1. Calcort
2. Dezacor
3. Emflaza
4. Zamene
1. 14484-47-0
2. Azacort
3. Calcort
4. Oxazacort
5. Flantadin
6. Emflaza
7. Cortax
8. Deflan
9. Mdl 458
10. Mdl-458
11. L-5458
12. Kr5yz6ae4b
13. Mdl458
14. Dezacor
15. Lantadin
16. Dsstox_cid_378
17. Dsstox_rid_75552
18. Dsstox_gsid_20378
19. 2-((6ar,6bs,7s,8as,8bs,11ar,12as,12bs)-7-hydroxy-6a,8a,10-trimethyl-4-oxo-1,2,4,6a,6b,7,8,8a,11a,12,12a,12b-dodecahydro-8bh-naphtho[2',1':4,5]indeno[1,2-d]oxazol-8b-yl)-2-oxoethyl Acetate
20. Deflazacortum
21. Decortil
22. Deflanil
23. Enzocort
24. Deflazacort (calcort)
25. 2-[(4ar,4bs,5s,6as,6bs,9ar,10as,10bs)-5-hydroxy-4a,6a,8-trimethyl-2-oxo-2,4a,4b,5,6,6a,9a,10,10a,10b,11,12-dodecahydro-6bh-naphtho[2',1':4,5]indeno[1,2-d][1,3]oxazol-6b-yl]-2-oxoethyl Acetate
26. Cas-14484-47-0
27. Dl-458-it
28. Unii-kr5yz6ae4b
29. Deflazacortum [inn-latin]
30. Deflazacort [usan:inn:ban]
31. Einecs 238-483-7
32. Emflaza (tn)
33. Mfcd00866106
34. Deflazacort [mi]
35. Deflazacort [inn]
36. Deflazacort (usan/inn)
37. Deflazacort [usan]
38. Schembl4018
39. Deflazacort [mart.]
40. Deflazacort [usp-rs]
41. Deflazacort [who-dd]
42. Dl-458it
43. Gtpl9477
44. Chembl1201891
45. Dtxsid9020378
46. Deflazacort, >=98% (hplc)
47. Deflazacort [orange Book]
48. Chebi:135720
49. Hms3714d15
50. Bcp08474
51. Zinc4212809
52. Tox21_112506
53. Tox21_301415
54. Bbl036672
55. S1888
56. Stl559051
57. Akos015895199
58. Tox21_112506_1
59. Ccg-220817
60. Db11921
61. Ks-1158
62. Ncgc00255189-01
63. Ncgc00263521-01
64. 11beta,21-dihydroxy-2'-methyl-5'betah-pregna-1,4-dieno(17,16-d)oxazole-3,20-dione 21-acetate
65. Hy-13609
66. Deflazacort 100 Microg/ml In Acetonitrile
67. D4523
68. D03671
69. T70289
70. Ab01274724-01
71. Ab01274724_02
72. 484d470
73. Q779118
74. Q-101371
75. 3-amino-3-(4-chloro-3-nitro-phenyl)-propionicacid
76. Deflazacort, United States Pharmacopeia (usp) Reference Standard
77. 11b,21-dihydroxy-2'-methyl-5'bh-pregna-1,4-dieno[17,16-d]oxazole-3,20-dione 21-acetate
78. (11beta,16beta)-21-(acetyloxy)-11-hydroxy-2'-methyl-5'h-pregna-1,4-dieno(17,16-d)oxazole-3,20-dione
79. [2-[(1s,2s,4r,8s,9s,11s,12s,13r)-11-hydroxy-6,9,13-trimethyl-16-oxo-5-oxa-7-azapentacyclo[10.8.0.02,9.04,8.013,18]icosa-6,14,17-trien-8-yl]-2-oxoethyl] Acetate
80. 11.beta.,21-dihydroxy-2'-methyl-5'.beta.h-pregna-1,4-dieno(17,16-d)oxazole-3,20-dione 21-acetate
81. 2-((6ar,6bs,7s,8as,8bs,11ar,12as,12bs)-7-hydroxy-6a,8a,10-trimethyl-4-oxo-2,4,6a,6b,7,8,8a,8b,11a,12,12a,12b-dodecahydro-1h-naphtho[2',1':4,5]indeno[1,2-d]oxazol-8b-yl)-2-oxoethyl Acetate
82. 5'-beta-h-pregna-1,4-dieno(17,16-d)oxazole-3,20-dione, 11-beta,21-dihydroxy-2'-methyl-, 21-acetate
83. 5'h-pregna-1,4-dieno(17,16-d)oxazole-3,20-dione, 21-(acetyloxy)-11-hydroxy-2'-methyl-, (11.beta.,16.beta.)-
84. 5'h-pregna-1,4-dieno(17,16-d)oxazole-3,20-dione, 21-(acetyloxy)-11-hydroxy-2'-methyl-, (11beta,16beta)-
| Molecular Weight | 441.5 g/mol |
|---|---|
| Molecular Formula | C25H31NO6 |
| XLogP3 | 2 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 7 |
| Rotatable Bond Count | 4 |
| Exact Mass | 441.21513771 g/mol |
| Monoisotopic Mass | 441.21513771 g/mol |
| Topological Polar Surface Area | 102 Ų |
| Heavy Atom Count | 32 |
| Formal Charge | 0 |
| Complexity | 996 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 8 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently Bonded Unit Count | 1 |
Deflazacort is indicated for the treatment of Duchenne Muscular Dystrophy (DMD) in patients 2 years of age and older.
