Acarbose
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Also known as BAY-G 5421AcarbosaBAY G 5421BAY-G-5421GlucobayNSC-758915PrecoseSID26719884SID144205150SID170464784C0164420
Summary
Acarbose (CHEMBL404271) is an approved oligosaccharide EC 3.2.1.20 (α-glucosidase) inhibitor (ATC A10BF01) targeting AMY2A and MGAM; indicated across 15 conditions including diabetes mellitus and type 2 diabetes mellitus.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Oligosaccharide
- ATC class: A10BF01
- Targets: 2 (AMY2A, MGAM)
- Indications: 15 conditions
- Clinical trials: 73
- Chemistry: 645.6 Da · C25H43NO18
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL404271 |
| Name | Acarbose |
| Type | Oligosaccharide |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 41774 |
| ChEBI | CHEBI:2376 |
| ATC | A10BF01 |
| Molecular formula | C25H43NO18 |
| Molecular weight | 645.6 |
| InChIKey | XUFXOAAUWZOOIT-UGEKTDRHSA-N |
SMILES: C[C@@H]1[C@H]([C@@H]([C@H]([C@H](O1)O[C@@H]2[C@H](O[C@@H]([C@@H]([C@H]2O)O)O[C@@H]3[C@H](OC([C@@H]([C@H]3O)O)O)CO)CO)O)O)N[C@H]4C=C([C@H]([C@@H]([C@H]4O)O)O)CO
IUPAC name: (3R,4R,5S,6R)-5-[(2R,3R,4R,5S,6R)-5-[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)cyclohex-2-en-1-yl]amino]oxan-2-yl]oxy-3,4-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-6-(hydroxymethyl)oxane-2,3,4-triol
ChEBI definition: A tetrasaccharide derivative consisting of a dideoxy-4-{[4,5,6-trihydroxy-3-(hydroxymethyl)cyclohex-2-en-1-yl C7 cyclitol moiety [called valienol (or valienamine)] linked via nitrogen to isomaltotriose.
Pharmacological roles (ChEBI): EC 3.2.1.20 (α-glucosidase) inhibitor, EC 3.2.1.1 (α-amylase) inhibitor, hypoglycemic agent, geroprotector.
Also known as: BAY-G 5421, Acarbosa, Acarbose, BAY G 5421, BAY-G-5421, Glucobay, NSC-758915, Precose, acarbose, SID26719884, ACARBOSE, SID144205150
Patent coverage: 10 distinct patent families (16 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 |
|---|---|---|---|---|---|
| AMY2A | amylase alpha 2A | Inhibition | 4.45 | 19.2% | P04746 |
| MGAM | maltase-glucoamylase | Inhibition | 8.05 | 0.1% | O43451 |
Broader ChEMBL bioactivity targets: 15 (assay-derived). Sample: Pancreatic alpha-amylase, Maltase-glucoamylase, Cannabinoid receptor 1, Prostaglandin G/H synthase 1, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A, Alpha-amylase 1A, 3’,5’-cyclic-AMP phosphodiesterase 4A, Lysosomal alpha-glucosidase, Sucrase-isomaltase, intestinal, Lysosomal alpha-glucosidase.
