Deflazacort

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Deflazacort
Clinical data
AHFS/Drugs.comInternational Drug Names
Routes of
administration
Oral
ATC code
Pharmacokinetic data
Protein binding40%
MetabolismBy plasma esterases, to active metabolite
Elimination half-life1.1–1.9 hours (metabolite)
ExcretionRenal (70%) and fecal (30%)
Identifiers
  • (11β,16β)-21-(acetyloxy)-11-hydroxy-2′-methyl-5′H-pregna-1,4-dieno[17,16-d]oxazole-3,20-dione
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.034.969 Edit this at Wikidata
Chemical and physical data
FormulaC25H31NO6
Molar mass441.517 g/mol g·mol−1
3D model (JSmol)
  • O=C(OCC(=O)[C@]25/N=C(\O[C@@H]5C[C@H]1[C@H]4[C@H]([C@@H](O)C[C@@]12C)[C@]/3(/C=C\C(=O)\C=C\3CC4)C)C)C
  • InChI=1S/C25H31NO6/c1-13-26-25(20(30)12-31-14(2)27)21(32-13)10-18-17-6-5-15-9-16(28)7-8-23(15,3)22(17)19(29)11-24(18,25)4/h7-9,17-19,21-22,29H,5-6,10-12H2,1-4H3/t17-,18-,19-,21+,22+,23-,24-,25+/m0/s1 ☒N
  • Key:FBHSPRKOSMHSIF-GRMWVWQJSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Deflazacort is a glucocorticoid used as an anti-inflammatory and immunosuppressant.

Deflazacort is an inactive prodrug which is metabolized rapidly to the active drug 21-desacetyldeflazacort.[1] Its potency is around 70–90% that of prednisone.[2]

It is sold in Bangladesh as Xalcort, marketed by Beacon Pharmaceuticals Limited, in the United Kingdom by Shire under the trade name Calcort;[2] in Brazil as Cortax, Decortil, and Deflanil; in India as MOAID, ZENFLAV BY TIGRIS, Defolet(Roussette), DFZ, Decotaz, and DefZot; in Panama as Zamen, Spain as Zamene and in Honduras as Flezacor.[3] It is not available in the United States. In January 2015, the FDA granted fast track status to Marathon Pharmaceuticals to pursue approval of deflazacort as a potential treatment for Duchenne muscular dystrophy. The company expects to make deflazacort available in the United States in 2016. [4]

References

  1. ^ Möllmann, H; Hochhaus, G; Rohatagi, S; Barth, J; Derendorf, H (1995). "Pharmacokinetic/pharmacodynamic evaluation of deflazacort in comparison to methylprednisolone and prednisolone". Pharmaceutical Research. 12 (7): 1096–100. PMID 7494809.
  2. ^ a b "Calcort". electronic Medicines Compendium. June 11, 2008. Retrieved on October 28, 2008.
  3. ^ "Substâncias: DEFLAZACORT" (in Portuguese). Centralx. 2008. Retrieved on October 28, 2008.
  4. ^ http://www.chicagotribune.com/business/ct-marathon-muscular-dystrophy-drug-0119-biz-20150119-story.html#page=1