Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C26H24N4O5 |
| Molecular Weight | 472.4926 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CNC1=NC2=C(C=C(OC)C(OC)=C2)C(=N1)C3=CC=CC(NC(=O)C4=CC=C(C=C4)C(=O)OC)=C3
InChI
InChIKey=BBTFKAOFCSOZMB-UHFFFAOYSA-N
InChI=1S/C26H24N4O5/c1-27-26-29-20-14-22(34-3)21(33-2)13-19(20)23(30-26)17-6-5-7-18(12-17)28-24(31)15-8-10-16(11-9-15)25(32)35-4/h5-14H,1-4H3,(H,28,31)(H,27,29,30)
E-6005 is a novel PDE4 inhibitor developed as a topical agent for atopic dermatitis (AD). It potently and selectively inhibited human PDE4 activity and suppressed the production of various cytokines from human lymphocytes and monocytes. In mice models, the topical application of E6005 produced an immediate antipruritic effect as well as an anti-inflammatory effect with reduced expression of cytokines/adhesion molecules. E-6005 increases the cutaneous concentration of cAMP to relieve dermatitis-associated itching. E-6005 may be a promising novel therapeutic agent with antipruritic activity for the treatment of AD. E-6005 is currently in phase 2 development for patients with mild-to-moderate atopic dermatitis.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Antipruritic effect of the topical phosphodiesterase 4 inhibitor E6005 ameliorates skin lesions in a mouse atopic dermatitis model. | 2013 Jul |
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| Antipruritic mechanisms of topical E6005, a phosphodiesterase 4 inhibitor: inhibition of responses to proteinase-activated receptor 2 stimulation mediated by increase in intracellular cyclic AMP. | 2014 Dec |
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| Effect of the phosphodiesterase 4 inhibitor E6005 on nerve growth factor elevation in irritated skin of NC/Nga mice. | 2014 Dec |
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| Safety and efficacy of topical E6005, a phosphodiesterase 4 inhibitor, in Japanese adult patients with atopic dermatitis: results of a randomized, vehicle-controlled, multicenter clinical trial. | 2014 Jul |
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| Topical E6005, a novel phosphodiesterase 4 inhibitor, attenuates spontaneous itch-related responses in mice with chronic atopy-like dermatitis. | 2014 May |
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| Hematocrit-independent recovery is a key for bioanalysis using volumetric absorptive microsampling devices, Mitra™. | 2015 |
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| Validation of a UPLC-MS/MS method for the simultaneous determination of E6005, a phosphodiesterase 4 inhibitor, and its metabolite in human plasma. | 2015 Aug 15 |
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| An inhaled phosphodiesterase 4 inhibitor E6005 suppresses pulmonary inflammation in mice. | 2015 Dec 5 |
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| A putative antipruritic mechanism of the phosphodiesterase-4 inhibitor E6005 by attenuating capsaicin-induced depolarization of C-fibre nerves. | 2015 Mar |
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| Safety, tolerability and pharmacokinetics of a novel phosphodiesterase inhibitor, E6005 ointment, in healthy volunteers and in patients with atopic dermatitis. | 2016 |
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| Effect of topical phosphodiesterase 4 inhibitor E6005 on Japanese children with atopic dermatitis: Results from a randomized, vehicle-controlled exploratory trial. | 2016 Aug |
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| Efficacy of a novel phosphodiesterase inhibitor, E6005, in patients with atopic dermatitis: An investigator-blinded, vehicle-controlled study. | 2016 Oct |
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| Topical E6005/RVT-501, a novel phosphodiesterase 4 inhibitor, for the treatment of atopic dermatitis. | 2017 Dec |
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| A dried blood spot assay with UPLC-MS/MS for the simultaneous determination of E6005, a phosphodiesterase 4 inhibitor, and its metabolite in human blood. | 2018 Aug 5 |
|
| Pharmacokinetic disposition of topical phosphodiesterase-4 inhibitor E6005 in patients with atopic dermatitis. | 2019 Aug |
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100000181118
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24864553
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947620-48-6
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ACTIVE MOIETY
