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Apremilast

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https://www.readbyqxmd.com/read/28638635/crystal-structure-of-an-apremilast-ethanol-hemisolvate-hemihydrate-solvatomorph
#1
Yun-Deng Wu, Xiao-Hong Liu, Jian Xu, Si-Han Zhang, Kun Shen, Ling Sun, Yong-Mei He, Yan Ma, Ai-Hua Zhang
The title compound, C22H24N2O7S·0.5C2H5OH·0.5H2O {systematic name: (S)-4-acetamido-2-[1-(3-eth-oxy-4-meth-oxy-phen-yl)-2-(methyl-sulfon-yl)eth-yl]iso-indo-line-1,3-dione ethanol hemisolvate hemihydrate}, is a novel solvatomorph of apremilast (AP), which is an inhibitor of phosphodiesterase 4 (PDE4) and is indicated for the treatment of adult patients with active psoriatic arthritis. The asymmetric unit contains one mol-ecule of AP and disordered mol-ecules of ethanol and water, both with half occupancy. The dihedral angle between the planes of the phenyl ring and the iso-indole ring is 67...
June 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28619562/apremilast-treatment-of-atopic-dermatitis-and-other-chronic-eczematous-dermatoses
#2
Michael Abrouk, Benjamin Farahnik, Tian Hao Zhu, Mio Nakamura, Rasnik Singh, Kristina Lee, Sara-Marian Lucking, Jessin Blossom, Wilson Liao, John Koo, Tina Bhutani, Kanade Shinkai, Tien Nguyen
No abstract text is available yet for this article.
July 2017: Journal of the American Academy of Dermatology
https://www.readbyqxmd.com/read/28617319/pde4-inhibition-and-inflammatory-bowel-disease-a-novel-therapeutic-avenue
#3
REVIEW
Marco Spadaccini, Silvia D'Alessio, Laurent Peyrin-Biroulet, Silvio Danese
BACKGROUND: In the last few decades, a better knowledge of the inflammatory pathways involved in the pathogenesis of Inflammatory Bowel Disease (IBD) has promoted biological therapy as an important tool to treat IBD patients. However, in spite of a wider spectrum of biological drugs, a significant proportion of patients is unaffected by or lose their response to these compounds, along with increased risks of infections and malignancies. For these reasons there is an urgent need to look for new pharmacological targets...
June 15, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28597182/apremilast-a-novel-oral-treatment-for-psoriasis-and-psoriatic-arthritis
#4
REVIEW
Tiago Torres, Luis Puig
Psoriasis is a chronic immune-mediated disease associated with several co-morbidities and negative impacts on a patient's quality of life. Despite the advances in biologic therapy, there are still unmet needs in the treatment of psoriasis, as current treatments are limited in terms of long-term efficacy, tolerability, safety, route of administration, and cost. Apremilast is an oral, small-molecule phosphodiesterase 4 inhibitor that works intracellularly by blocking the degradation of cyclic adenosine 3',5'-monophosphate, resulting in increased intracellular cyclic adenosine 3',5'-monophosphate levels in phosphodiesterase 4-expressing cells...
June 8, 2017: American Journal of Clinical Dermatology
https://www.readbyqxmd.com/read/28581873/budget-impact-model-in-moderate-to-severe-psoriasis-vulgaris-assessing-effects-of-calcipotriene-and-betamethasone-dipropionate-foam-on-per-patient-standard-of-care-costs
#5
Carl V Asche, Minchul Kim, Steven R Feldman, Panagiotis Zografos, Minyi Lu
AIMS: To develop a budget impact model (BIM) for estimating the financial impact of formulary adoption and uptake of calcipotriene and betamethasone dipropionate (C/BD) foam (0.005%/0.064%) on the costs of biologics for treating moderate-to-severe psoriasis vulgaris in a hypothetical US healthcare plan with 1 million members. METHODS: This BIM incorporated epidemiologic data, market uptake assumptions, and drug utilization costs, simulating the treatment mix for patients who are candidates for biologics before (Scenario #1) and after (Scenario #2) the introduction of C/BD foam...
