Rapalogues as hCES2A Inhibitors: In Vitro and In Silico Investigations
ConclusionOur findings demonstrate that several marketed rapalogues are potent and specific hCES2A inhibitors, and these agents can serve as leading compounds for the development of more efficacious hCES2A inhibitors to modulate the pharmacokinetic profiles and toxicity of hCES2A-substrate drugs (such as the anticancer agent irinotecan).Graphic Abstract (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - November 2, 2020 Category: Drugs & Pharmacology Source Type: research
Topical Calcineurin Inhibitors and Skin Cancer
For most people with atopic dermatitis, management of their skin disease includes years of continuous or intermittent use of topical medications. Counseling on that element of chronic disease management is a crucial part of physician visits for patients with atopic dermatitis. Inevitably, discussions about the long-term safety of patients ’ treatment plans are included and these discussions are usually based on little long-term evidence. Randomized clinical trials are often underpowered and too short to detect long-term, rare adverse events. Those clinical discussions became more nuanced with the introduction of the topi...
Source: JAMA Dermatology - August 12, 2020 Category: Dermatology Source Type: research
Pediatric mastocytosis
Purpose of review
The current article highlights recent developments in the field of pediatric cutaneous mastocytosis. Mastocytosis is a spectrum of conditions that range from fleetingly benign to aggressively malignant. Through recognizing the natural progression of disease, the role of biomarkers and mutational analysis, treatment and risk of triggers, physicians can confidently stage, counsel and manage patients with pediatric cutaneous mastocytosis.
Recent findings
Many lesions of cutaneous mastocytosis are chronic with some resolving around the mid-teenage years. KIT mutations are found in the majority of pediatr...
Source: Current Opinion in Pediatrics - July 30, 2020 Category: Pediatrics Tags: DERMATOLOGY: Edited by Albert C. Yan Source Type: research
Quercitrin, the Main Compound in Wikstroemia indica, Mitigates Skin Lesions in a Mouse Model of 2,4-Dinitrochlorobenzene-Induced Contact Hypersensitivity.
Authors: Jegal J, Park NJ, Lee SY, Jo BG, Bong SK, Kim SN, Yang MH
Abstract
Hapten-induced contact hypersensitivity (CHS) is widely utilized to induce immune activation in animal models of allergic contact dermatitis. Our previous findings suggested that the 95% EtOH extract of Wikstroemia indica (L.) C. A. Mey. has antiallergic and anti-inflammatory effects in DNCB-treated CHS SKH-1 hairless mice. The aim of this study was to evaluate the protective effects of compounds isolated from the EtOAc fraction of W. indica in RBL-2H3 cells and 2,4-dinitrochlorobenzene- (DNCB-) induced CHS mice. Of eight compounds...
Source: Evidence-based Complementary and Alternative Medicine - July 23, 2020 Category: Complementary Medicine Tags: Evid Based Complement Alternat Med Source Type: research
Pearls in Mitigating Application Pain of Topical Nonsteroidal Agents
Background: Topical steroid-sparing agents (SSA), such as tacrolimus, pimecrolimus, and crisaborole, represent an important therapeutic option in the treatment of inflammatory dermatoses such as atopic dermatitis. While these agents lack the common side effects associated with topical corticosteroids, they all share application site pain as an important adverse effect.Summary: Based on the available evidence and our experience, we suggest the following 7 practical strategies for decreasing the pain associated with SSA use. (1) Use a topical corticosteroid for a few days to reduce inflammation before starting the SSA treatm...
Source: Dermatology - July 13, 2020 Category: Dermatology Source Type: research
Racial and Ethnic Disparities in Access to Emerging and Frontline Therapies in Common Dermatological Conditions: A Cross-Sectional Study.
CONCLUSIONS: This study demonstrates a racial and ethnic disparity in accessing newly approved and standard of care medical therapies for acne, atopic dermatitis, and psoriasis within the past three years.
PMID: 32641259 [PubMed - as supplied by publisher] (Source: Journal of the National Medical Association)
Source: Journal of the National Medical Association - July 11, 2020 Category: General Medicine Tags: J Natl Med Assoc Source Type: research
Crisaborole Ointment, 2%, for Treatment of Patients with Mild-to-Moderate Atopic Dermatitis: Systematic Literature Review and Network Meta-Analysis
ConclusionsCrisaborole was shown to be superior to vehicle and pimecrolimus and comparable to tacrolimus, 0.1% or 0.03%, with respect to ISGA 0/1 at 28 –42 days in patients aged ≥ 2 years with mild-to-moderate AD. This evaluation of comparative efficacy of crisaborole further supports use of crisaborole as an effective therapeutic option in this population. (Source: Dermatology and Therapy)
Source: Dermatology and Therapy - May 19, 2020 Category: Dermatology Source Type: research
Novel therapeutic approaches and targets for treatment of vulvar lichen sclerosus.
CONCLUSION: The available evidence provides useful indications for the management of VLS. Both the identification of new therapeutic targets and the optimization of the available options represent the main objectives of future research.
PMID: 32416670 [PubMed - as supplied by publisher] (Source: Current Pharmaceutical Biotechnology)
Source: Current Pharmaceutical Biotechnology - May 15, 2020 Category: Biotechnology Authors: Borghi A, Corazza M Tags: Curr Pharm Biotechnol Source Type: research
Atopic Dermatitis: Diagnosis and Treatment.
