Drug intelligence / Profile preview

clofazimine + corticosteroids

Development stage
Unknown
Lead developer
Novartis
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

Clofazimine + corticosteroids is a combination therapy used primarily in the management of leprosy, especially for severe or complicated cases such as lepromatous leprosy and erythema nodosum leprosum (ENL). Clofazimine is a fat-soluble riminophenazine dye with both antimycobacterial and anti-inflammatory properties. It acts by binding to mycobacterial DNA, interfering with bacterial replication, disrupting membrane function through redox cycling and generation of reactive oxygen species (ROS), and inhibiting T-lymphocyte activation via antagonism of potassium channels. Corticosteroids are synthetic analogs of endogenous glucocorticoids that exert potent anti-inflammatory and immunosuppressive effects by modulating gene expression through the glucocorticoid receptor, reducing cytokine production, suppressing immune cell activity, and stabilizing cellular membranes. The combination is often used when monotherapy is insufficient to control inflammatory reactions or complications in leprosy patients[2][3][10].

02

Targets

KCNA3 (Potassium voltage-gated channel subfamily A member 3)GR (Glucocorticoid receptor)

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