Bioactivity
ChEMBL activities: 63 potent at pChembl ≥ 5 of 112 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| AMY1A | 6.92 | IC50 | 120 | nM | CHEMBL_ACT_25045862 |
| Q6P7A9 | 6.8 | IC50 | 160 | nM | CHEMBL_ACT_5140282 |
| Q6P7A9 | 6.75 | IC50 | 180 | nM | CHEMBL_ACT_12148407 |
| Q6P7A9 | 6.75 | IC50 | 180 | nM | CHEMBL_ACT_15063066 |
| AMY1A | 6.68 | IC50 | 210 | nM | CHEMBL_ACT_25086292 |
| Q6P7A9 | 6.46 | IC50 | 350 | nM | CHEMBL_ACT_2556845 |
| P23739 | 6.4 | IC50 | 400 | nM | CHEMBL_ACT_13406432 |
| MGAM | 6.38 | IC50 | 421 | nM | CHEMBL_ACT_25834363 |
| AMY1A | 6.37 | IC50 | 430 | nM | CHEMBL_ACT_26039070 |
| MGAM | 6.36 | Ki | 440 | nM | CHEMBL_ACT_25077848 |
| AMY1A | 6.3 | IC50 | 500 | nM | CHEMBL_ACT_15725517 |
| P23739 | 6.25 | IC50 | 560 | nM | CHEMBL_ACT_2556867 |
| AMY1A | 6.18 | IC50 | 660 | nM | CHEMBL_ACT_26117833 |
| AMY1A | 6 | IC50 | 996 | nM | CHEMBL_ACT_2347277 |
| P07265 | 5.97 | IC50 | 1060 | nM | CHEMBL_ACT_25613039 |
| P07265 | 5.95 | IC50 | 1120 | nM | CHEMBL_ACT_25613134 |
| P00690 | 5.87 | IC50 | 1353 | nM | CHEMBL_ACT_18685894 |
| AMY1A | 5.84 | IC50 | 1460 | nM | CHEMBL_ACT_18547888 |
| AMY1A | 5.84 | IC50 | 1460 | nM | CHEMBL_ACT_18774917 |
| Q6P7A9 | 5.82 | IC50 | 1500 | nM | CHEMBL_ACT_13413430 |
| P23739 | 5.82 | IC50 | 1500 | nM | CHEMBL_ACT_6176796 |
| Q6P7A9 | 5.82 | IC50 | 1500 | nM | CHEMBL_ACT_8030755 |
| AMY1A | 5.81 | IC50 | 1560 | nM | CHEMBL_ACT_25601517 |
| P00690 | 5.78 | IC50 | 1660 | nM | CHEMBL_ACT_23172320 |
| P23739 | 5.77 | IC50 | 1700 | nM | CHEMBL_ACT_25063533 |
| P07265 | 5.77 | IC50 | 1700 | nM | CHEMBL_ACT_25612879 |
| P23739 | 5.77 | IC50 | 1700 | nM | CHEMBL_ACT_5245462 |
| Q6P7A9 | 5.77 | IC50 | 1700 | nM | CHEMBL_ACT_6164309 |
| Q6P7A9 | 5.77 | IC50 | 1700 | nM | CHEMBL_ACT_6176788 |
| P23739 | 5.77 | IC50 | 1700 | nM | CHEMBL_ACT_8009273 |
Target pathways
Aggregated over 2 target gene(s): AMY2A, MGAM.
Top Reactome pathways
9 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Digestion of dietary carbohydrate | 2 | AMY2A, MGAM |
| Digestion | 2 | AMY2A, MGAM |
| Digestion and absorption | 2 | AMY2A, MGAM |
| Developmental Biology | 1 | AMY2A |
| Innate Immune System | 1 | MGAM |
| Immune System | 1 | MGAM |
| Neutrophil degranulation | 1 | MGAM |
| Developmental Cell Lineages | 1 | AMY2A |
| Developmental Lineage of Pancreatic Acinar Cells | 1 | AMY2A |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| carbohydrate metabolic process | 2 |
| carbohydrate catabolic process | 1 |
| polysaccharide digestion | 1 |
| maltose catabolic process | 1 |
| starch catabolic process | 1 |
| dextrin catabolic process | 1 |
| disaccharide catabolic process | 1 |
Indications & clinical
Indications
15 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 |
| metabolic syndrome X | 3 | MONDO:0011565 | EFO:0000195 |
| gestational diabetes | 3 | MONDO:0005406 | EFO:0004593 |
| hypertensive disorder | 3 | MONDO:0005044 | EFO:0000537 |
| atherosclerosis | 3 | MONDO:0005311 | EFO:0003914 |
| metabolic disease | 3 | MONDO:0005066 | EFO:0000589 |
| coronary artery disorder | 3 | MONDO:0005010 | EFO:0001645 |