June 19, 2017: Journal of Medical Economics
https://www.readbyqxmd.com/read/28554321/phosphodiesterase-4-inhibitors-in-immune-mediated-diseases-mode-of-action-clinical-applications-current-and-future-perspectives
#6
Lazaros I Sakkas, Athanasios Mavropoulos, Dimitrios P Bogdanos
Phosphodiesterase (PDE) 4 is a superfamily of enzymes that catalyze the hydrolysis of cyclic adenosine 3',5'-monophosphate (cAMP), an intracellular second messenger and regulator of a wide array of genes and proteins. Increased levels of intracellular cAMP lead to activation of genes but also to inhibition of nuclear factor-kappa B, involved in pro-inflammatory responses. By increasing cAMP levels, PDE4 inhibitors, such as apremilast, reduced production of pro-inflammatory TNFα, IFNγ, and IL-17 and increased production of anti-inflammatory IL-10 in lipopolysaccharide-stimulated peripheral blood mononuclear cells, and in patients with psoriatic arthritis (PsA)...
May 29, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28543445/psoriasis-in-those-planning-a-family-pregnant-or-breast-feeding-the-australasian-psoriasis-collaboration
#7
REVIEW
Marius Rademaker, Karen Agnew, Megan Andrews, Katherine Armour, Chris Baker, Peter Foley, John Frew, Kurt Gebauer, Monisha Gupta, Debra Kennedy, Gillian Marshman, John Sullivan
The Australasian Psoriasis Collaboration has reviewed the evidence for managing moderate to severe psoriasis in those who are pregnant or are breast-feeding, or planning a family. The severity of the psoriasis, associated comorbidities and specific anti-psoriasis treatment, along with other exposures, can have a deleterious effect on pregnancy outcomes. Psoriasis itself increases the risk of preterm and low birthweight babies, along with spontaneous and induced abortions, but no specific birth defects have been otherwise demonstrated...
May 23, 2017: Australasian Journal of Dermatology
https://www.readbyqxmd.com/read/28537861/use-of-an-oral-phosphodiesterase-4-inhibitor-apremilast-for-the-treatment-of-chronic-severe-atopic-dermatitis-a-case-report
#8
Benjamin Farahnik, Kourosh Beroukhim, Mio Nakamura, Michael Abrouk, Tian Hao Zhu, Rasnik Singh, Kristina Lee, Tina Bhutani, John Koo, Wilson Liao
Atopic dermatitis (AD) is a common inflammatory dermatosis characterized by pruritus, erythema, induration, and lichenification. Current treatment options for generalized atopic dermatitis are limited and have potentially serious adverse effects, especially in patients with severe, chronic AD who frequently require systemic anti-inflammatory agents. Apremilast, an oral phosphodiesterase-4 inhibitor, was FDA approved in September 2014 for the treatment of moderate-to-severe plaque psoriasis. However, its upstream anti-inflammatory effects, ease of use as an oral agent, and mild side-effect profile make it an interesting treatment option for AD as well...
May 15, 2017: Dermatology Online Journal
https://www.readbyqxmd.com/read/28535721/short-and-long-term-management-of-an-acute-pustular-psoriasis-flare-a-case-report
#9
Jorge R Georgakopoulos, Arvin Ighani, Jensen Yeung
BACKGROUND: Generalised pustular psoriasis (GPP) and acrodermatitis continua of Hallopeau (ACH) are chronic, relapsing variants of pustular psoriasis proven to be remarkably challenging to treat. Due to their uncommon presentation, there are few described cases in literature and scarce evidence for management. Further information is needed to help dermatologists formulate treatment plans for patients presenting with such diseases. CASE SUMMARY: We report the case of a 68-year-old man with a 3-year history of psoriasis presenting to our clinic with a severe breakout of GPP and associated ACH...
May 1, 2017: Journal of Cutaneous Medicine and Surgery
https://www.readbyqxmd.com/read/28522043/apremilast-in-the-treatment-of-moderate-to-severe-hidradenitis-suppurativa-a-case-series-of-9-patients
#10
Patrizia Weber, S Morteza Seyed Jafari, Nikhil Yawalkar, Robert E Hunger
No abstract text is available yet for this article.
