deflazacort Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
corticosteroids, except prednisolone derivatives 793 14484-47-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • deflazacort
  • azacort
  • azacortinol
  • calcort
  • dezacor
  • dezacort
  • flantadin
  • lantadin
  • oxazacort
Deflazacort is a corticosteroid prodrug, whose active metabolite, 21-desDFZ, acts through the glucocorticoid receptor to exert anti-inflammatory and immunosuppressive effects. The precise mechanism by which deflazacort exerts its therapeutic effects in patients with Duchenne muscular dystrophy is unknown.
  • Molecular weight: 441.52
  • Formula: C25H31NO6
  • CLOGP: 2.86
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 1
  • TPSA: 102.26
  • ALOGS: -4.40
  • ROTB: 4

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
15 mg O

ADMET properties:

PropertyValueReference
BA (Bioavailability) 68 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Feb. 9, 2017 FDA MARATHON PHARMACEUTICALS LLC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Bursitis infective 111.64 22.40 23 2613 1154 46682272
Angioedema 72.37 22.40 38 2598 39304 46644122
Allergy test positive 72.02 22.40 13 2623 321 46683105
Bronchiectasis 57.03 22.40 21 2615 9295 46674131
Peripheral vascular disorder 50.02 22.40 17 2619 5960 46677466
Drug reaction with eosinophilia and systemic symptoms 47.18 22.40 26 2610 29522 46653904
Apraxia 46.24 22.40 12 2624 1663 46681763
Perseveration 42.34 22.40 8 2628 255 46683171
Urticaria 38.60 22.40 40 2596 117852 46565574
Localised infection 38.15 22.40 21 2615 23780 46659646
Toxic epidermal necrolysis 33.90 22.40 19 2617 22259 46661167
Respiratory tract infection 33.65 22.40 21 2615 29951 46653475
Hyperreflexia 32.72 22.40 12 2624 5242 46678184
Osteoporosis 32.41 22.40 23 2613 40585 46642841
Skin ulcer 32.12 22.40 21 2615 32437 46650989
Bone disorder 30.25 22.40 17 2619 20016 46663410
Tenosynovitis 28.56 22.40 12 2624 7503 46675923
Staphylococcal infection 27.94 22.40 20 2616 35751 46647675
Hemianopia 27.44 22.40 7 2629 906 46682520
Skin discolouration 27.21 22.40 19 2617 32661 46650765
Myoclonus 23.92 22.40 13 2623 14339 46669087
Gastroenteritis bacterial 22.47 22.40 4 2632 91 46683335

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Weight increased 283.52 36.39 133 2360 74780 29875205
Nasopharyngitis 108.69 36.39 65 2428 58784 29891201
Influenza 104.44 36.39 57 2436 43341 29906644
Myoglobinuria 100.41 36.39 21 2472 763 29949222
Increased appetite 79.08 36.39 26 2467 5591 29944394
Gastroenteritis viral 77.68 36.39 26 2467 5907 29944078
Off label use 76.11 36.39 98 2395 249192 29700793
Behaviour disorder 58.72 36.39 17 2476 2395 29947590
Product dose omission issue 57.79 36.39 53 2440 91578 29858407
Anger 51.92 36.39 23 2470 11097 29938888
Systemic inflammatory response syndrome 49.10 36.39 19 2474 6527 29943458
Pyrexia 45.96 36.39 85 2408 294404 29655581
Fall 42.44 36.39 63 2430 181809 29768176
Malaise 40.62 36.39 59 2434 166903 29783082
Tachypnoea 39.67 36.39 21 2472 14931 29935054
Swelling face 37.91 36.39 23 2470 21181 29928804
Cushingoid 36.95 36.39 12 2481 2475 29947510
Rhabdomyolysis 36.59 36.39 35 2458 63545 29886440

Pharmacologic Action:

SourceCodeDescription
ATC H02AB13 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
CORTICOSTEROIDS FOR SYSTEMIC USE
CORTICOSTEROIDS FOR SYSTEMIC USE, PLAIN
Glucocorticoids
FDA MoA N0000175450 Corticosteroid Hormone Receptor Agonists
FDA EPC N0000175576 Corticosteroid
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D007155 Immunologic Factors
MeSH PA D007166 Immunosuppressive Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Duchenne muscular dystrophy indication 76670001 DOID:11723

