Drug intelligence / Profile preview

deflazacort + rifampin

Development stage
Phase 1
Lead developer
Marathon Pharmaceuticals
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Deflazacort + rifampin is a combination of two pharmaceutical agents. Deflazacort is a synthetic corticosteroid prodrug that is rapidly converted in the body to its active metabolite, 21-desDFZ. This metabolite acts as an agonist at the glucocorticoid receptor and exerts anti-inflammatory and immunosuppressive effects. Deflazacort is primarily indicated for the treatment of Duchenne muscular dystrophy (DMD) in patients aged 5 years and older[2][5][8]. Rifampin is an antibiotic belonging to the rifamycin class; it inhibits bacterial DNA-dependent RNA polymerase and is used mainly for treating tuberculosis and as prophylaxis against *Neisseria meningitidis*[1]. When administered together, there are significant pharmacokinetic interactions—rifampin strongly induces CYP3A4 enzymes, which markedly reduces exposure to deflazacort’s active metabolite (by up to 90%), potentially leading to loss of efficacy[2][4][6].

Brand names
RifadinRimactane
02

Targets

rpoB (DNA-directed RNA polymerase subunit beta)GR (Glucocorticoid receptor)RNAP (Bacterial dna-dependent RNA polymerase)

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