| metabolic dysfunction-associated steatotic liver disease | 2 | MONDO:0013209 | EFO:0003095 |
| kidney cancer | 2 | MONDO:0002367 | MONDO:0002367 |
| orthostatic hypotension | 1 | MONDO:0005469 | EFO:0005252 |
| hyperinsulinemic hypoglycemia | 1 | MONDO:0005803 | EFO:0007318 |
| obesity disorder | 1 | MONDO:0011122 | EFO:0001073 |
2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 73.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 36 |
| PHASE3 | 13 |
| Not specified | 11 |
| PHASE2 | 7 |
| PHASE1 | 6 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00417729 | PHASE4 | COMPLETED | Effects of Acarbose Versus Glibenclamide on MAGE and Oxidative Stress in Patients With Type 2 DM |
| NCT00437918 | PHASE4 | COMPLETED | The Effects of Nateglinide and Acarbose on the Post-Prandial Glucose Control in Type 2 Diabetic Patients |
| NCT00829660 | PHASE4 | COMPLETED | Acarbose Cardiovascular Evaluation Trial |
| NCT00846521 | PHASE4 | TERMINATED | Study of Post-meal Blood Sugar Peaks in Association With Vascular Disease in Childhood Obesity |
| NCT00858676 | PHASE4 | UNKNOWN | Impact of Acarbose on Abnormal Glucose Regulation in Patients With Coronary Artery Disease (AAA Trial) |
| NCT00928889 | PHASE4 | COMPLETED | Effects of Nateglinide vs Acarbose on Postprandial Glucose Fluctuation, Dyslipidemia, and Inflammatory Factors |
| NCT01025765 | PHASE4 | UNKNOWN | The Effects of Oral Hypoglycemic Agents on Chronic Hepatitis C Patients Receiving Peg-Intron Plus Ribavirin |
| NCT01030952 | PHASE4 | COMPLETED | Effects of Nateglinide on Postprandial Glucose Excursion by Restoring Early Phase Insulin Secretion |
| NCT01175486 | PHASE4 | UNKNOWN | Thiazolidinedione (TZD) on the Diabetic Retinopathy and Nephropathy |
| NCT01181674 | PHASE4 | COMPLETED | Remission Evaluation of Metabolic Interventions in Type 2 Diabetes (REMIT Pilot Trial) |
| NCT01244971 | PHASE4 | COMPLETED | Exercise and Acarbose in Type 2 Diabetes |
| NCT01279512 | PHASE4 | COMPLETED | Metformin Versus Acarbose Treatment in Infertile Overweight Women With Polycystic Ovary Syndrome (PCOS) |
| NCT01470937 | PHASE4 | COMPLETED | Early Diabetes Intervention Program |
| NCT01490918 | PHASE4 | COMPLETED | Study to Evaluate the Efficacy of Acarbose,Metformin,Sitagliptin Combination Treatment in DM Patients |
| NCT01709305 | PHASE4 | COMPLETED | A Study of the Safety and Efficacy of Glimepiride, Gliclazide, Repaglinide or Acarbose When Added to Sitagliptin + Metformin Combination Therapy in Chinese Participants With Diabetes (MK-0431-313) |
| NCT01758471 | PHASE4 | UNKNOWN | Efficacy of Acarbose on Intestinal Microbiome and Incretins of Type 2 Diabetes |
| NCT01863147 | PHASE4 | COMPLETED | Sitagliptin Reduces Left Ventricular Mass in Normotensive Type 2 Diabetic Patients With Coronary Artery Disease |
| NCT02049814 | PHASE4 | COMPLETED | Efficacy and Safety of Voglibose Compared With Acarbose in Participants With Type 2 Diabetes |
| NCT02072096 | PHASE4 | TERMINATED | A Comparison of Two Treatment Strategies in Older Participants With Type 2 Diabetes Mellitus (T2DM) |
| NCT02143765 | PHASE4 | COMPLETED | Efficacy and Safety of Mitiglinide vs Acarbose in Patients With Type 2 Diabetes Mellitus |
