Details of the Drug

General Information of Drug (ID: DMXBQAM)

• Drug Name: Miglitol
• Synonyms: Diastabol; Glyset; Plumarol; Seibule; Glyset (TN); SK-983; Bay-m-1099; Miglitol (JAN/USAN/INN); (2R,3R,4R,5S)-1-(2-hydroxyethyl)-2-(hydroxymethyl)piperidine-3,4,5-triol

Indication

Disease Entry	ICD 11	Status	REF
Diabetic complication	5A2Y	Approved	[1]

• Therapeutic Class: Hypoglycemic Agents
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 1:
  Molecular Weight (mw); 207.22
  Logarithm of the Partition Coefficient (xlogp); -2.6
  Rotatable Bond Count (rotbonds); 3
  Hydrogen Bond Donor Count (hbonddonor); 5
  Hydrogen Bond Acceptor Count (hbondacc); 6
• ADMET Property:
  BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 3: high solubility and low permeability [2]
  Bioavailability: 60% of drug becomes completely available to its intended biological destination(s) [3]
  Clearance: The drug present in the plasma can be removed from the body at the rate of 1.7 mL/min/kg [4]
  Elimination: 80% of drug is excreted from urine in the unchanged form [2]
  Half-life: The concentration or amount of drug in body reduced by one-half in 2 hours [4]
  Metabolism: The drug is not metabolised []
  MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 20.6811 micromolar/kg/day [5]
  Unbound Fraction: The unbound fraction of drug in plasma is 1% [4]
  Vd: The volume of distribution (Vd) of drug is 0.18 L/kg []
• Chemical Identifiers:
  Formula: C8H17NO5
  IUPAC Name: (2R,3R,4R,5S)-1-(2-hydroxyethyl)-2-(hydroxymethyl)piperidine-3,4,5-triol
  Canonical SMILES: C1[C@@H]([C@H]([C@@H]([C@H](N1CCO)CO)O)O)O
  InChI: InChI=1S/C8H17NO5/c10-2-1-9-3-6(12)8(14)7(13)5(9)4-11/h5-8,10-14H,1-4H2/t5-,6+,7-,8-/m1/s1
  InChIKey: IBAQFPQHRJAVAV-ULAWRXDQSA-N
• Cross-matching ID:
  PubChem CID: 441314
  ChEBI ID: CHEBI:6935
  CAS Number: 72432-03-2
  DrugBank ID: DB00491
  TTD ID: D0D0ZD
  ACDINA ID: D00433

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Intestinal maltase-glucoamylase (MGAM)	TTXWASR	MGA_HUMAN	Inhibitor	[6]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Interleukin-1 beta (IL1B)	OT0DWXXB	IL1B_HUMAN	Gene/Protein Processing	[7]
Interleukin-6 (IL6)	OTUOSCCU	IL6_HUMAN	Protein Interaction/Cellular Processes	[7]
Protein S100-A10 (S100A10)	OTI71243	S10AA_HUMAN	Gene/Protein Processing	[7]
Protein S100-A11 (S100A11)	OTI57KDN	S10AB_HUMAN	Gene/Protein Processing	[7]
Protein S100-A12 (S100A12)	OTF9IIXW	S10AC_HUMAN	Gene/Protein Processing	[7]
Protein S100-A4 (S100A4)	OTLRGFSQ	S10A4_HUMAN	Gene/Protein Processing	[7]
Protein S100-A6 (S100A6)	OTHHPZQ8	S10A6_HUMAN	Gene/Protein Processing	[7]
Protein S100-A9 (S100A9)	OTOARHCS	S10A9_HUMAN	Gene/Protein Processing	[7]
Tumor necrosis factor (TNF)	OT4IE164	TNFA_HUMAN	Gene/Protein Processing	[7]

Molecular Expression Atlas of This Drug

• The Studied Disease: Diabetic complication
• ICD Disease Classification: 5A2Y

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Intestinal maltase-glucoamylase (MGAM)	DTT	MGAM	4.59E-01	-0.02	-0.24

Drug-Drug Interaction (DDI) Information of This Drug

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

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Pramlintide	DM0EZ9Q	Moderate	Altered absorption of Miglitol due to GI dynamics variation caused by Pramlintide.	Type-1/2 diabete [5A10-5A11]	[8]

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

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Magnesium stearate	E00208	11177	lubricant
Polyethylene glycol 400	E00653	Not Available	Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polysorbate 80	E00665	Not Available	Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Miglitol 100 mg tablet	100 mg	Oral Tablet	Oral
Miglitol 25 mg tablet	25 mg	Oral Tablet	Oral
Miglitol 50 mg tablet	50 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

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: 4842).
• [2] BDDCS applied to over 900 drugs
• [3] Critical Evaluation of Human Oral Bioavailability for Pharmaceutical Drugs by Using Various Cheminformatics Approaches
• [4] Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
• [5] Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
• [6] Drug therapy of postprandial hyperglycaemia. Drugs. 1999 Jan;57(1):19-29.
• [7] The -glucosidase inhibitor miglitol decreases glucose fluctuations and inflammatory cytokine gene expression in peripheral leukocytes of Japanese patients with type 2 diabetes mellitus. Metabolism. 2010 Dec;59(12):1816-22. doi: 10.1016/j.metabol.2010.06.006. Epub 2010 Jul 29.
• [8] Product Information. Symlin (pramlintide). Amphastar Pharmaceuticals Inc, South El Monte, CA.