Details of the Drug

General Information of Drug (ID: DMRF9YK)

Drug Name

Empagliflozin

Synonyms

864070-44-0; JARDIANCE; BI 10773; UNII-HDC1R2M35U; Empagliflozin (BI 10773); BI-10773; BI10773; HDC1R2M35U; CHEBI:82720; 1-chloro-4-(glucopyranos-1-yl)-2-(4-(tetrahydrofuran-3-yloxy)benzyl)benzene; AK160980; (1S)-1,5-anhydro-1-(4-chloro-3-{4-[(3S)-tetrahydrofuran-3-yloxy]benzyl}phenyl)-D-glucitol; (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-(((S)-tetrahydrofuran-3-yl)oxy)benzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol

Indication

Disease Entry	ICD 11	Status	REF
Type-1 diabetes	5A10	Approved	[1]
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Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

450.9

Logarithm of the Partition Coefficient (xlogp)

2

Rotatable Bond Count (rotbonds)

6

Hydrogen Bond Donor Count (hbonddonor)

4

Hydrogen Bond Acceptor Count (hbondacc)

7

ADMET Property

Absorption AUC: The area under the plot of plasma concentration (AUC) of drug is 1.870 micromolh/L [2]
Absorption Cmax: The maximum plasma concentration (Cmax) of drug is 0.259 micromol/L [2]
Absorption Tmax: The time to maximum plasma concentration (Tmax) is 1.5 h [2]
BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [3]
Clearance: The apparent oral clearance of drug is 10.6 L/h [2]
Elimination: After oral administration of radiolabeled empagliflozin approximately 41.2% of the administered dose was found eliminated in feces and 54.4% eliminated in urine [2]
Half-life: The concentration or amount of drug in body reduced by one-half in 12.4 hours [2]
Metabolism: The drug is metabolized via the glucuronidation [2]
Vd: The volume of distribution (Vd) of drug is 73.8 L [2]

Chemical Identifiers

Formula: C23H27ClO7
IUPAC Name: (2S,3R,4R,5S,6R)-2-[4-chloro-3-[[4-[(3S)-oxolan-3-yl]oxyphenyl]methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
Canonical SMILES: C1COC[C@H]1OC2=CC=C(C=C2)CC3=C(C=CC(=C3)[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)Cl
InChI: InChI=1S/C23H27ClO7/c24-18-6-3-14(23-22(28)21(27)20(26)19(11-25)31-23)10-15(18)9-13-1-4-16(5-2-13)30-17-7-8-29-12-17/h1-6,10,17,19-23,25-28H,7-9,11-12H2/t17-,19+,20+,21-,22+,23-/m0/s1
InChIKey: OBWASQILIWPZMG-QZMOQZSNSA-N

Cross-matching ID

PubChem CID: 11949646
ChEBI ID: CHEBI:82720
CAS Number: 864070-44-0
DrugBank ID: DB09038
TTD ID: D06ALD
VARIDT ID: DR00271
INTEDE ID: DR1755
ACDINA ID: D01043

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
Sodium/glucose cotransporter 2 (SGLT2)	TTLWPVF	SC5A2_HUMAN	Modulator	[4]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
Breast cancer resistance protein (ABCG2)	DTI7UX6	ABCG2_HUMAN	Substrate	[5]
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
UDP-glucuronosyltransferase 2B7 (UGT2B7)	DEB3CV1	UD2B7_HUMAN	Substrate	[7]
UDP-glucuronosyltransferase 1A9 (UGT1A9)	DE85D2P	UD19_HUMAN	Substrate	[7]
UDP-glucuronosyltransferase 1A3 (UGT1A3)	DEF2WXN	UD13_HUMAN	Substrate	[7]
UDP-glucuronosyltransferase 1A8 (UGT1A8)	DE2GB8N	UD18_HUMAN	Substrate	[7]

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Molecular Interaction Atlas (MIA)