Abstract
Atopic dermatitis (atopic eczema) is a chronic relapsing and remitting inflammatory skin disease affecting one in 10 people in their lifetime. Atopic dermatitis is caused by a complex interaction of immune dysregulation, epidermal gene mutations, and environmental factors that disrupts the epidermis causing intensely pruritic skin lesions. Repeated scratching triggers a self-perpetuating itch-scratch cycle, which can have a significant impact on the patient's quality of life. The American Academy of Dermatology has created simple diagnostic criteria based on symptoms and physical examination findi...
Source: American Family Physician - May 14, 2020 Category: Primary Care Authors: Frazier W, Bhardwaj N Tags: Am Fam Physician Source Type: research
Efficacy and safety of topical calcineurin inhibitors for the treatment of atopic dermatitis: meta-analysis of randomized clinical trials.
Conclusions: Calcineurin inhibitors seem to be more effective and contrarily they elicit more AEs than TCS.
PMID: 31998006 [PubMed] (Source: Advances in Dermatology and Allergology)
Source: Advances in Dermatology and Allergology - February 1, 2020 Category: Dermatology Tags: Postepy Dermatol Alergol Source Type: research
The Utility of A Transcriptomic Signature to Assess Atopic Dermatitis Treatment Outcomes
Previously our group identified a transcriptome signature (89ADGES) which can be used to monitor Atopic Dermatitis (AD) treatment outcomes. Herein, we hypothesized that expression of 89ADGES member genes can be predict treatment outcomes in response to topical corticosteroids (Betamethasone; BC) and calcineurin inhibitors (Pimecrolimus; PC). (Source: Journal of Allergy and Clinical Immunology)
Source: Journal of Allergy and Clinical Immunology - January 31, 2020 Category: Allergy & Immunology Authors: Debayoti Ghosh, Jonathan Bernstein, Tesfaye Mersha Source Type: research
Topical tacrolimus in adult atopic dermatitis: a consensus based on a 15-year experience.
Authors: Calzavara-Pinton P, Fabbrocini G, Girolomoni G, Matiucci A, Micali G, Musumeci ML, Patruno C, Pellacani G, Rossi MT, Stingeni L, Castello M
Abstract
Atopic dermatitis (AD) is one of the most common cutaneous inflammatory diseases both in adults and in children. It is a chronic, remitting-relapsing dermatitis, primarily managed by dermatologists, but also by allergists and primary care physicians. Due to coexistence of comorbidities, often a multidisciplinary team is required. Topical calcineurin inhibitors (TCIs - i.e. tacrolimus and pimecrolimus) are a class of steroid- sparing, anti-inflammatory...
Source: Giornale Italiano di Dermatologia e Venereologia - November 27, 2019 Category: Dermatology Tags: G Ital Dermatol Venereol Source Type: research
Efficacy of the Topical Calcineurin Inhibitors Tacrolimus and Pimecrolimus in the Treatment of Vitiligo in Infants Under 2 Years of Age: A Randomized, Open-Label Pilot Study
ConclusionsTopical tacrolimus ointment 0.03% or pimecrolimus cream 1% have efficacy for vitiligo in infants, which serves to achieve an appropriate level of safety and tolerability during the 6-month period of applications. Thus, TCIs proved to be a therapeutic option for vitiligo in infants under 2 years of age. (Source: Clinical Drug Investigation)
Source: Clinical Drug Investigation - September 13, 2019 Category: Drugs & Pharmacology Source Type: research
Drugs for Psoriasis
Date: June 17, 2019
Issue #:
1574Summary:
Mild to moderate psoriasis can be treated with topical
drugs or with phototherapy. Patients with moderate to
severe disease generally require systemic therapy. (Source: The Medical Letter)
Source: The Medical Letter - April 3, 2019 Category: Drugs & Pharmacology Authors: admin Tags: Acitretin Adalimumab Amjevita apremilast Betamethasone Brenzys brodalumab Calcipotriene calcipotriol Calcitriol Certolizumab Cimzia Cosentyx Cyclosporine Cyltezo Dovobet Dovonex Duobril Elidel Enbrel Enstilar Erel Source Type: research
Topical calcineurin inhibitors in the treatment of oral lichen planus: a systematic review and meta-analysis.
CONCLUSIONS: The evidence for tacrolimus (n=12), pimecrolimus (n=3) and cyclosporine (n=6) demonstrated that TCI may be alternative approaches when OLP does not respond to the standard protocols. Tacrolimus 0.1% should be the first drug of choice in TCI for the short-term treatment in recalcitrant OLP. Further well-designed trials are warranted to evaluate the long-term efficacy and safety of TCI. This article is protected by copyright. All rights reserved.
PMID: 30903622 [PubMed - as supplied by publisher] (Source: The British Journal of Dermatology)
Source: The British Journal of Dermatology - March 21, 2019 Category: Dermatology Authors: Sun SL, Liu JJ, Zhong B, Wang JK, Jin X, Xu H, Yin FY, Liu TN, Chen QM, Zeng X Tags: Br J Dermatol Source Type: research
