Miglitol
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Also known as BAY M 1099BAY-M-1099DiastabolGlysetNSC-758702SID26719889SID49681630SID144204989SID170465326C0164417
Summary
Miglitol (CHEMBL1561) is an approved small molecule (ATC A10BF02) targeting GAA and MGAM; indicated across 3 conditions including diabetes mellitus and type 2 diabetes mellitus.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: A10BF02
- Targets: 2 (GAA, MGAM)
- Indications: 3 conditions
- Clinical trials: 7
- Chemistry: 207.22 Da · C8H17NO5
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1561 |
| Name | Miglitol |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 441314 |
| ATC | A10BF02 |
| Molecular formula | C8H17NO5 |
| Molecular weight | 207.22 |
| InChIKey | IBAQFPQHRJAVAV-ULAWRXDQSA-N |
SMILES: C1[C@@H]([C@H]([C@@H]([C@H](N1CCO)CO)O)O)O
IUPAC name: (2R,3R,4R,5S)-1-(2-hydroxyethyl)-2-(hydroxymethyl)piperidine-3,4,5-triol
Also known as: BAY M 1099, BAY-M-1099, Diastabol, Glyset, Miglitol, NSC-758702, miglitol, SID26719889, SID49681630, MIGLITOL, SID144204989, SID170465326
Patent coverage: 7,002 distinct patent families (29,089 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| GAA | alpha glucosidase | Inhibition | 6.46 | 0.4% | P10253 |
| MGAM | maltase-glucoamylase | Inhibition | 6 | 0.1% | O43451 |
Broader ChEMBL bioactivity targets: 12 (assay-derived). Sample: Lactase/phlorizin hydrolase, Maltase-glucoamylase, Lysosomal acid glucosylceramidase, Lysosomal alpha-glucosidase, Sucrase-isomaltase, intestinal, Sucrase-isomaltase, intestinal, Alpha-mannosidase, Alpha-glucosidase, Beta-galactosidase, Lysosomal alpha-glucosidase.
Bioactivity
ChEMBL activities: 25 potent at pChembl ≥ 5 of 34 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| P23739 | 6.96 | IC50 | 110 | nM | CHEMBL_ACT_2556870 |
| GAA | 6.46 | IC50 | 350 | nM | CHEMBL_ACT_2556884 |
| P35574 | 6.41 | IC50 | 390 | nM | CHEMBL_ACT_2556914 |
| P23739 | 6.37 | IC50 | 430 | nM | CHEMBL_ACT_16616228 |
| Q6P7A9 | 6.34 | Ki | 460 | nM | CHEMBL_ACT_12146623 |
| SI | 6.3 | IC50 | 500 | nM | CHEMBL_ACT_3204029 |
| Q6P7A9 | 6.23 | IC50 | 590 | nM | CHEMBL_ACT_5140284 |
| P23739 | 6 | IC50 | 1000 | nM | CHEMBL_ACT_12146689 |
| P23739 | 6 | IC50 | 1000 | nM | CHEMBL_ACT_15063089 |
| GAA | 6 | IC50 | 1000 | nM | CHEMBL_ACT_2556929 |
| MGAM | 6 | Ki | 1000 | nM | CHEMBL_ACT_3558642 |
| P23739 | 6 | IC50 | 1000 | nM | CHEMBL_ACT_5140317 |
| P23739 | 5.92 | IC50 | 1200 | nM | CHEMBL_ACT_2556856 |
| Q6P7A9 | 5.89 | IC50 | 1300 | nM | CHEMBL_ACT_12146671 |
| Q6P7A9 | 5.89 | IC50 | 1300 | nM | CHEMBL_ACT_15063068 |
| Q6P7A9 | 5.89 | IC50 | 1300 | nM | CHEMBL_ACT_2556848 |
| GAA | 5.7 | IC50 | 2000 | nM | CHEMBL_ACT_3204093 |
| GAA | 5.65 | Potency | 2239 | nM | CHEMBL_ACT_4402794 |
| GAA | 5.65 | Potency | 2239 | nM | CHEMBL_ACT_4926246 |
| GAA | 5.45 | Potency | 3548 | nM | CHEMBL_ACT_4980995 |
| GAA | 5.45 | Potency | 3548 | nM | CHEMBL_ACT_5026073 |
| MGAM | 5.43 | IC50 | 3700 | nM | CHEMBL_ACT_16616252 |
| MGAM | 5.43 | IC50 | 3700 | nM | CHEMBL_ACT_22445279 |
| P23739 | 5.34 | IC50 | 4600 | nM | CHEMBL_ACT_16616239 |
| MGAM | 5.22 | IC50 | 6000 | nM | CHEMBL_ACT_3204042 |
Target pathways
Aggregated over 2 target gene(s): GAA, MGAM.
