Drug intelligence / Profile preview

apremilast + clobetasol propionate

Development stage
Preclinical
Lead developer
Bristol Myers Squibb
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Topical
01

Overview

This is a combination therapy consisting of apremilast, an oral small molecule phosphodiesterase 4 (PDE4) inhibitor, and clobetasol propionate, a high-potency topical corticosteroid. Apremilast works by inhibiting PDE4, leading to increased intracellular cAMP levels and downregulation of inflammatory mediators involved in psoriasis and other inflammatory conditions. Clobetasol propionate acts as a potent anti-inflammatory agent by binding to the glucocorticoid receptor and modulating gene expression to suppress inflammation. This combination has been used off-label for the treatment of moderate-to-severe plaque psoriasis when monotherapy is insufficient or in patients with recalcitrant disease. The rationale for combining these agents is to target different pathways in the inflammatory cascade—apremilast systemically modulates immune response while clobetasol provides rapid local symptom control[1][8].

02

Targets

GR (Glucocorticoid receptor)PDE4 (Phosphodiesterase 4A1)

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