Drug intelligence / Profile preview

diflucortolone valerate

Development stage
Phase 1
Lead developer
Bayer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Topical
01

Overview

Diflucortolone valerate is a potent topical corticosteroid used primarily in dermatology for the treatment of corticosteroid-responsive acute and chronic skin diseases. It exhibits anti-inflammatory, antipruritic (anti-itch), and vasoconstrictive properties. The drug acts by binding to the glucocorticoid receptor, inducing the production of lipocortins (phospholipase A2 inhibitory proteins), which inhibit the release of arachidonic acid—a precursor to inflammatory mediators. Additionally, it modulates gene expression by stimulating anti-inflammatory genes and suppressing proinflammatory genes such as cytokines and growth factors. Diflucortolone valerate is typically formulated as a cream or ointment at concentrations of 0.1% or 0.3%, with its main indication being short-term topical management of inflammatory skin conditions. Developed by Schering and now manufactured by Bayer, it is used for dermatological conditions. It should not be used for more than four weeks continuously due to risk of systemic absorption and hypothalamic-pituitary-adrenal axis suppression.

Brand names
NerisoneNeriderm
Other names
diflucortolone valerateジフルコルトロン
02

Targets

GR (Glucocorticoid receptor)PLA2 (Phospholipase A2 group IID)

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