Literature DB >> 2164070

Pharmacologic and clinical effects of lonapalene (RS 43179), a 5-lipoxygenase inhibitor, in psoriasis.

A K Black1, R D Camp, A I Mallet, F M Cunningham, M Hofbauer, M W Greaves.   

Abstract

The pharmacologic and clinical effects of the 5-lipoxygenase inhibitor, lonapalene, have been determined in a double-blind, placebo-controlled, topical study in ten volunteers with psoriasis. A statistically significant clinical improvement was seen in lesions treated with 2% lonapalene ointment as compared with vehicle-treated sites. Although there was a statistically significant reduction in the levels of material similar or identical to the chemoattractant arachidonate 5-lipoxygenase product, leukotriene B4, in skin chamber fluid samples from lonapalene versus vehicle treated lesions, no significant reduction in arachidonic acid or 12-hydroxy-5,8,10,14-eicosatetraenoic acid was seen. The reduction in leukotriene B4 equivalents occurred before significant clinical improvement in lesions was seen. This and the selectivity of the pharmacologic response suggest that the therapeutic effect of topical lonapalene in psoriasis might be related to inhibition of leukotriene B4 synthesis. These results support the view that 5-lipoxygenase inhibitors may be useful in the treatment of psoriasis, and that leukotriene B4 is a relevant mediator of the pathology of this disease.

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Year:  1990        PMID: 2164070     DOI: 10.1111/1523-1747.ep12873300

Source DB:  PubMed          Journal:  J Invest Dermatol        ISSN: 0022-202X            Impact factor:   8.551


  5 in total

1.  CGS 22745: a selective orally active inhibitor of 5-lipoxygenase.

Authors:  E Kimble; T Kowalski; D White; A Raychauduri; G Pastor; H Chertock; W Lee; R Neale; A Hamdan; J Wasley
Journal:  Agents Actions       Date:  1991-09

2.  The design and synthesis of second generation leukotriene B4 (LTB4) receptor antagonists related to SC-41930.

Authors:  T D Penning; S W Djuric; S H Docter; S S Yu; D Spangler; C P Anglin; D J Fretland; J F Kachur; R H Keith; B S Tsai
Journal:  Agents Actions       Date:  1993

3.  Pharmacokinetics and pharmacodynamics of the leukotriene B4 receptor antagonist CP-105,696 in man following single oral administration.

Authors:  T E Liston; M J Conklyn; J Houser; K D Wilner; A Johnson; G Apseloff; C Whitacre; H J Showell
Journal:  Br J Clin Pharmacol       Date:  1998-02       Impact factor: 4.335

Review 4.  Leukotriene B4 and platelet-activating factor in human skin.

Authors:  L Michel; L Dubertret
Journal:  Arch Dermatol Res       Date:  1992       Impact factor: 3.017

5.  Percutaneous absorption and metabolism of lonapalene in psoriatic skin.

Authors:  P A Lehman; R V Tomlinson; J I Johnson; J E Olerud; W A Akers; T J Franz
Journal:  Pharm Res       Date:  1992-09       Impact factor: 4.200

  5 in total

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