adriforant   Click here for help

GtoPdb Ligand ID: 8985

Synonyms: PF 3893787 | PF-03893787 | ZPL-389 | ZPL-3893787 | ZPL389 | ZPL3893787
Immunopharmacology Ligand
Compound class: Synthetic organic
Comment: Adriforant (ZPL-3893787) was a clinical stage immunomodulatory compound being developed by Ziarco Pharma (a Novartis subsidiary). Mechanistically it is a selective histamine H4 receptor antagonist. Novartis announced in their second-quarter financial report of 2020, that they were terminating the adriforant development programme.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 6
Hydrogen bond donors 3
Rotatable bonds 5
Topological polar surface area 79.1
Molecular weight 262.19
XLogP 1.61
No. Lipinski's rules broken 0
SMILES / InChI / InChIKey
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Canonical SMILES CNC1CCN(C1)c1cc(NCC2CC2)nc(n1)N
Isomeric SMILES CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N
InChI InChI=1S/C13H22N6/c1-15-10-4-5-19(8-10)12-6-11(17-13(14)18-12)16-7-9-2-3-9/h6,9-10,15H,2-5,7-8H2,1H3,(H3,14,16,17,18)/t10-/m1/s1
InChI Key ISBHYKVAFKTATD-SNVBAGLBSA-N
No information available.
Summary of Clinical Use Click here for help
ZPL-3893787 reached Phase 2 clinical trial for evaluation as an antiinflammatory agent in patients with plaque psoriasis (see NCT02618616), and a Phase 1 in atopic dermatitis has been completed. Although the compound was better than placebo at reducing eczema symptoms such as inflammation in a phase 2a study for moderate-severe atopic dermatitis, it failed to meet an itch-related endpoint. Novartis terminated their ZPL-3893787 programme in mid-2020.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Allergic inflammation is reported to be augmented via histamine H4 receptor activation [1]. In light of this H4 receptor antagonists would be expected to inhibit this effect,
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT02618616 A Study to Determine the Efficacy of ZPL-3893787 in Subjects With Plaque Psoriasis Phase 2 Interventional Ziarco Pharma Ltd