miglitol
Trade name: glyset
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
Earliest trial started Sep 13, 2005 (NCT00213109)
Timeline
1990s
- Dec 18, 1996
Pharmacia & Upjohn — Earliest FDA Approval
- Dec 18, 1996
Pfizer — Marketing Organization
- Dec 18, 1996
Pharmacia & Upjohn — NDA Organization
- Dec 18, 1996
Pfizer — NDA Secondary Org
2000s
- Jan 1, 2005
Earliest Phase 3 Sponsor(trial)
2010s
- Jan 1, 2010
Earliest Phase 1 Sponsor(trial)
- Feb 24, 2015
Westminster Pharms — Marketing Organization
- Feb 24, 2015
Orient Pharma Co., Ltd. — Marketing Organization
Indications
Approved for
Mechanism of action
- Lysosomal alpha-glucosidaseINHIBITOR
GAA inhibitor
- Maltase-glucoamylaseINHIBITOR
MGAM inhibitor
Approval history
- approvedDec 18, 1996
Chemistry & pharmacology
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
- WikipediaMiglitol ↗
- NCATS0V5436JAQW ↗
- ChEMBLCHEMBL1561 ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02954692 | Phase 4 | Nov 30, 2016 | Sanofi |
| NCT02730377 | Phase 4 | Mar 28, 2016 | Novo Nordisk |
| NCT01595893 | Phase 3 | Apr 1, 2012 | Austrian Science Fund (FWF), Medical University of Graz |
| NCT01099839 | Phase 1 | Feb 1, 2010 | Astellas |
| NCT00366470 | Phase 3 | Nov 1, 2009 | Christian Medical College, Vellore, India, Dalhousie University |
| NCT00419068 | Phase 3 | Jan 1, 2007 | Barts & The London NHS Trust, British Lung Foundation, University of London |
| NCT00380822 | Phase 3 | Sep 25, 2006 | Sanwa Kagaku Kenkyusho Co., Ltd. |
| NCT00334503 | Phase 3 | Jun 5, 2006 | Sanwa Kagaku Kenkyusho Co., Ltd. |
| NCT00334399 | Phase 3 | May 26, 2006 | Sanwa Kagaku Kenkyusho Co., Ltd. |
| NCT00213070 | Phase 3 | Sep 13, 2005 | Sanwa Kagaku Kenkyusho Co., Ltd. |
| NCT00213122 | Phase 3 | Sep 13, 2005 | Sanwa Kagaku Kenkyusho Co., Ltd. |
| NCT00213109 | Phase 3 | Sep 13, 2005 | Sanwa Kagaku Kenkyusho Co., Ltd. |
Organizations
Research & Development (11)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Sanwa Kagaku Kenkyusho Co., Ltd. | For profit | 6 | 6 | 1 | 2005 |
| Astellas | For profit | 1 | 1 | 1 | 2010 |
| Austrian Science Fund (FWF) | Government | 1 | 0 | 1 | 2012 |
| Barts & The London NHS Trust | Academic/Hospital | 1 | 1 | 1 | 2007 |
| British Lung Foundation | Academic/Hospital | 1 | 0 | 1 | 2007 |
| Christian Medical College, Vellore, India | Academic/Hospital | 1 | 1 | 1 | 2009 |
| Dalhousie University | Academic/Hospital | 1 | 0 | 1 | 2009 |
| Medical University of Graz | Academic/Hospital | 1 | 1 | 1 | 2012 |
| Novo Nordisk | For profit | 1 | 1 | 1 | 2016 |
| Sanofi | For profit | 1 | 1 | 1 | 2016 |
| University of London | Academic/Hospital | 1 | 0 | 1 | 2007 |
Marketing (6)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Orient Pharma Co., Ltd. | For profit | MKTG | Feb 24, 2015 |
| Orient Pharma Co., Ltd. | For profit | SYN | Feb 24, 2015 |
| Pfizer | For profit | MKTG | Dec 18, 1996 |
| Pfizer | For profit | NDA2 | Dec 18, 1996 |
| Pharmacia & Upjohn | For profit | NDA | Dec 18, 1996 |
| Westminster Pharms | For profit | MKTG | Feb 24, 2015 |