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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
Chris Fellner
Emtricitabine/rilpivirine/tenofovir alafenamide (Odefsey) for combination HIV-1 therapy; dapsone gel, 7.5% (Aczone) for acne vulgaris; extended-release tofacitinib (Xeljanz XR) for rheumatoid arthritis; and brivaracetam (Briviact) for epilepsy.
April 2016: P & T: a Peer-reviewed Journal for Formulary Management
Aditya K Gupta, Deanne Daigle, William Abramovits, Kimberly Dawn Vincent
No abstract text is available yet for this article.
May 2015: Skinmed
Na-Na Wang, Dao-Lin Zhang, Xin-Hui Jiang
A high-performance liquid chromatography (HPLC) method was established to detect Xeljanz enantiomers in active pharmaceutical ingredients (APIs) and tablets. The separation was achieved on a Chiralpak IC column using a mobile phase of hexane-ethanol-diethylamine (65:35:0.1, v/v). The detection wavelength was 289 nm. The peak areas and the enantiomer concentrations in the range of 0.15-2.25 μg•mL(-1) were in high linearity, with correlation coefficients higher than 0.999. The recoveries were 86.44% at the concentrations of 7...
March 2015: Chirality
Takuma Harada, Hiroyuki Nakamura
No abstract text is available yet for this article.
September 2014: Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica
Pierre-Alain Varisco, Alexander So
In the last 15 years, the therapeutical options for the treatment of chronic inflammatory diseases in rheumatology have increased a lot. Nevertheless, some patients do not respond or respond partially to the current therapies--including to the biologics therapy. Tofacitinib (Xeljanz) is now on the Swiss market. It inhibits the JAK pathway. Tofacitinib--as monotherapy or with methotrexate--improves the control of rheumatoid arthritis (RA). In a comparative study, tofacitinib was as effective as adalimumab. Further, tofacitinib reduced structural damages in RA and is considered as an alternative, in case of non-response, to anti-TNF and probably to other biologics therapy...
January 22, 2014: Revue Médicale Suisse
Lesley J Scott
Tofacitinib (Xeljanz(®)) is the first approved drug in a new class of disease modifying antirheumatic drugs (DMARDs), the Janus kinase (JAK) inhibitors. JAKs have a pivotal role in triggering cytokine-induced signal transduction pathways that influence normal and pathological cellular processes of haematopoiesis and immune cell function, including pathogenic mechanisms involved in rheumatoid arthritis (RA). Selective inhibition of JAKs by tofacitinib potentially modulates inflammatory processes and provides a novel approach for the treatment of RA...
June 2013: Drugs
David L Simmons
After two decades of research and development activity focussed on orally active kinase inhibitors, the first such drug (the JAK inhibitor Xeljanz, tofacitinib) was approved by the FDA in November 2012 for the treatment of rheumatoid arthritis (RA). There is an intense activity in many companies both on expanding the utility of JAK inhibitors in other auto-immune indications and in discovering inhibitors of the JAK family with different and more selective profiles. Progress is also being made with orally active Syk inhibitors...
June 2013: Current Opinion in Pharmacology
Brian W Dymock, Cheng Shang See
INTRODUCTION: Janus kinases (JAKs) comprise a family of four enzymes, JAK1, JAK2, JAK3 and tyrosine kinase 2 (TYK2), centrally implicated in cell signaling processes important in cancer and immune-inflammatory diseases. Progression in the field has taken a recent step forward with the approval of ruxolitinib (Jakafi), a selective inhibitor of JAK1/2 and very recently tofacitinib (Xeljanz), a pan-JAK inhibitor. There are many new JAK family enzyme inhibitors in the clinic now with a range of selectivity profiles...
April 2013: Expert Opinion on Therapeutic Patents
(no author information available yet)
No abstract text is available yet for this article.
January 7, 2013: Medical Letter on Drugs and Therapeutics
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