نتایج جستجو برای: fingolimod

تعداد نتایج: 1102  

2016
Hisanao Akiyama Yu Suzuki Daisuke Hara Kensuke Shinohara Hana Ogura Masashi Akamatsu Yasuhiro Hasegawa

INTRODUCTION Generally, fingolimod administration is simply discontinued when fingolimod-associated macular edema (ME) appears, and the majority of cases are said to recover spontaneously. However, to the best of our knowledge, this is the 1st report regarding improvement of ME without discontinuation of fingolimod administration. CASE PRESENTATION The patient was a 66-year-old woman with rel...

2018
Olivier J. David Amy Berwick Nicole Pezous Michael Lang Klaus Tiel‐Wilck Tjalf Ziemssen Peng Li Hisanori Hara Robert Schmouder

The safety profile of fingolimod 0.5 mg, approved therapy for relapsing multiple sclerosis, is well established in clinical and real-world studies. As fingolimod is teratogenic in rats, it was considered important to assess the concentrations of fingolimod and its active metabolite, fingolimod-phosphate, in the semen of male patients on treatment and the risk of harming a fetus in a pregnant pa...

Journal: :Journal of clinical pharmacology 2009
John M Kovarik Kiran Dole Gilles-Jacques Riviere Francoise Pommier Steve Maton Yi Jin Kenneth C Lasseter Robert L Schmouder

The sphingosine-1-phosphate receptor modulator fingolimod is predominantly hydroxylated by cytochrome CYP4F2. In vitro experiments showed that ketoconazole significantly inhibited the oxidative metabolism of fingolimod by human liver microsomes and by recombinant CYP4F2. The authors used ketoconazole as a putative CYP4F2 inhibitor to quantify its influence on fingolimod pharmacokinetics in heal...

2016
Chihiro Fujii Takayuki Kondo Hirofumi Ochi Yoichiro Okada Yuichiro Hashi Tetsuya Adachi Masaharu Shin-Ya Sadayuki Matsumoto Ryosuke Takahashi Masanori Nakagawa Toshiki Mizuno

Multiple sclerosis (MS) is a T cell-mediated autoimmune disease. Fingolimod, a highly effective disease-modifying drug for MS, retains CCR7+ central memory T cells in which autoaggressive T cells putatively exist, in secondary lymphoid organs, although relapse may still occur in some patients. Here, we analyzed the T cell phenotypes of fingolimod-treated, fingolimod-untreated patients, and heal...

Journal: :Current neurology and neuroscience reports 2011
Matthias Mehling Ludwig Kappos Tobias Derfuss

The oral sphingosine 1-phosphate receptor (S1PR) modulator fingolimod functionally antagonizes S1PR hereby blocking lymphocyte egress from secondary lymphoid organs to the peripheral blood circulation. This results in a reduction in peripheral lymphocyte counts, including potentially encephalitogenic T cells. In patients with relapsing multiple sclerosis fingolimod has been shown to be an effec...

2014
Nelleke Snelder Bart A. Ploeger Olivier Luttringer Donald. R. Stanski Meindert Danhof

A complicating factor in the translational pharmacology of sphingosine 1-phosphate agonists is that they exert their pharmacological effect through their respective phosphate metabolites, which are formed by the enzyme sphingosine kinase (S1PHK). In this investigation, we present a semimechanistic pharmacokinetic model for the interconversion of S1PHK substrates and their respective phosphates ...

Journal: :Drug metabolism and disposition: the biological fate of chemicals 2011
Markus Zollinger Hans-Peter Gschwind Yi Jin Claudia Sayer Frédéric Zécri Stefan Hartmann

Fingolimod [(FTY720), Gilenya; 2-amino-2-[2-(4-octylphenyl)ethyl]-1,3-propanediol], a new drug for the treatment of relapsing multiple sclerosis, acts through its phosphate metabolite, which modulates sphingosine 1-phosphate receptors. This represents a novel mechanism of action. In the present work, the absorption and disposition of (14)C-labeled fingolimod were investigated in healthy male vo...

Multiple sclerosis (MS) is an autoimmune disease which affects myelin in the central nervous system (CNS) and leads to serious disability. Currently available treatments for MS mainly suppress the immune system. Regenerative medicine-based approaches attempt to increase myelin repair by targeting endogenous progenitors or transplanting stem cells or their derivatives. Fingolimod exerts anti-inf...

2014
Jorge Correale Erwin Chiquete Snezana Milojevic Nadina Frider Imre Bajusz

BACKGROUND Fingolimod is a once-daily oral treatment for relapsing multiple sclerosis, the proprietary production processes of which are tightly controlled, owing to its susceptibility to contamination by impurities, including genotoxic impurities. Many markets produce nonproprietary medicines; assessing their efficacy and safety is difficult as regulators may approve nonproprietary drugs witho...

Journal: :Journal of natural products 2011
Cherilyn R Strader Cedric J Pearce Nicholas H Oberlies

Fingolimod (Gilenya; FTY720), a synthetic compound based on the fungal secondary metabolite myriocin (ISP-I), is a potent immunosuppressant that was approved (September 2010) by the U.S. FDA as a new treatment for multiple sclerosis (MS). Fingolimod was synthesized by the research group of Tetsuro Fujita at Kyoto University in 1992 while investigating structure-activity relationships of derivat...

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