General Information of Drug (ID: DMV0RNS)

Drug Name
Deflazacort
Synonyms C25H33NO6; Deflazacort (Calcort); Deflazacortum [INN-Latin]; EINECS 238-483-7; Deflan (TN); D09WYX; AC1L1BQ2; Deflazacort [USAN:BAN:INN]; CTK8F9001; MolPort-035-394-927
Indication
Disease Entry ICD 11 Status REF
Duchenne dystrophy 8C70 Approved [1], [2], [3], [4]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 441.5
Topological Polar Surface Area (xlogp) 2
Rotatable Bond Count (rotbonds) 4
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 7
ADMET Property
Absorption Cmax
The maximum plasma concentration (Cmax) of drug is 4.00 ng/L [5]
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 0.25 h [5]
Bioavailability
The bioavailability of drug is 3.3-4.1% [5]
Clearance
The clearance of drug is 114 +/- 27 L/h [6]
Elimination
Urinary excretion is the major route of deflazacort elimination, accounting for about about 70% of the excreted dose [6]
Half-life
The concentration or amount of drug in body reduced by one-half in 1.1 - 1.9 hours [6]
Metabolism
The drug is metabolized via plasma esterases [7]
Vd
The volume of distribution (Vd) of drug is 204 +/- 84 L [6]
Chemical Identifiers
Formula
C25H31NO6
IUPAC Name
[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
Canonical SMILES
CC1=N[C@@]2([C@H](O1)C[C@@H]3[C@@]2(C[C@@H]([C@H]4[C@H]3CCC5=CC(=O)C=C[C@]45C)O)C)C(=O)COC(=O)C
InChI
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
InChIKey
FBHSPRKOSMHSIF-GRMWVWQJSA-N
Cross-matching ID
PubChem CID
189821
ChEBI ID
CHEBI:135720
CAS Number
14484-47-0
DrugBank ID
DB11921
TTD ID
D09WYX
VARIDT ID
DR00146
INTEDE ID
DR0430
ACDINA ID
D00174

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Glucocorticoid receptor (NR3C1) TTYRL6O GCR_HUMAN Modulator [8]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [9]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME
DE4LYSA CP3A4_HUMAN Substrate [10]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Duchenne dystrophy
ICD Disease Classification 8C70
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
P-glycoprotein 1 (ABCB1) DTP P-GP 7.23E-01 -8.20E-02 -3.22E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 9.85E-01 2.24E-02 7.33E-02
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Deflazacort (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
ABT-492 DMJFD2I Major Increased risk of tendinitis/tendon rupture by the combination of Deflazacort and ABT-492. Bacterial infection [1A00-1C4Z] [33]
Troleandomycin DMUZNIG Major Decreased metabolism of Deflazacort caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [34]
Pexidartinib DMS2J0Z Major Increased metabolism of Deflazacort caused by Pexidartinib mediated induction of CYP450 enzyme. Bone/articular cartilage neoplasm [2F7B] [34]
MK-8228 DMOB58Q Major Decreased metabolism of Deflazacort caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [34]
Tazemetostat DMWP1BH Moderate Increased metabolism of Deflazacort caused by Tazemetostat mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [35]
Bempedoic acid DM1CI9R Major Increased risk of tendinitis/tendon rupture by the combination of Deflazacort and Bempedoic acid. Hyper-lipoproteinaemia [5C80] [36]
Berotralstat DMWA2DZ Major Decreased metabolism of Deflazacort caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [34]
PF-06463922 DMKM7EW Major Increased metabolism of Deflazacort caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [34]
Selpercatinib DMZR15V Moderate Decreased metabolism of Deflazacort caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [34]
IPI-145 DMWA24P Major Decreased metabolism of Deflazacort caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [34]
Cemiplimab DMKMJHE Moderate Additive immunosuppressive effects by the combination of Deflazacort and Cemiplimab. Melanoma [2C30] [37]
Siponimod DM2R86O Major Additive immunosuppressive effects by the combination of Deflazacort and Siponimod. Multiple sclerosis [8A40] [38]
Ocrelizumab DMEZ2KH Moderate Additive immunosuppressive effects by the combination of Deflazacort and Ocrelizumab. Multiple sclerosis [8A40] [39]
Fedratinib DM4ZBK6 Major Decreased metabolism of Deflazacort caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [34]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Deflazacort caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [40]
Abametapir DM2RX0I Moderate Decreased metabolism of Deflazacort caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [41]
Lefamulin DME6G97 Moderate Decreased metabolism of Deflazacort caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [42]
Choline salicylate DM8P137 Moderate Increased risk of GI mucosal injury/bleeding risk by the combination of Deflazacort and Choline salicylate. Postoperative inflammation [1A00-CA43] [43]
Voxelotor DMCS6M5 Moderate Decreased metabolism of Deflazacort caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [44]
Larotrectinib DM26CQR Moderate Decreased metabolism of Deflazacort caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [38]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Deflazacort caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [45]
⏷ Show the Full List of 21 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Deflazacort 18 mg tablet 18 mg Oral Tablet Oral
Deflazacort 30 mg tablet 30 mg Oral Tablet Oral
Deflazacort 36 mg tablet 36 mg Oral Tablet Oral
Deflazacort 6 mg tablet 6 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

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