Drug intelligence / Profile preview

deflazacort + clarithromycin

Development stage
Phase 1
Lead developer
Marathon Pharmaceuticals
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, RNA-Targeting Small Molecules → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Deflazacort + clarithromycin is a combination of two pharmaceutical drugs. Deflazacort is a synthetic corticosteroid prodrug that is rapidly converted to its active metabolite, 21-desDFZ, which acts as an agonist at the glucocorticoid receptor to exert anti-inflammatory and immunosuppressive effects. It is primarily used for the treatment of Duchenne muscular dystrophy (DMD)[3][4][5][6]. Clarithromycin is a macrolide antibiotic that inhibits bacterial protein synthesis by binding to domain V of the 23S ribosomal RNA of the 50S subunit in susceptible bacteria, thereby blocking translocation and polypeptide synthesis[2]. Clarithromycin also acts as a strong inhibitor of CYP3A4 and P-glycoprotein. When used together, clarithromycin can significantly increase blood levels of deflazacort’s active metabolite due to inhibition of CYP3A4-mediated metabolism, increasing risk for adverse effects[1][8].

02

Targets

Bacterial 50S ribosomal subunitGR (Glucocorticoid receptor)

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