MIA Detail

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Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Empagliflozin (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Arn-509	DMT81LZ	Moderate	Accelerated clearance of Empagliflozin due to the transporter induction by Arn-509.	Acute myeloid leukaemia [2A60]	[8]
Gilteritinib	DMTI0ZO	Moderate	Decreased clearance of Empagliflozin due to the transporter inhibition by Gilteritinib.	Acute myeloid leukaemia [2A60]	[9]
Ag-221	DMS0ZBI	Moderate	Decreased clearance of Empagliflozin due to the transporter inhibition by Ag-221.	BCR-ABL1-negative chronic myeloid leukaemia [2A41]	[9]
Erdafitinib	DMI782S	Moderate	Decreased clearance of Empagliflozin due to the transporter inhibition by Erdafitinib.	Bladder cancer [2C94]	[10]
Tucatinib	DMBESUA	Moderate	Decreased clearance of Empagliflozin due to the transporter inhibition by Tucatinib.	Breast cancer [2C60-2C6Y]	[11]
PF-04449913	DMSB068	Moderate	Decreased clearance of Empagliflozin due to the transporter inhibition by PF-04449913.	Chronic myelomonocytic leukaemia [2A40]	[8]
Fostemsavir	DM50ILT	Moderate	Decreased clearance of Empagliflozin due to the transporter inhibition by Fostemsavir.	Human immunodeficiency virus disease [1C60-1C62]	[12]
Bempedoic acid	DM1CI9R	Moderate	Decreased clearance of Empagliflozin due to the transporter inhibition by Bempedoic acid.	Hyper-lipoproteinaemia [5C80]	[13]
PF-06463922	DMKM7EW	Moderate	Increased metabolism of Empagliflozin caused by PF-06463922 mediated induction of UGT.	Lung cancer [2C25]	[9]
Capmatinib	DMYCXKL	Moderate	Decreased clearance of Empagliflozin due to the transporter inhibition by Capmatinib.	Lung cancer [2C25]	[14]
Lasmiditan	DMXLVDT	Moderate	Decreased clearance of Empagliflozin due to the transporter inhibition by Lasmiditan.	Migraine [8A80]	[15]
Darolutamide	DMV7YFT	Moderate	Decreased clearance of Empagliflozin due to the transporter inhibition by Darolutamide.	Prostate cancer [2C82]	[16]
Tedizolid	DMG2SKR	Moderate	Decreased clearance of Empagliflozin due to the transporter inhibition by Tedizolid.	Skin and skin-structure infection [1F28-1G0Z]	[8]
Fostamatinib	DM6AUHV	Moderate	Decreased clearance of Empagliflozin due to the transporter inhibition by Fostamatinib.	Thrombocytopenia [3B64]	[17]
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Carmellose sodium	E00625	Not Available	Disintegrant
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Hydroxypropyl cellulose	E00632	Not Available	Binding agent; Coating agent; Emulsifying agent; Film/Membrane-forming agent; Modified-release agent; Suspending agent; Viscosity-controlling agent
Hypromellose	E00634	Not Available	Coating agent
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Polyethylene glycol 4000	E00654	Not Available	Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Hydrophobic colloidal silica	E00285	24261	Anticaking agent; Emulsion stabilizing agent; Glidant; Suspending agent; Viscosity-controlling agent
Cellulose microcrystalline	E00698	Not Available	Adsorbent; Suspending agent; Diluent
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Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Empagliflozin 10mg tablet	10mg	Tablet	Oral
Empagliflozin 25mg tablet	25mg	Tablet	Oral

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References

1	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4754).
2	FDA Approved Drug Products: Jardiance (empagliflozin) oral tablets
3	BDDCS predictions, self-correcting aspects of BDDCS assignments, BDDCS assignment corrections, and classification for more than 175 additional drugs
4	2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
5	KEGG: new perspectives on genomes, pathways, diseases and drugs. Nucleic Acids Res. 2017 Jan 4;45(D1):D353-D361. (dg:DG01913)
6	KEGG: new perspectives on genomes, pathways, diseases and drugs. Nucleic Acids Res. 2017 Jan 4;45(D1):D353-D361. (dg:DG01665)
7	Empagliflozin (Jardiance): a novel SGLT2 inhibitor for the treatment of type-2 diabetes. P T. 2015 Jun;40(6):364-8.
8	Cerner Multum, Inc. "UK Summary of Product Characteristics.".
9	Cerner Multum, Inc. "Australian Product Information.".
10	Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.
11	Product Information. Tukysa (tucatinib). Seattle Genetics Inc, Bothell, WA.
12	Product Information. Rukobia (fostemsavir). ViiV Healthcare, Research Triangle Park, NC.
13	Product Information. Nexletol (bempedoic acid). Esperion Therapeutics, Ann Arbor, MI.
14	Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ.
15	Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
16	Product Information. Nubeqa (darolutamide). Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ.
17	Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.