June 2017: Journal of the American Academy of Dermatology
https://www.readbyqxmd.com/read/28499587/the-phosphodiesterase-4-inhibitor-apremilast-inhibits-th1-but-promotes-th17-responses-induced-by-6-sulfo-lacnac-slan-dendritic-cells
#11
Stephanie Oehrl, Hridayesh Prakash, Annette Ebling, Nina Trenkler, Priscila Wölbing, Anja Kunze, Thomas Döbel, Marc Schmitz, Alexander Enk, Knut Schäkel
BACKGROUND: The phosphodiesterase 4 (PDE4) inhibitor apremilast increases cellular cAMP levels and has proven effective in the treatment of psoriasis and psoriasis arthritis. We recently described 6-sulfo LacNAc dendritic cells (slanDCs) as immature DCs in blood and as a subset of inflammatory dermal DCs in psoriasis with a pronounced capacity to produce proinflammatory cytokines and to program Th17/Th1 T cell responses. OBJECTIVE: The aim of this study was to investigate possible immune regulatory effects of the PDE4 inhibitor apremilast on slanDCs...
April 20, 2017: Journal of Dermatological Science
https://www.readbyqxmd.com/read/28493709/rh-duanphos-catalyzed-asymmetric-hydrogenation-of-%C3%AE-acetylamino-vinylsulfides-an-approach-to-chiral-%C3%AE-acetylamino-sulfides
#12
Wenchao Gao, Hui Lv, Xumu Zhang
Rh/DuanPhos-catalyzed asymmetric hydrogenation of challenging β-acetylamino vinylsulfides has been developed, affording chiral β-acetylamino sulfides with high yields and excellent ee's (up to 99% ee). This novel methodology provides an efficient and concise synthetic route to chiral β-acetylamino sulfides. The potential utility of this protocol in the synthesis of Apremilast has also been disclosed.
May 11, 2017: Organic Letters
https://www.readbyqxmd.com/read/28481664/beyond-monotherapy-a-systematic-review-on-creative-strategies-in-topical-therapy-of-psoriasis
#13
Karina Koo, Caleb Jeon, Tina Bhutani
The largest proportion of psoriasis patients are candidates for topical treatment rather than treatment paradigms encompassing systemic, biologic and apremilast, and phototherapy, making skillfulness with topical therapy of paramount importance. As such, numerous studies have been conducted to demonstrate the benefits of using topical therapy in combination with other therapies. In addition, innovative uses of otherwise conventional methods, such as proactive use to minimize flare, have been developed. This article reviews five types of strategies for improved efficacy from topical agents beyond monotherapy...
June 6, 2017: Journal of Dermatological Treatment
https://www.readbyqxmd.com/read/28455829/a-novel-apremilast-nail-lacquer-formulation-for-the-treatment-of-nail-psoriasis
#14
Avadhesh Singh Kushwaha, Michael A Repka, S Narasimha Murthy
The objective was to prepare a novel nail lacquer formulation to improve the ungual and trans-ungual delivery of apremilast for the potential treatment of nail psoriasis. Nail lacquer formulation was prepared using Eudragit® S 100 as a film-forming polymer and the mixture of ethanol, ethyl acetate, and water as a solvent system. As a result of high-throughput screening studies, dexpanthenol and salicylic acid were found to be the potential penetration enhancers. After 7 days of in vitro studies, the cumulative amount of apremilast delivered by the nail lacquer formulation across the nail plate was found to be ~3-fold (0...
April 28, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28454058/identification-and-characterization-of-process-related-substances-and-degradation-products-in-apremilast-process-optimization-and-degradation-pathway-elucidation
#15
Yuting Lu, Xiaoyue Shen, Taijun Hang, Min Song
This study aims at investigating the separation, identification and characterization of related substances in apremilast by LC-MS hyphenated techniques, as well as the synthesis optimization and the degradation pathways elucidation. Forced degradation studies were conducted under the ICH prescribed stress conditions. The chromatographic separation was achieved on XBridge C18 column (4.6mm×150mm, 3.5μm) using a mobile phase consisting of water adjusted to pH 3.0 with formic acid as solvent A and acetonitrile as solvent B in linear gradient elution program...
