Details of the Drug

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]
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Affected Organisms

Humans and other mammals

ATC Code

H02AB13: Deflazacort

H02AB: Glucocorticoids

H02A: CORTICOSTEROIDS FOR SYSTEMIC USE, PLAIN

H02: CORTICOSTEROIDS FOR SYSTEMIC USE

H: SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

441.5

Logarithm of the Partition Coefficient (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 [2]
Absorption Tmax: The time to maximum plasma concentration (Tmax) is 0.25 h [2]
Bioavailability: The bioavailability of drug is 3.3-4.1% [2]
Clearance: The clearance of drug is 114 +/- 27 L/h [3]
Elimination: Urinary excretion is the major route of deflazacort elimination, accounting for about about 70% of the excreted dose [3]
Half-life: The concentration or amount of drug in body reduced by one-half in 1.1 - 1.9 hours [3]
Metabolism: The drug is metabolized via plasma esterases [4]
Vd: The volume of distribution (Vd) of drug is 204 +/- 84 L [3]

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
UNII: KR5YZ6AE4B
DrugBank ID: DB11921
TTD ID: D09WYX
VARIDT ID: DR00146
INTEDE ID: DR0430
ACDINA ID: D00174

Combinatorial Drugs (CBD)

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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	[5]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[6]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)_{Main DME}	DE4LYSA	CP3A4_HUMAN	Substrate	[7]

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Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Glucocorticoid receptor (NR3C1)	OTCI2YDI	GCR_HUMAN	Gene/Protein Processing	[8]

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Molecular Interaction Atlas (MIA)

MIA Detail

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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)

MEA Detail

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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]	[9]
Troleandomycin	DMUZNIG	Major	Decreased metabolism of Deflazacort caused by Troleandomycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[10]
Pexidartinib	DMS2J0Z	Major	Increased metabolism of Deflazacort caused by Pexidartinib mediated induction of CYP450 enzyme.	Bone/articular cartilage neoplasm [2F7B]	[10]
MK-8228	DMOB58Q	Major	Decreased metabolism of Deflazacort caused by MK-8228 mediated inhibition of CYP450 enzyme.	Cytomegaloviral disease [1D82]	[10]
Tazemetostat	DMWP1BH	Moderate	Increased metabolism of Deflazacort caused by Tazemetostat mediated induction of CYP450 enzyme.	Follicular lymphoma [2A80]	[11]
Bempedoic acid	DM1CI9R	Major	Increased risk of tendinitis/tendon rupture by the combination of Deflazacort and Bempedoic acid.	Hyper-lipoproteinaemia [5C80]	[12]
Berotralstat	DMWA2DZ	Major	Decreased metabolism of Deflazacort caused by Berotralstat mediated inhibition of CYP450 enzyme.	Innate/adaptive immunodeficiency [4A00]	[10]
PF-06463922	DMKM7EW	Major	Increased metabolism of Deflazacort caused by PF-06463922 mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[10]
Selpercatinib	DMZR15V	Moderate	Decreased metabolism of Deflazacort caused by Selpercatinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[10]
IPI-145	DMWA24P	Major	Decreased metabolism of Deflazacort caused by IPI-145 mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[10]
Cemiplimab	DMKMJHE	Moderate	Additive immunosuppressive effects by the combination of Deflazacort and Cemiplimab.	Melanoma [2C30]	[13]
Siponimod	DM2R86O	Major	Additive immunosuppressive effects by the combination of Deflazacort and Siponimod.	Multiple sclerosis [8A40]	[14]
Ocrelizumab	DMEZ2KH	Moderate	Additive immunosuppressive effects by the combination of Deflazacort and Ocrelizumab.	Multiple sclerosis [8A40]	[15]
Fedratinib	DM4ZBK6	Major	Decreased metabolism of Deflazacort caused by Fedratinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[10]
Rucaparib	DM9PVX8	Moderate	Decreased metabolism of Deflazacort caused by Rucaparib mediated inhibition of CYP450 enzyme.	Ovarian cancer [2C73]	[16]
Abametapir	DM2RX0I	Moderate	Decreased metabolism of Deflazacort caused by Abametapir mediated inhibition of CYP450 enzyme.	Pediculosis [1G00]	[17]
Lefamulin	DME6G97	Moderate	Decreased metabolism of Deflazacort caused by Lefamulin mediated inhibition of CYP450 enzyme.	Pneumonia [CA40]	[18]
Choline salicylate	DM8P137	Moderate	Increased risk of GI mucosal injury/bleeding risk by the combination of Deflazacort and Choline salicylate.	Postoperative inflammation [1A00-CA43]	[19]
Voxelotor	DMCS6M5	Moderate	Decreased metabolism of Deflazacort caused by Voxelotor mediated inhibition of CYP450 enzyme.	Sickle-cell disorder [3A51]	[20]
Larotrectinib	DM26CQR	Moderate	Decreased metabolism of Deflazacort caused by Larotrectinib mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[14]
Fostamatinib	DM6AUHV	Moderate	Decreased metabolism of Deflazacort caused by Fostamatinib mediated inhibition of CYP450 enzyme.	Thrombocytopenia [3B64]	[21]
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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
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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

References

1	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2	Stimate (desmopressin acetate) nasal spray FDA Label
3	Pharmacokinetic/pharmacodynamic evaluation of deflazacort in comparison to methylprednisolone and prednisolone. Pharm Res. 1995 Jul;12(7):1096-100.
4	van Zwieten PA: Amlodipine: an overview of its pharmacodynamic and pharmacokinetic properties. Clin Cardiol. 1994 Sep;17(9 Suppl 3):III3-6.
5	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
6	KEGG: new perspectives on genomes, pathways, diseases and drugs. Nucleic Acids Res. 2017 Jan 4;45(D1):D353-D361. (dg:DG01665)
7	Mechanisms and clinical significance of pharmacokinetic-based drug-drug interactions with drugs approved by the U.S. Food and Drug Administration in 2017. Drug Metab Dispos. 2019 Feb;47(2):135-144.
8	Transactivation via the human glucocorticoid and mineralocorticoid receptor by therapeutically used steroids in CV-1 cells: a comparison of their glucocorticoid and mineralocorticoid properties. Eur J Endocrinol. 2004 Sep;151(3):397-406. doi: 10.1530/eje.0.1510397.
9	FDA. U.S. Food and Drug Administration "Information for Healthcare Professionals. Fluoroquinolone Antimicrobial Drugs. FDA Alert [7/8/2008].".
10	Cerner Multum, Inc. "UK Summary of Product Characteristics.".
11	Product Information. Tazverik (tazemetostat). Epizyme, Inc, Cambridge, MA.
12	Product Information. Nexletol (bempedoic acid). Esperion Therapeutics, Ann Arbor, MI.
13	Agencia Espaola de Medicamentos y Productos Sanitarios Healthcare "Centro de informacion online de medicamentos de la AEMPS - CIMA.".
14	Cerner Multum, Inc. "Australian Product Information.".
15	Product Information. Ocrevus (ocrelizumab). Genentech, South San Francisco, CA.
16	EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.".
17	Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
18	Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
19	Baer PA, Shore A, Ikeman RL "Transient fall in serum salicylate levels following intraarticular injection of steroid in patients with rheumatoid arthritis." Arthritis Rheum 30 (1987): 345-7. [PMID: 3566826]
20	Product Information. Oxbryta (voxelotor). Global Blood Therapeutics, Inc., South San Francisco, CA.
21	Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.