miglitol

Trade name: glyset

Small moleculeapproved

Approved

Dec 18, 1996

Miglitol, an oral alpha-glucosidase inhibitor, is a desoxynojirimycin derivative that delays the digestion of ingested carbohydrates, thereby resulting in a smaller rise in blood glucose concentration following meals. As a consequence of plasma glucose reduction, miglitol reduce levels of glycosylated hemoglobin in patients with Type II (non-insulin-dependent) diabetes mellitus. Systemic nonenzymatic protein glycosylation, as reflected by levels of glycosylated hemoglobin, is a function of average blood glucose concentration over time. Because its mechanism of action is different, the effect of miglitol to enhance glycemic control is additive to that of sulfonylureas when used in combination. In addition, miglitol diminishes the insulinotropic and weight-increasing effects of sulfonylureas. Miglitol has minor inhibitory activity against lactase and consequently, at the recommended doses, would not be expected to induce lactose intolerance. In contrast to sulfonylureas, miglitol does not enhance insulin secretion. The antihyperglycemic action of miglitol results from a reversible inhibition of membrane-bound intestinal a-glucoside hydrolase enzymes. Membrane-bound intestinal a-glucosidases hydrolyze oligosaccharides and disaccharides to glucose and other monosaccharides in the brush border of the small intestine. In diabetic patients, this enzyme inhibition results in delayed glucose absorption and lowering of postprandial hyperglycemia. Miglitol is used as an adjunct to diet to improve glycemic control in patients with non-insulin-dependent diabetes mellitus (NIDDM) whose hyperglycemia cannot be managed with diet alone. — NCATS

Clinical trial activity

12 trials · 11 clinical orgs · 4 marketing orgs

Phase 1
1
Phase 2
9
Phase 3
9
Phase 4
2

Earliest trial started Sep 13, 2005 (NCT00213109)

Timeline

1990s

  1. Dec 18, 1996

    Pharmacia & Upjohn — Earliest FDA Approval

  2. Dec 18, 1996

    Pfizer — Marketing Organization

  3. Dec 18, 1996

    Pharmacia & Upjohn — NDA Organization

  4. Dec 18, 1996

    Pfizer — NDA Secondary Org

2000s

  1. Jan 1, 2005

    Earliest Phase 3 Sponsor(trial)

2010s

  1. Jan 1, 2010

    Earliest Phase 1 Sponsor(trial)

  2. Feb 24, 2015

    Westminster Pharms — Marketing Organization

  3. Feb 24, 2015

    Orient Pharma Co., Ltd. — Marketing Organization

Indications

Mechanism of action

Approval history

  • approvedDec 18, 1996

Chemistry & pharmacology

Loading structure…

SMILES

OCCN1C[C@H](O)[C@@H](O)[C@H](O)[C@H]1CO
Mol. weight
207.2243 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • bay m 1099
  • bay-m 1099
  • bay-m-1099
  • bay-m-1099
  • bay-m-1099
  • diastabol
  • diastabol
  • diastabol
  • diastabol
  • glyset
  • glyset
  • glyset
  • glyset
  • glyset
  • lacer brand of miglitol
  • migliol
  • migliol
  • miglitol
  • miglitol
  • miglitol
  • miglitol
  • miglitol
  • miglitol
  • miglitol
  • miglitol
  • miglitol
  • miglitol
  • miglitol
  • miglitol, 4-methylbenzenesulfonate salt, ((d)-isomer)
  • miglitolum
  • miglitolum
  • n-hydroxyethyl-1-desoxynojirimycin
  • n-hydroxyethyl-1-desoxy-nojirimycin
  • plumarol
  • sanofi-synthelabo brand of miglitol
  • seibule

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT02954692Phase 4Nov 30, 2016Sanofi
NCT02730377Phase 4Mar 28, 2016Novo Nordisk
NCT01595893Phase 3Apr 1, 2012Austrian Science Fund (FWF), Medical University of Graz
NCT01099839Phase 1Feb 1, 2010Astellas
NCT00366470Phase 3Nov 1, 2009Christian Medical College, Vellore, India, Dalhousie University
NCT00419068Phase 3Jan 1, 2007Barts & The London NHS Trust, British Lung Foundation, University of London
NCT00380822Phase 3Sep 25, 2006Sanwa Kagaku Kenkyusho Co., Ltd.
NCT00334503Phase 3Jun 5, 2006Sanwa Kagaku Kenkyusho Co., Ltd.
NCT00334399Phase 3May 26, 2006Sanwa Kagaku Kenkyusho Co., Ltd.
NCT00213070Phase 3Sep 13, 2005Sanwa Kagaku Kenkyusho Co., Ltd.
NCT00213122Phase 3Sep 13, 2005Sanwa Kagaku Kenkyusho Co., Ltd.
NCT00213109Phase 3Sep 13, 2005Sanwa Kagaku Kenkyusho Co., Ltd.
Showing 12 of 12 trials
Page 1 / 1

Organizations

Research & Development (11)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Sanwa Kagaku Kenkyusho Co., Ltd.For profit6612005
AstellasFor profit1112010
Austrian Science Fund (FWF)Government1012012
Barts & The London NHS TrustAcademic/Hospital1112007
British Lung FoundationAcademic/Hospital1012007
Christian Medical College, Vellore, IndiaAcademic/Hospital1112009
Dalhousie UniversityAcademic/Hospital1012009
Medical University of GrazAcademic/Hospital1112012
Novo NordiskFor profit1112016
SanofiFor profit1112016
University of LondonAcademic/Hospital1012007
11 organizations
Page 1 / 1

Marketing (6)

OrganizationOrg typeRelationshipDate
Orient Pharma Co., Ltd.For profitMKTGFeb 24, 2015
Orient Pharma Co., Ltd.For profitSYNFeb 24, 2015
PfizerFor profitMKTGDec 18, 1996
PfizerFor profitNDA2Dec 18, 1996
Pharmacia & UpjohnFor profitNDADec 18, 1996
Westminster PharmsFor profitMKTGFeb 24, 2015