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tofacitinib citrate

Serena Gianfaldoni, Georgi Tchernev, Uwe Wollina, Maria Grazia Roccia, Massimo Fioranelli, Jacopo Lotti, Miriam Rovesti, Francesca Satolli, Yan Valle, Andy Goren, Michael Tirant, Mirna Situm, Maja Kovacevic, Katlein França, Torello Lotti
BACKGROUND: Vitiligo is an acquired pigmentary cutaneous disease, characterised by the progressive loss of melanocytes, resulting in hypopigmented skin areas which progressively become amelanotic. Classically, vitiligo treatments are unsatisfactory and challenging. Despite the continuous introduction of new therapies, phototherapy is still the mainstay for vitiligo repigmentation. AIM: The aim of this multicenter observational retrospective study was to evaluate the efficacy and safety of the nb - UVB micro - phototherapy (BIOSKIN EVOLUTION®), used alone or in associations with an oral Janus kinase inhibitor (Tofacitinib citrate), in the treatment of stable or active forms of localised vitiligo...
January 25, 2018: Open Access Macedonian Journal of Medical Sciences
Chieyeon Chough, Misuk Joung, Sunmin Lee, Jaemin Lee, Jong Hoon Kim, B Moon Kim
A series of 3(R)-aminopyrrolidine derivatives were designed and synthesized for JAK1-selective inhibitors through the modification of tofacitinib's core structure, (3R,4R)-3-amino-4-methylpiperidine. From the new core structures, we selected (R)-N-methyl-N-(pyrrolidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine as a scaffold for further SAR studies. From biochemical enzyme assays and liver microsomal stability tests, (R)-3-(3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)-3-oxopropanenitrile (6) was chosen for further in vivo test through oral administration...
February 3, 2018: Bioorganic & Medicinal Chemistry
(no author information available yet)
No abstract text is available yet for this article.
December 1, 2017: Rheumatology
Xiao Wu, Xuefang Zeng, Lei Wang, Taijun Hang, Min Song
A specific LC-MS method was developed for separation, identification and characterization of the process-related substances and degradation products in tofacitinib citrate. The separation was achieved on a LiChrospher C18 column (250mm×4.6mm, 5μm) by linear gradient elution of 0.1% ammonium acetate solution (pH adjusted to 4.0 by formic acid) and acetonitrile at a flow rate of 1.0mL/min. Forced degradation studies were conducted under hydrolytic (acidic, basic), oxidative, photolytic and thermal stress conditions as described in ICH...
September 5, 2017: Journal of Pharmaceutical and Biomedical Analysis
Matthew D Vesely, Suguru Imaeda, Brett A King
No abstract text is available yet for this article.
January 2017: JAAD Case Reports
S Lam
Pfizer's Xeljanz (tofacitinib citrate) was the first Janus kinase (JAK) inhibitor to reach the market for rheumatoid arthritis (RA) following its U.S. approval in November 2012, and it has since gained approval in more than 45 countries as a second-line therapy for RA after failure of disease-modifying antirheumatic drugs (DMARDs). This emerging category has heralded an attractive new class of oral treatment options in RA, with a notable opportunity in patients who stop responding to DMARDs, but they are facing a challenging market...
August 2016: Drugs of Today
Milène Kennedy Crispin, Justin M Ko, Brittany G Craiglow, Shufeng Li, Gautam Shankar, Jennifer R Urban, James C Chen, Jane E Cerise, Ali Jabbari, Mårten C G Winge, M Peter Marinkovich, Angela M Christiano, Anthony E Oro, Brett A King
BACKGROUND: Alopecia areata (AA) is an autoimmune disease characterized by hair loss mediated by CD8+ T cells. There are no reliably effective therapies for AA. Based on recent developments in the understanding of the pathomechanism of AA, JAK inhibitors appear to be a therapeutic option; however, their efficacy for the treatment of AA has not been systematically examined. METHODS: This was a 2-center, open-label, single-arm trial using the pan-JAK inhibitor, tofacitinib citrate, for AA with >50% scalp hair loss, alopecia totalis (AT), and alopecia universalis (AU)...
