Literature DB >> 30265585

Pharmacokinetic disposition of topical phosphodiesterase-4 inhibitor E6005 in patients with atopic dermatitis.

Yasumi Kitahara1,2, Seiichiro Hojo3, Maiko Nomoto4, Daisuke Onozuka2, Masutaka Furue5, Akihito Hagihara2.   

Abstract

Background: A novel topical phosphodiesterase-4 inhibitor E6005 shows potential as effective treatment option for atopic dermatitis (AD); however, systemic exposure may cause potentially undesirable adverse reactions. In this study, we evaluated the relationship between the systemic exposure of E6005 and clinical parameters including skin condition and the incidence of AEs in patients with AD.
Methods: The association analysis used the clinical data obtained in a previously conducted clinical study with topical E6005 in adult patients with AD. To estimate associations with drug exposure, generalized estimating equation logistic regression models were used, along with clinical data and plasma concentrations of M11, the major metabolite of E6005 (as an indicator for E6005 exposure).
Results: The metabolite M11 was detected in 62 of 221 plasma samples from 72 subjects. From association analysis, SCORAD-A obtained prior to E6005 treatment was identified as the clinical parameter influenced to M11 detection with statistical significance (p = .003). M11 detection was not clearly associated with the incidence of adverse events occurred.
Conclusion: Exposure to topical E6005 is associated with the eczema-associated area, however, that is not distinctly associated with its adverse drug reactions occurred after drug applications possibly due to E6005's characteristics of tissue distribution.

Entities:  

Keywords:  Atopic dermatitis; E6005; RVT-501; phosphodiesterase-4

Mesh:

Substances:

Year:  2018        PMID: 30265585     DOI: 10.1080/09546634.2018.1530439

Source DB:  PubMed          Journal:  J Dermatolog Treat        ISSN: 0954-6634            Impact factor:   3.359


  2 in total

1.  DRM02, a novel phosphodiesterase-4 inhibitor with cutaneous anti-inflammatory activity.

Authors:  David W C Hunt; Iordanka A Ivanova; Lina Dagnino
Journal:  Tissue Barriers       Date:  2020-06-01

2.  New and Emerging Therapies for Pediatric Atopic Dermatitis.

Authors:  Henry L Nguyen; Katelyn R Anderson; Megha M Tollefson
Journal:  Paediatr Drugs       Date:  2019-08       Impact factor: 3.930

  2 in total

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