Top Reactome pathways
15 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Innate Immune System | 2 | GAA, MGAM |
| Immune System | 2 | GAA, MGAM |
| Neutrophil degranulation | 2 | GAA, MGAM |
| Metabolism | 1 | GAA |
| Disease | 1 | GAA |
| Digestion of dietary carbohydrate | 1 | MGAM |
| Glycogen storage diseases | 1 | GAA |
| Glycogen storage disease type II (GAA) | 1 | GAA |
| Diseases of carbohydrate metabolism | 1 | GAA |
| Diseases of metabolism | 1 | GAA |
| Glycogen breakdown (glycogenolysis) | 1 | GAA |
| Metabolism of carbohydrates and carbohydrate derivatives | 1 | GAA |
| Digestion | 1 | MGAM |
| Digestion and absorption | 1 | MGAM |
| Glycogen metabolism | 1 | GAA |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| carbohydrate metabolic process | 2 |
| maltose metabolic process | 1 |
| regulation of the force of heart contraction | 1 |
| diaphragm contraction | 1 |
| heart morphogenesis | 1 |
| glycogen catabolic process | 1 |
| sucrose metabolic process | 1 |
| glucose metabolic process | 1 |
| lysosome organization | 1 |
| locomotory behavior | 1 |
| tissue development | 1 |
| aorta development | 1 |
| obsolete vacuolar sequestering | 1 |
| muscle cell cellular homeostasis | 1 |
| neuromuscular process controlling posture | 1 |
Indications & clinical
Indications
3 indications (2 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| diabetes mellitus | 4 | MONDO:0005015 | EFO:0000400 |
| type 2 diabetes mellitus | 4 | MONDO:0005148 | MONDO:0005148 |
| type 1 diabetes mellitus | 3 | MONDO:0005147 | MONDO:0005147 |
Clinical trials
Total trials: 7.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 6 |
| PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00213070 | PHASE3 | COMPLETED | Double-Blind Trial of Miglitol in Type 2 Diabetic Patients With Insulin Treatment |
| NCT00213109 | PHASE3 | COMPLETED | Open Trial of Miglitol in Type 1 Diabetic Patients With Insulin Treatment |
| NCT00213122 | PHASE3 | COMPLETED | Effects of Miglitol on Daily Plasma Glucose in type2 Diabetes Treated With Insulin |
| NCT00334399 | PHASE3 | COMPLETED | Double-Blind Trial of Miglitol in Type 2 Diabetic Patients Treated With Biguanide |
| NCT00334503 | PHASE3 | COMPLETED | Open Trial of Miglitol in Type 2 Diabetic Patients Treated With Biguanide |
| NCT00380822 | PHASE3 | COMPLETED | Double-Blind Study of Miglitol in Japanese With type2 Diabetes |
| NCT01099839 | PHASE1 | COMPLETED | A Study to Assess Drug-Drug Interaction Between ASP1941 and Miglitol |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
109 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| ACARBOSE | ChEMBL | Phase 4 (approved) | GAA, MGAM |
| MIGALASTAT | ChEMBL | Phase 4 (approved) | GAA, MGAM |
| MIGLUSTAT | ChEMBL | Phase 4 (approved) | GAA, MGAM |
| VOGLIBOSE | ChEMBL | Phase 4 (approved) | GAA, MGAM |
| LUCERASTAT | ChEMBL | Phase 3 | GAA, MGAM |
| QUERCETIN | ChEMBL | Phase 3 | GAA, MGAM |
| THIAZOLIDINEDIONE | ChEMBL | Phase 3 | GAA, MGAM |
