Details of the Drug

General Information of Drug (ID: DM28UJG)

• Drug Name: Dapagliflozin
• Synonyms: BMS 512148; BMS-512148; BMS-512148, Dapagliflozin; Dapagliflozin (INN/USAN); 2-(3-(4-Ethoxybenzyl)-4-chlorophenyl)-6-hydroxymethyltetrahydro-2H-pyran-3,4,5-triol

Indication

Disease Entry	ICD 11	Status	REF
Type-2 diabetes	5A11	Approved	[1], [2], [3]

• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 408.9
  Topological Polar Surface Area (xlogp); 2.3
  Rotatable Bond Count (rotbonds); 6
  Hydrogen Bond Donor Count (hbonddonor); 4
  Hydrogen Bond Acceptor Count (hbondacc); 6
• ADMET Property:
  BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [4]
  Clearance: The drug present in the plasma can be removed from the body at the rate of 3 mL/min/kg [5]
  Half-life: The concentration or amount of drug in body reduced by one-half in 12.2 hours [5]
  Unbound Fraction: The unbound fraction of drug in plasma is 0.09% [5]
  Vd: Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 1.7 L/kg [5]
• Chemical Identifiers:
  Formula: C21H25ClO6
  IUPAC Name: (2S,3R,4R,5S,6R)-2-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
  Canonical SMILES: CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O)Cl
  InChI: InChI=1S/C21H25ClO6/c1-2-27-15-6-3-12(4-7-15)9-14-10-13(5-8-16(14)22)21-20(26)19(25)18(24)17(11-23)28-21/h3-8,10,17-21,23-26H,2,9,11H2,1H3/t17-,18-,19+,20-,21+/m1/s1
  InChIKey: JVHXJTBJCFBINQ-ADAARDCZSA-N
• Cross-matching ID:
  PubChem CID: 9887712
  ChEBI ID: CHEBI:85078
  CAS Number: 461432-26-8
  DrugBank ID: DB06292
  TTD ID: D01TNW
  VARIDT ID: DR00918
  INTEDE ID: DR0412
  ACDINA ID: D00167

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	[2], [6]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Substrate	[7]
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Substrate	[7]
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Substrate	[7]
Cytochrome P450 2A6 (CYP2A6)	DEJVYAZ	CP2A6_HUMAN	Substrate	[7]
Cytochrome P450 1A2 (CYP1A2)	DEJGDUW	CP1A2_HUMAN	Substrate	[7]
UDP-glucuronosyltransferase 2B7 (UGT2B7)	DEB3CV1	UD2B7_HUMAN	Substrate	[7]
UDP-glucuronosyltransferase 1A9 (UGT1A9)	DE85D2P	UD19_HUMAN	Substrate	[7]

Drug-Drug Interaction (DDI) Information of This Drug

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

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Arn-509	DMT81LZ	Moderate	Increased metabolism of Dapagliflozin caused by Arn-509 mediated induction of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[69]
Regorafenib	DMHSY1I	Minor	Decreased metabolism of Dapagliflozin caused by Regorafenib mediated inhibition of UGT.	Colorectal cancer [2B91]	[70]
PF-06463922	DMKM7EW	Moderate	Increased metabolism of Dapagliflozin caused by PF-06463922 mediated induction of UGT.	Lung cancer [2C25]	[71]

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

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Crospovidone	E00626	Not Available	Disintegrant
Magnesium stearate	E00208	11177	lubricant
Polyethylene glycol 4000	E00654	Not Available	Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyvinyl alcohol	E00666	Not Available	Coating agent; Emulsion stabilizing agent; Film/Membrane-forming agent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Colcothar yellow	E00436	518696	Colorant
Cellulose microcrystalline	E00698	Not Available	Adsorbent; Suspending agent; Diluent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Dapagliflozin Propanediol 5mg tablet	5mg	Tablet	Oral
Dapagliflozin Propanediol 10mg tablet	10mg	Tablet	Oral
Dapagliflozin 10 mg tablet	10 mg	Oral Tablet	Oral
Dapagliflozin 5 mg tablet	5 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

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