Deflazacort exerts anti-inflammatory activity in DMD, likely improving various symptoms, including muscle weakness and cardiorespiratory symptoms in addition to delaying their onset. This allows for an increased quality of life and prevents the necessity for surgical procedures, such as those for scoliosis, which is associated with DMD. Studies showed significant preservation of muscle mass in patients generally treated with 0.9 mg/kg/day of deflazacort compared to a control group. The following findings are based on clinical studies using deflazacort on a long term basis: **Effects on muscle strength** At age 16, individuals treated with long-term deflazacort had 63 4% score in muscle strength compared to a mean muscle strength score of 31 3% for control patients. Significant improvements in climbing stairs and rising from a supine position were also seen in patients taking deflazacort. **Effects on ambulation** Ambulation was significantly higher by 12 years of age and 18 years of age in patients taking deflazacort when compared with the control group. The control group showed a mean loss of ambulation of 2 years sooner than with deflazacort treatment. **Effects on cardiac function** Mean left ventricular ejection fraction (a measure of cardiac function) was higher in patients treated with deflazacort over the long term. Preservation of cardiac function was demonstrated by a mean difference in ejection fraction of about 7%, favoring study groups taking deflazacort over control groups. **Effects on spinal alignment** Children treated with deflazacort also significantly lowered the rate and severity of scoliosis and eliminated the need for scoliosis surgery after long-term treatment.
Anti-Inflammatory Agents
Substances that reduce or suppress INFLAMMATION. (See all compounds classified as Anti-Inflammatory Agents.)
Immunosuppressive Agents
Agents that suppress immune function by one of several mechanisms of action. Classical cytotoxic immunosuppressants act by inhibiting DNA synthesis. Others may act through activation of T-CELLS or by inhibiting the activation of HELPER CELLS. While immunosuppression has been brought about in the past primarily to prevent rejection of transplanted organs, new applications involving mediation of the effects of INTERLEUKINS and other CYTOKINES are emerging. (See all compounds classified as Immunosuppressive Agents.)
H02AB13
S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355
H - Systemic hormonal preparations, excl. sex hormones and insulins
H02 - Corticosteroids for systemic use
H02A - Corticosteroids for systemic use, plain
H02AB - Glucocorticoids
H02AB13 - Deflazacort
Absorption
Deflazacort is rapidly absorbed after oral administration with peak concentration occurring within 1-2 hours. One pharmacokinetic study determined an AUC (area under the curve) of 280 ng/ml h. The bioavailability of both the oral suspension and tablet are similar. In clinical studies, coadministration of deflazacort crushed with food or applesauce did not affect absorption or bioavailability.
Route of Elimination
Urinary excretion is the major route of deflazacort elimination, accounting for about about 70% of the excreted dose. The remainder of the dose (about 30%) is excreted in the feces. Elimination is almost completed by 24 hours post-dose. 21-deflazacort makes up about 18% of the eliminated drug in the urine.
Volume of Distribution
One study determined the volume of distribution to be 204 84 L.
Clearance
114 27 L/h, according to one noncompartmental pharmacokinetic study. The clearance of corticosteroids is enhanced in hypothyroid patients and increased in patients with hyperthyroidism. Dosing adjustments may be considered according to thyroid status. A study of corticosteroid clearance was performed in patients with a creatinine clearance of 15 mL/min or less, and determined that the active metabolite of deflazacort, 21-deflazacort was similar to that in patients with normal renal clearance.
After oral ingestion, deflazacort is deacetylated at position 21 by plasma esterases, producing the active metabolite 21-deflazacort. 21-deflazacort is then further metabolized by CYP3A4 to inactive metabolite products. Deflazacort 21-OH metabolism is extensive. The metabolite of deflazacort-21-OH is deflazacort 6-beta-OH.
The half-life of deflazacort ranges from 1.1 to 1.9 h
Deflazacort is a corticosteroid prodrug with an active metabolite, 21-deflazacort, which binds to the glucocorticoid receptor to exert anti-inflammatory and immunosuppressive effects on the body. The exact mechanism by which deflazacort exerts its therapeutic effects in patients with DMD is unknown but likely occurs via its anti-inflammatory activities.
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