Calcium ionophore A23187 induced time and concentration dependent pro‐duction of immunoreactive leukotriene (LT) B4 by equine heparinized whole blood in vitro. Time dependent production of immunoreactive LTB4 by equine neutrophils and immunoreactive LTC4 by equine eosinophils in vitro was also demonstrated. The 5‐lipoxygenase activating protein (FLAP) inhibitors, BAY X 1005 and BAY Y 1015, produced concentration dependent inhibition of ionophore‐induced LTB4 synthesis by equine whole blood (mean ± SEM IC50sn= 5; 6.14 ± 0.28 μm vs. 12.30 ± 0.75 μm for BAY Y 1015 and BAY X 1005, respectively) and neutrophils (mean ± SEM IC50sn= 5; 0.003 ± 0.001 μm vs. 0.045 ± 0.021 μm for BAY Y 1015 and BAY X 1005, respectively) and LTC4 synthesis by equine eosinophils (mean ± SEM IC50sn= 5; 0.0036 ± 0.0002 μm and 0.108 ± 0.023 μm for BAY Y 1015 and BAY X 1005, respectively) in vitro. In all three assays, BAY Y 1015 was more potent than BAY X 1005, and for both compounds much higher concentrations were required to inhibit LT synthesis by whole blood compared to isolated neutrophils and eosinophils. Plasma concentration–time relationships and pharmacokinetic parameters for BAY Y 1015 administered intravenously and orally to six horses at a dosage of 10 mg/kg in a two period cross‐over study were established. The study also evaluated the anti‐inflammatory properties of BAY Y 1015 and its ability to inhibit ex vivo whole blood LTB4 synthesis and in vivo LTB4 synthesis in a tissue cage model of acute inflammation. At this dosage, BAY Y 1015 failed to significantly inhibit immunoreactive LTB4 synthesis or the oedema produced by intradermal injection of the mild irritant, carrageenan.

01 Jun 1997·Inflammation ResearchQ3 · MEDICINE

The efficacy of BAY y 1015 in dextran sulfate model of mouse colitis

Q3 · MEDICINE

Article

Author: Murthy, S. ; Coppola, D. ; Murthy, N. S. ; Wood, D. L.

OBJECTIVE AND DESIGNThere is crucial evidence that leukotrienes are significant mediators of inflammation in inflammatory bowel diseases (IBD). Thus, selective inhibition of leukotriene synthesis is believed to provide a novel approach to therapy of IBD. The aim of the study is to study the efficacy of a potent 5-lipoxygenase activating protein inhibitor (FLAP), BAY y 1015 in a dextran sulfate model of mouse colitis.MATERIALOutbred female mice weighing approximately 25 grams were used to produce acute or chronic colitis by feeding 5% dextran sulfate in drinking water.TREATMENTColitic mice were treated with placebo (3% starch suspension, 0.1 ml. p.o., bid) or BAY y 1015 at 8 or 24 mg/kg, p.o., bid or olsalazine, 150 mg/kg/day, p.o.METHODSEfficacy was determined by measuring daily disease activity index (DAI), quantitative histological scores, qualitative histology and measurement of tissue myeloperoxidase (MPO) and leukotriene B4 (LTB4) levels.RESULTSBAY y 1015 was significantly more effective in improving the qualitative histology, inhibiting the DAI, inflammation scores (37-79%), crypt scores (28-71%), MPO (49-57%) and LTB4 levels (56-63%) compared to placebo treatment at all levels of colitis. The two doses of BAY y 1015 were equipotent in decreasing TLB4 levels. BAY y 1015 was significantly better than olsalazine in two of the three protocols used in this study. In the advanced disease level both doses of BAY y 1015 were equipotent in inhibiting crypt and (28-32%) inflammation scores (34-36%), LTB4 (34-56%) and MPO 41-49%) compared to olsalazine.CONCLUSIONThis study suggests the possibility of investigating the use of this compound for the treatment of human inflammatory bowel diseases.

01 Mar 1996·Arthritis & Rheumatism

The effect of leukotriene synthesis inhibitors in models of acute and chronic inflammation

Article

Author: Eugene D. Medvedeff ; Cheryl L. Nickerson-Nutter

AbstractObjective. To assess the efficacy of leukotriene synthesis inhibitors, alone and in combination with a nonsteroidal antiinflammatory drug, as potential treatments for rheumatoid arthritis (RA), using the mouse air pouch model and the collagen‐induced arthritis (CIA) model.Methods. Two selective leukotriene synthesis inhibitors, Bay x 1005 and Bay y 1015, were compared with zileuton in terms of their ability to decrease exudate volume, cell infiltration, and leukotriene B4 (LTB4) production in response to zymosan injection in the mouse air pouch model. The mouse CIA model was used to assess the effect of leukotriene synthesis inhibitors in a model of chronic inflammation. Bay y 1015 and Bay x 1005, and the cyclooxygenase inhibitor naproxen, were evaluated individually and in combination, for their antiarthritic potency in the mouse CIA model.Results. The results indicate that neither zileuton, Bay x 1005, nor Bay y 1015 inhibited exudate production. All 3 compounds decreased LTB4 levels in the air pouch, with Bay y 1015 being the most effective. Cell infiltration was significantly decreased with Bay x 1005, but the degree of this decrease did not appear to correlate with LTB4 levels. No inhibition of arthritis was observed with any compound administered alone. In contrast, a significant inhibition of CIA was observed in animals that received both naproxen and either Bay y 1015 or Bay x 1005.Conclusion. Inhibitors of both cyclooxygenase and leukotriene synthesis in combination may be a more effective treatment of RA than either class of inhibitors alone.

100 Deals associated with Bay-y-1015

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Indication	Highest Phase	Country/Location	Organization	Date
Asthma	Phase 2	Germany	Bayer AG	-
Colitis, Ulcerative	Phase 2	United States	Bayer AG	-
Rheumatoid Arthritis	Phase 2	United States	Bayer AG	-

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