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.27 acidic
pKa2 7.14 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
18MG EMFLAZA PTC THERAP N208684 Feb. 9, 2017 RX TABLET ORAL Feb. 9, 2022 NEW CHEMICAL ENTITY
30MG EMFLAZA PTC THERAP N208684 Feb. 9, 2017 RX TABLET ORAL Feb. 9, 2022 NEW CHEMICAL ENTITY
36MG EMFLAZA PTC THERAP N208684 Feb. 9, 2017 RX TABLET ORAL Feb. 9, 2022 NEW CHEMICAL ENTITY
6MG EMFLAZA PTC THERAP N208684 Feb. 9, 2017 RX TABLET ORAL Feb. 9, 2022 NEW CHEMICAL ENTITY
22.75MG/ML EMFLAZA PTC THERAP N208685 Feb. 9, 2017 RX SUSPENSION ORAL Feb. 9, 2022 NEW CHEMICAL ENTITY
18MG EMFLAZA PTC THERAP N208684 Feb. 9, 2017 RX TABLET ORAL Feb. 9, 2024 TREATMENT OF DUCHENNE MUSCULAR DYSTROPHY IN PATIENTS 5 YEARS OF AGE AND OLDER
30MG EMFLAZA PTC THERAP N208684 Feb. 9, 2017 RX TABLET ORAL Feb. 9, 2024 TREATMENT OF DUCHENNE MUSCULAR DYSTROPHY IN PATIENTS 5 YEARS OF AGE AND OLDER
36MG EMFLAZA PTC THERAP N208684 Feb. 9, 2017 RX TABLET ORAL Feb. 9, 2024 TREATMENT OF DUCHENNE MUSCULAR DYSTROPHY IN PATIENTS 5 YEARS OF AGE AND OLDER
6MG EMFLAZA PTC THERAP N208684 Feb. 9, 2017 RX TABLET ORAL Feb. 9, 2024 TREATMENT OF DUCHENNE MUSCULAR DYSTROPHY IN PATIENTS 5 YEARS OF AGE AND OLDER
22.75MG/ML EMFLAZA PTC THERAP N208685 Feb. 9, 2017 RX SUSPENSION ORAL Feb. 9, 2024 TREATMENT OF DUCHENNE MUSCULAR DYSTROPHY IN PATIENTS 5 YEARS OF AGE AND OLDER
18MG EMFLAZA PTC THERAP N208684 Feb. 9, 2017 RX TABLET ORAL June 7, 2026 TREATMENT OF DUCHENE MUSCULAR DYSTROPHY IN PATIENTS 2 YEARS OF AGE TO LESS THAN 5 YEARS OF AGE
30MG EMFLAZA PTC THERAP N208684 Feb. 9, 2017 RX TABLET ORAL June 7, 2026 TREATMENT OF DUCHENE MUSCULAR DYSTROPHY IN PATIENTS 2 YEARS OF AGE TO LESS THAN 5 YEARS OF AGE
36MG EMFLAZA PTC THERAP N208684 Feb. 9, 2017 RX TABLET ORAL June 7, 2026 TREATMENT OF DUCHENE MUSCULAR DYSTROPHY IN PATIENTS 2 YEARS OF AGE TO LESS THAN 5 YEARS OF AGE
6MG EMFLAZA PTC THERAP N208684 Feb. 9, 2017 RX TABLET ORAL June 7, 2026 TREATMENT OF DUCHENE MUSCULAR DYSTROPHY IN PATIENTS 2 YEARS OF AGE TO LESS THAN 5 YEARS OF AGE
22.75MG/ML EMFLAZA PTC THERAP N208685 Feb. 9, 2017 RX SUSPENSION ORAL June 7, 2026 TREATMENT OF DUCHENE MUSCULAR DYSTROPHY IN PATIENTS 2 YEARS OF AGE TO LESS THAN 5 YEARS OF AGE

Bioactivity Summary:

None

External reference:

IDSource
D03671 KEGG_DRUG
13649-57-5 SECONDARY_CAS_RN
4036431 VANDF
C0593761 UMLSCUI
CHEBI:135720 CHEBI
CHEMBL1201891 ChEMBL_ID
DB11921 DRUGBANK_ID
189821 PUBCHEM_CID
C021988 MESH_SUPPLEMENTAL_RECORD_UI
C014725 MESH_SUPPLEMENTAL_RECORD_UI
9477 IUPHAR_LIGAND_ID
4323 INN_ID
KR5YZ6AE4B UNII
3081431 PUBCHEM_CID
T1LWN33J2P UNII
153100 RXNORM
18036 MMSL
d04977 MMSL
006032 NDDF
116578002 SNOMEDCT_US
396012006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
EMFLAZA HUMAN PRESCRIPTION DRUG LABEL 1 52856-501 TABLET 6 mg ORAL NDA 27 sections
EMFLAZA HUMAN PRESCRIPTION DRUG LABEL 1 52856-502 TABLET 18 mg ORAL NDA 27 sections
EMFLAZA HUMAN PRESCRIPTION DRUG LABEL 1 52856-503 TABLET 30 mg ORAL NDA 27 sections
EMFLAZA HUMAN PRESCRIPTION DRUG LABEL 1 52856-504 TABLET 36 mg ORAL NDA 27 sections
EMFLAZA HUMAN PRESCRIPTION DRUG LABEL 1 52856-505 SUSPENSION 22.75 mg ORAL NDA 27 sections