| In Vitro | In vitro activity: Deflazacort (also known as MDL 458; trade name: Emflaza) is a glucocorticoid used as an anti-inflammatory and immunosuppressant. It was approved by FDA in 2017 to treat patients age 5 years and older with Duchenne muscular dystrophy (DMD). Deflazacort is an inactive prodrug which is metabolized rapidly to the active drug 21-desacetyldeflazacort. |
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| In Vivo | Deflazacort results in a significant and equal decrease of thymus weight, indicating a marked reduction in total immunogenic tissue in rats. Deflazacort reduces thymus weight and Daily weight gain in rats. Deflazacort lowers liver IFG-I and GHR mRNA in rats. Deflazacort (DFC) is a heterocyclic glucocorticoid with anti-inflammatory activity but with decreased side effects. Deflazacort and [3H]dexamethasone (DEX) similarly induce in vivo ornithine decarboxylase activity in hippocampus and liver, although body weight loss after chronic treatment is significantly less for DFC. Deflazacort induces dose-dependent decreases in osteocalcin (OC) plasma production rate (PPR). Deflazacort and prednisolone increase both postabsorptive plasma glucose and plasma calcium levels in sheep, but there are no significant differences between their effects. Deflazacort, especially combined with L-arginine, spares quadriceps muscle from injury-induced regeneration (myf5 expression) compared with placebo treatment, despite an increase in membrane permeability immediately after exercise. Deflazacort alone prevents the typical progressive loss of function (measured as voluntary distance run over 24 hours) that is observed 3 months later in placebo-treated mice. Deflazacort causes a less significant alteration in the pattern of GH secretion and does not negatively affect the overall amount of GH secreted. |
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| Animal model | Deflazacort results in a significant and equal decrease of thymus weight, indicating a marked reduction in total immunogenic tissue in rats. Deflazacort reduces thymus weight and Daily weight gain in rats. Deflazacort lowers liver IFG-I and GHR mRNA in rats. |
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| Formulation & Dosage | N/A |
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| References | Neuropharmacology. 2012 Jun;62(7):2261-6; Eur J Endocrinol. 1994 Dec;131(6):652-7. |
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