| DUVOGLUSTAT | ChEMBL | Phase 2 | GAA, MGAM |
| ACRISORCIN | ChEMBL | Phase 4 (approved) | GAA |
| ALFUZOSIN | ChEMBL | Phase 4 (approved) | GAA |
| AMILORIDE | ChEMBL | Phase 4 (approved) | GAA |
| AMLEXANOX | ChEMBL | Phase 4 (approved) | GAA |
| APOMORPHINE | ChEMBL | Phase 4 (approved) | GAA |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | GAA |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | GAA |
| BETAXOLOL | ChEMBL | Phase 4 (approved) | GAA |
| CARBARIL | ChEMBL | Phase 4 (approved) | GAA |
| CARVEDILOL | ChEMBL | Phase 4 (approved) | GAA |
| CHLORPROMAZINE | ChEMBL | Phase 4 (approved) | GAA |
| CHLORTETRACYCLINE | ChEMBL | Phase 4 (approved) | GAA |
| CINNARIZINE | ChEMBL | Phase 4 (approved) | GAA |
| DEFEROXAMINE | ChEMBL | Phase 4 (approved) | GAA |
| DEMECLOCYCLINE | ChEMBL | Phase 4 (approved) | GAA |
| DIBUCAINE | ChEMBL | Phase 4 (approved) | GAA |
| DICLOFENAC | ChEMBL | Phase 4 (approved) | GAA |
| DIENESTROL | ChEMBL | Phase 4 (approved) | GAA |
| DIPYRIDAMOLE | ChEMBL | Phase 4 (approved) | GAA |
| DITHIAZANINE IODIDE | ChEMBL | Phase 4 (approved) | GAA |
| DOPAMINE | ChEMBL | Phase 4 (approved) | GAA |
| DOXAZOSIN | ChEMBL | Phase 4 (approved) | GAA |
| DULOXETINE | ChEMBL | Phase 4 (approved) | GAA |
| ECONAZOLE NITRATE | ChEMBL | Phase 4 (approved) | GAA |
| EDARAVONE | ChEMBL | Phase 4 (approved) | GAA |
| EPINEPHRINE BITARTRATE | ChEMBL | Phase 4 (approved) | GAA |
| FELBINAC | ChEMBL | Phase 4 (approved) | GAA |
| FLUOROMETHOLONE | ChEMBL | Phase 4 (approved) | GAA |
| FLUSPIRILENE | ChEMBL | Phase 4 (approved) | GAA |
| FOLIC ACID | ChEMBL | Phase 4 (approved) | GAA |
| INDAPAMIDE | ChEMBL | Phase 4 (approved) | GAA |
| INDOPROFEN | ChEMBL | Phase 4 (approved) | GAA |
| IRBESARTAN | ChEMBL | Phase 4 (approved) | GAA |
| ISOETHARINE | ChEMBL | Phase 4 (approved) | GAA |
| ISOPROTERENOL | ChEMBL | Phase 4 (approved) | GAA |
| LABETALOL | ChEMBL | Phase 4 (approved) | GAA |
| LANSOPRAZOLE | ChEMBL | Phase 4 (approved) | GAA |
| MAPROTILINE | ChEMBL | Phase 4 (approved) | GAA |
| MECLOFENAMATE | ChEMBL | Phase 4 (approved) | GAA |
| MENADIONE | ChEMBL | Phase 4 (approved) | GAA |
| METHYLDOPA | ChEMBL | Phase 4 (approved) | GAA |
| METHYSERGIDE | ChEMBL | Phase 4 (approved) | GAA |
| MICONAZOLE NITRATE | ChEMBL | Phase 4 (approved) | GAA |
| MORICIZINE | ChEMBL | Phase 4 (approved) | GAA |
| NIACIN | ChEMBL | Phase 4 (approved) | GAA |
| OLANZAPINE | ChEMBL | Phase 4 (approved) | GAA |
| OXYTETRACYCLINE | ChEMBL | Phase 4 (approved) | GAA |
| PHENELZINE | ChEMBL | Phase 4 (approved) | GAA |
| PHENYLEPHRINE | ChEMBL | Phase 4 (approved) | GAA |
| PRAZOSIN | ChEMBL | Phase 4 (approved) | GAA |
| PRILOCAINE | ChEMBL | Phase 4 (approved) | GAA |
| PROCHLORPERAZINE | ChEMBL | Phase 4 (approved) | GAA |
Related Atlas pages
- Genes: GAA, MGAM
- Diseases: diabetes mellitus, type 2 diabetes mellitus, type 1 diabetes mellitus
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