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ZPL389 + topical corticosteroids + topical calcineurin inhibitors

Development stage
Unknown
Lead developer
Novartis
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Topical
01

Overview

This is a **combination therapy** for atopic dermatitis composed of **ZPL389 (adriforant)**, a once-daily oral small molecule antagonist of the histamine H4 receptor, used together with **topical corticosteroids (TCS)** and **topical calcineurin inhibitors (TCI)**. ZPL389 inhibits histamine-mediated inflammation and pruritus by selectively blocking the histamine H4 receptor, a key component in allergic inflammatory responses. Topical corticosteroids are anti-inflammatory agents acting through glucocorticoid receptor agonism, and topical calcineurin inhibitors (such as tacrolimus and pimecrolimus) are non-steroidal immunomodulators that inhibit T-cell activation and cytokine production by blocking calcineurin phosphatase. This combination is intended for use in moderate to severe atopic dermatitis and was studied in clinical trials focusing on safety and efficacy, particularly for patients inadequately treated with topical agents alone[1][3][5][6].

Other names
adriforantNVP-ZPL389-NXNVP-ZPL-389-NXNVP-ZPL 389-NXPF-03893787PF03893787PF 03893787
02

Targets

GR (Glucocorticoid receptor)CN (Calcineurin)HRH4 (Histamine H4 receptor)

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