Drug intelligence / Profile preview

mapracorat

Development stage
Phase 3
Lead developer
Bausch & Lomb
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Ophthalmic, Topical
01

Overview

Mapracorat is a selective glucocorticoid receptor agonist (SEGRA) developed as a non-steroidal anti-inflammatory drug. It binds with high affinity and selectivity to the human glucocorticoid receptor, exerting potent anti-inflammatory effects while displaying reduced transactivation of genes associated with side effects typical of classical glucocorticoids. Mapracorat has been investigated primarily for topical use in the treatment of atopic dermatitis, eczema, inflammation following cataract surgery, allergic conjunctivitis, and other ocular or skin inflammatory diseases. Its mechanism involves partial attenuation of the classical NF-κB pathway and unique upregulation of RelB in the alternative NF-κB pathway, as well as augmentation of MAPK phosphatase 1 (MKP-1), contributing to its anti-inflammatory profile with potentially improved safety compared to traditional steroids[1][3][4][5][6][8].

Other names
ZK-245186ZK245186ZK 245186BOL-303242XBOL303242XBOL 303242X
02

Targets

GR (Glucocorticoid receptor)

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