September 22, 2016: JCI Insight
A K Gupta, J L Carviel, W Abramovits
BACKGROUND: Autoimmune-triggered non-scarring hair loss is a feature of alopecia areata (AA). Initially patchy and often self-limited, severe hair loss forms include the complete loss of scalp hair or alopecia totalis (AT) and complete loss of all hair or alopecia universalis (AU). For AT and AU a reliable treatment has remained elusive. The targeted kinase inhibitor tofacitinib, in current use for treatment of other immune diseases, has been hypothesized as a viable option for AA, AT and AU therapy and a few case reports support this...
August 2016: Journal of the European Academy of Dermatology and Venereology: JEADV
Drew J B Kurtzman, Natalie A Wright, Janice Lin, Alisa N Femia, Joseph F Merola, Mital Patel, Ruth Ann Vleugels
No abstract text is available yet for this article.
August 1, 2016: JAMA Dermatology
Ali Jabbari, Nhan Nguyen, Jane E Cerise, Grace Ulerio, Annemieke de Jong, Raphael Clynes, Angela M Christiano, Julian Mackay-Wiggan
No abstract text is available yet for this article.
August 2016: Experimental Dermatology
V Di Lernia, F Bardazzi
The outlook for patients with psoriasis has improved significantly over the last 10 years with the introduction of targeted therapies. Cytokines exert their effects by activating intracellular signaling and transcription pathways, among which there are Janus kinases (JAKs) and signal transducers and activators of transcription (STAT) pathways. JAKs are intracellular second messengers that are crucial for transmitting extracellular cytokine signals to the cell. JAK inhibition interrupts intracellular signaling and can suppress immune cell activation and inflammation in T-cell-mediated disorders, such as psoriasis...
2016: Drug Design, Development and Therapy
Arjun Dhayalan, Brett A King
No abstract text is available yet for this article.
April 2016: JAMA Dermatology
Lauren L Levy, Jennifer Urban, Brett A King
BACKGROUND: Treatment of moderate to severe atopic dermatitis (AD) is often inadequate. OBJECTIVE: We sought to evaluate the efficacy of the oral Janus kinase inhibitor tofacitinib citrate in the treatment of moderate to severe AD. METHODS: Six consecutive patients with moderate to severe AD who had failed standard treatment were treated with tofacitinib citrate. Response to treatment was assessed using the Scoring of AD index. RESULTS: Decreased body surface area involvement of dermatitis and decreased erythema, edema/papulation, lichenification, and excoriation were observed in all patients...
September 2015: Journal of the American Academy of Dermatology
Brittany G Craiglow, Brett A King
IMPORTANCE: Vitiligo is a common condition that is often emotionally devastating for patients. At present, no reliably effective treatments are available. OBSERVATIONS: Recent advances in the understanding of the pathogenesis of vitiligo suggest that Janus kinase inhibitors may be a therapeutic option. We report a case of generalized vitiligo for which treatment with tofacitinib citrate, an oral Janus kinase 1/3 inhibitor, resulted in significant repigmentation...
October 2015: JAMA Dermatology
Takuma Harada, Hiroyuki Nakamura
No abstract text is available yet for this article.
September 2014: Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica
Philip B Meadow, Jacqueline Nguyen, Keerthana Kesavarapu
Purpose. To report a case of a patient with rheumatoid arthritis (RA) treated with tofacitinib citrate. Methods. Observational case report. Results. A 59-year-old patient, with a history of rheumatoid arthritis, on methotrexate 10 mg PO qwk and IV abatacept 750 mg/month, presented with photosensitivity, foreign body sensation, pain, redness, and blurry vision of her right eye (RE). Visual acuity of the RE was 20/200 and 20/20 of the left eye (LE). The slit lamp examination of the RE revealed dryness, 2+ injection of the conjunctiva, and pericentral ulceration of the cornea with 20-30% stromal thinning, pannus, and diffuse punctate epithelial erosions...
2014: Case Reports in Rheumatology
Daniel A Hussar, Nicholas J Hurrey
No abstract text is available yet for this article.
January 2013: Journal of the American Pharmacists Association: JAPhA
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