Drug intelligence / Profile preview

methylprednisolone aceponate

Development stage
Approved
Lead developer
Bayer HealthCare Pharmaceuticals
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Topical
01

Overview

Methylprednisolone aceponate is a synthetic glucocorticoid and corticosteroid ester, specifically the C17α propionate and C21 acetate diester of methylprednisolone. It is primarily used as a topical medication for the treatment of corticosteroid-responsive dermatoses, including atopic dermatitis (eczema), allergic contact eczema, and psoriasis. The drug acts by binding to intracellular glucocorticoid receptor in skin cells; its principal metabolite, 6α-methylprednisolone-17-propionate, also binds these receptors after ester cleavage in the skin. This receptor complex modulates gene expression to induce synthesis of macrocortin (which inhibits arachidonic acid release), suppresses inflammatory mediators such as prostaglandins and leukotrienes, inhibits cytokine synthesis (immunosuppressive effect), and reduces vasodilation through multiple mechanisms. Methylprednisolone aceponate is available in various topical formulations—cream, ointment, fatty ointment, emulsion/lotion—to tailor therapy to individual patient needs.

Brand names
AdvantanAvancort
Other names
methylprednisolone acetate propionatemethylprednisolone 17α-propionate 21-acetate
02

Targets

GR (Glucocorticoid receptor)

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