Uses
A related intermediate of Prednisolone (P703740).
Biological Activity
Vamorolone, a synthetic steroid, is an orally available dissociative steroid with anti-inflammatory efficacy. It is a partial agonist of the glucocorticoid receptor (NR3C1) th at appear to be safe and well tolerated. Also, vamorolone is a potent antagonist of the mineralocorticoid receptor (NR3C2). It is under development for children with Duchenne muscular dystrophy.
in vivo
Vamorolone (5-30 mg/kg; cherry syrup) shows a superior side effect profile compared to pharmacological glucocorticoids in mdx mice[1].
Vamorolone (30 mg/kg; orally; daily for 20 days) reduces CNS Inflammation in murine experimental autoimmune encephalomyelitis[2].
| Animal Model: | C57BL/6 mice (experimental autoimmune encephalomyelitis)[2] |
| Dosage: | 30 mg/kg |
| Administration: | Orally; daily for 20 days (starting one day prior to MOG 33-55 peptide immunization and continuing) |
| Result: | Reduced CNS inflammation in murine experimental autoimmune encephalomyelitis. |
Toxics Screening Level
The ITSL for 17, 21-dihydroxy-16 alpha-methylpregna-1,4,9 (11)-triene-3, 20-dione has been changed from 0.04 μg/m3 to 0.1 μg/m3 based on annual averaging time.
