compared with apremilast. ME3183 showed extensive cytokine suppression in vitro studies using human peripheral blood mononuclear cells and T cells. ME3183 also significantly suppressed skin inflammation in a chronic oxazolone-induced dermatitis model and showed antipruritic effects in a substance P-induced mouse pruritus model. In these in vitro and in vivo studies, ME3183 also significantly suppressed cytokines, and focusing on tumor necrosis factor-α as a psoriasis-related cytokine and interleukin-4 as an atopic dermatitis-related cytokine, ME3183 potently inhibited both cytokines. ME3183 showed in vivo efficacy at lower doses than apremilast. The brain distribution of ME3183 was sufficiently low in mice and rats. The effective dose of ME3183 for emesis was similar to that of apremilast in ferrets. Given its high-potency inhibitory effects, ME3183 would have a wide margin of efficacy and tolerability. These wide margins demonstrate the effectiveness of ME3183 in treating many inflammatory diseases, such as psoriasis and atopic dermatitis. An on-going phase 2 trial is expected to further demonstrate the efficacy and safety of ME3183.
MeSH term(s)	Animals ; Mice ; Humans ; Rats ; Phosphodiesterase 4 Inhibitors/pharmacology ; Phosphodiesterase 4 Inhibitors/therapeutic use ; Dermatitis, Atopic/drug therapy ; Cyclic Nucleotide Phosphodiesterases, Type 4 ; Leukocytes, Mononuclear ; Ferrets ; Psoriasis/pathology ; Cytokines ; Inflammation/drug therapy ; Anti-Inflammatory Agents/therapeutic use
Chemical Substances	Phosphodiesterase 4 Inhibitors ; Cyclic Nucleotide Phosphodiesterases, Type 4 (EC 3.1.4.17) ; apremilast (UP7QBP99PN) ; Cytokines ; Anti-Inflammatory Agents
Language	English
Publishing date	2023-11-22
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	80121-5
ISSN	1879-0712 ; 0014-2999
ISSN (online)	1879-0712
ISSN	0014-2999
DOI	10.1016/j.ejphar.2023.176202
Database	MEDical Literature Analysis and Retrieval System OnLINE

Full text online

Accessible to users with ZB MED library card

In stock of ZB MED Cologne/Königswinter

Zs.A 522: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
Jg. 1995 - 2021: Lesesall (1.OG)
ab Jg. 2022: Lesesaal (EG)

Order via subito

Details ▾

To top

Full text online

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

More links

Kategorien

Order via subito

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

Full text online

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

More links

Kategorien

Order via subito

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

Full text online

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

Full text online

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito