This article reviews the mechanisms and potential therapeutic uses of compounds with inhibitory effects on leukotriene B4 (LTB4) production or its activity, and focuses on compounds that have been shown in animal and/or human studies to have potential efficacy in treating dermatological disorders. These compounds, many of which are not familiar to many dermatologists, include inhibitors of 5-lipoxygenase such as ETH615, 15-hydroxyeicosatetraenoic acid, leflunomide, linetastine, lonapalene, MK886, R-68151 and zileuton, and antagonists of LTB4 such as SC53228, SC50605, SC51146 and VML295. The purpose of this paper is to introduce our colleagues to these potentially useful compounds currently in preclinical or early clinical testing.

01 Apr 1997·Ceska a Slovenska farmacie : casopis Ceske farmaceuticke spolecnosti a Slovenske farmaceuticke spolecnosti

[Substances affecting the synthesis and activity of leukotrienes].

Article

Author: Bĕhounková, M ; Opletalová, V ; Hartl, J

Leukotrienes play an important role in inflammation and asthma. This paper briefly deals with compounds influencing leukotriene biosynthesis and activity. 5-Lipoxygenase inhibitors (e.g., zileuton) and FLAP inhibitors (e.g., quiflapon) hinder biosynthesis of all leukotrienes. LTB4 production may be limited by LTA4-hydrolase inhibitors. Attention is also paid to leukotriene receptor antagonists. LTB4 antagonists (e.g., SC-51146) should be useful in the treatment of diseases in which a prominent neutrophil infiltrate is present, especially psoriasis and inflammatory bowel disease. Peptidoleukotriene (LTC4, LTD4, LTE4) antagonists, such as zafirlukast and pranlukast, are currently being developed as antiasthmatics.

01 Sep 1994·Journal of lipid mediators and cell signalling

Phorbol ester-induced dermal inflammation in mice: evaluation of inhibitors of 5-lipoxygenase and antagonists of leukotriene B4 receptor.

Article

Author: Isakson, P C ; Djuric, S W ; Rao, T S ; Yu, S S

In the present investigation, the effects of selective inhibitors of 5-lipoxygenase (5-LO), zileuton and TZI-41127, E-6080, AA-861 and antagonists of leukotriene B4 (LTB4) receptors, SC-41930, and SC-51146 and a selective cyclooxygenase inhibitor, indomethacin, were examined in TPA-induced acute mouse dermal inflammation. Topical application of all these agents, except indomethacin, resulted in marked attenuation of TPA-induced edema and influx of neutrophils reflected in myeloperoxidase measurements. Topically applied SC-41930 attenuated TPA-induced edema and neutrophil influx in a dose-related manner. Oral administration of LTB4 receptor antagonists either as a pre-treatment or post-treatment attenuated TPA-induced edema and influx of neutrophils. The O-demethyl analog of SC-41930, SC-37920, which was nearly 1000-fold less active than SC-41930 in LTB4 receptor binding assays, was inactive in inflammation assays, suggesting a role for LTB4 in this response. Zileuton and TZI-41127 were more effective as anti-inflammatory agents following oral administration than after i.p. administration. Intraperitoneally administered indomethacin attenuated edema response but not influx of neutrophils. Taken together, these results suggest a role for leukotrienes in acute inflammation induced by TPA and possible utility of this model to test in vivo 5-LO inhibitors and LTB4 receptor antagonists.

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Indication	Highest Phase	Country/Location	Organization	Date
Inflammation	Discovery	US	G.D. Searle & Co., Inc.	-

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