April 2, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28449227/apremilast-for-a-psoriasis-patient-with-hiv-and-hepatitis-c
#16
Shivani P Reddy, Vidhi V Shah, Jashin J Wu
A 46-year old male with HIV, hepatitis C, and moderate psoriasis was resistant to starting ultra violet B phototherapy due to scheduling issues. The patient had 8% body surface area (BSA) affected on the dorsal hands, elbows, and legs, did not have associated psoriatic arthritis, and had not tried any systemic therapy in the past. He was initiated on an apremilast starter pack (dosages titrated up from 10 mg to 30 mg over the course of one week) and maintained on 30 mg twice a day after one week. This article is protected by copyright...
April 27, 2017: Journal of the European Academy of Dermatology and Venereology: JEADV
https://www.readbyqxmd.com/read/28443317/novel-use-of-apremilast-for-adjunctive-treatment-of-recalcitrant-pyoderma-gangrenosum
#17
Mary E Laird, Lana X Tong, Kristen I Lo Sicco, Randie H Kim, Shane A Meehan, Andrew G Franks
No abstract text is available yet for this article.
May 2017: JAAD Case Reports
https://www.readbyqxmd.com/read/28416342/long-term-safety-and-tolerability-of-apremilast-in-patients-with-psoriasis-pooled-safety-analysis-for-%C3%A2-156%C3%A2-weeks-from-2-phase-3-randomized-controlled-trials-esteem-1-and-2
#18
Jeffrey Crowley, Diamant Thaçi, Pascal Joly, Ketty Peris, Kim A Papp, Joana Goncalves, Robert M Day, Rongdean Chen, Kamal Shah, Carlos Ferrándiz, Jennifer C Cather
BACKGROUND: Randomized, controlled trials demonstrated efficacy and safety of apremilast for moderate-to-severe plaque psoriasis and psoriatic arthritis. OBJECTIVE: Assess long-term safety of oral apremilast in psoriasis patients. METHODS: Safety findings are reported for 0 to ≥156 weeks from the Efficacy and Safety Trial Evaluating the Effects of Apremilast in Psoriasis (ESTEEM) 1 and 2. RESULTS: The 0 to ≥156-week apremilast-exposure period included 1184 patients treated twice daily with apremilast 30 mg (1902...
April 14, 2017: Journal of the American Academy of Dermatology
https://www.readbyqxmd.com/read/28400896/treatment-of-recalcitrant-erosive-oral-lichen-planus-and-desquamative-gingivitis-with-oral-apremilast
#19
Mohn'd AbuHilal, Scott Walsh, Neil Shear
BACKGROUND: Erosive oral lichen planus and desquamative gingivitis are uncommon but severe debilitating variants of oral lichen planus. Treatment of these presentations is difficult and challenging. MAIN OBSERVATION: A 44-year-old woman was referred to the dermatology clinic with chronic painful lichen planus-related gingivitis and buccal erosions. She has failed multiple treatments including topical clobetasol and tacrolimus, intralesional corticosteroids and several systemic and immunosuppressive agents...
November 30, 2016: Journal of Dermatological Case Reports
https://www.readbyqxmd.com/read/28391657/apremilast-an-oral-phosphodiesterase-4-inhibitor-in-the-treatment-of-japanese-patients-with-moderate-to-severe-plaque-psoriasis-efficacy-safety-and-tolerability-results-from-a-phase-2b-randomized-controlled-trial
#20
Mamitaro Ohtsuki, Yukari Okubo, Mayumi Komine, Shinichi Imafuku, Robert M Day, Peng Chen, Rosemary Petric, Allan Maroli, Osamu Nemoto
Apremilast, an oral, small-molecule phosphodiesterase 4 inhibitor, works intracellularly within immune cells to regulate inflammatory mediators. This phase 2b randomized, placebo-controlled study evaluated efficacy and safety of apremilast among Japanese patients with moderate to severe plaque psoriasis. In total, 254 patients were randomized to placebo, apremilast 20 mg b.i.d. (apremilast 20) or apremilast 30 mg b.i.d. (apremilast 30) through week 16; thereafter, all placebo patients were re-randomized to apremilast 20 or 30 through week 68...
April 9, 2017: Journal of Dermatology
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