| NCT02243176 | PHASE4 | COMPLETED | 24-Week, Multicenter, Randomized, Parallel-group, Open-label, Active Controlled Phase IV Study to Assess the Efficacy, Safety and Tolerability of Saxagliptin Compared With Acarbose When in Combination With Metformin in Patients With T2D Inadequately Controlled With Metformin Monotherapy |
| NCT02355509 | PHASE4 | COMPLETED | Effect of Acarbose on Postprandial Lipoprotein Levels in Glucose Intolerant Patients |
| NCT02438397 | PHASE4 | UNKNOWN | the Efficacy of Acarbose and Metformin on Blood Glucose Fluctuation When Combined With Premix Insulin |
| NCT02500329 | PHASE4 | UNKNOWN | Effect of Gemigliptin or Acarbose on Endothelial Function in Type 2 DM Patients |
| NCT02527993 | PHASE4 | COMPLETED | Treatment of Hypoglycemia Following Gastric Bypass Surgery |
| NCT02589353 | PHASE4 | COMPLETED | Human Oral Detection of Glucose Olygomers |
| NCT02605772 | PHASE4 | UNKNOWN | Safety and Efficacy of Acarbose+Saxagliptin Compared With Metformin+Saxagliptin in Patients With Type 2 Diabetes |
| NCT02836704 | PHASE4 | COMPLETED | Comparison of Standard vs Higher Starting Dose of Insulin Glargine in Chinese Patients With Type 2 Diabetes (Glargine Starting Dose) |
| NCT02999841 | PHASE4 | UNKNOWN | Effect of Acarbose and Vildagliptin on Visceral Fat Distribution in Newly Diagnosed Type 2 Diabetes Patients |
| NCT03344341 | PHASE4 | TERMINATED | A Phase IV Study in Drug-Naive Patients With T2DM in China |
| NCT03359837 | PHASE4 | COMPLETED | Comparison of Two Treatment Regimens in Patients With Type 2 Diabetes After Short-term Intensive Insulin Therapy |
| NCT03383068 | PHASE4 | UNKNOWN | Research of Intensive Metabolic Intervention Before Pregnancy in PCOS |
| NCT03602638 | PHASE4 | UNKNOWN | Effects of a Dipeptidyl Peptidase-4 Inhibitor Sitagliptininsulin on the Progression of Coronary Atherosclerosis in Patients With Type 2 Diabetes |
| NCT03794336 | PHASE4 | COMPLETED | Efficacy and Safety of Alogliptin vs. Acarbose in Chinese Type 2 Diabetes Mellitus (T2DM) Patients With High CV Risk or CHD Treated With Aspirin and Inadequately Controlled With Metformin Monotherapy or Drug Naive |
| NCT04287387 | PHASE4 | UNKNOWN | Response of Gut Microbiota in Type 2 Diabetes to Hypoglycemic Agents |
| NCT05542849 | PHASE4 | COMPLETED | The Efficacy and Tolerability of Acarbose in Healthy Individuals |
| NCT00221156 | PHASE3 | COMPLETED | Acarbose and Secondary Prevention After Coronary Stenting |
| NCT00551954 | PHASE3 | COMPLETED | Effects of Acarbose on Endothelial Function After a Mixed Meal in Newly Diagnosed Type 2 Diabetes |
| NCT00558883 | PHASE3 | COMPLETED | AI(I)DA Acarbose and the Subclinical Inflammation |
| NCT00629213 | PHASE3 | COMPLETED | Metabolic Syndrome Risk Factor in IGT: STOP-NIDDM Trial |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
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.
10 molecules share ≥1 primary target. Top 10 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| MIGALASTAT | ChEMBL | Phase 4 (approved) | MGAM |
| MIGLITOL | ChEMBL | Phase 4 (approved) | MGAM |
| MIGLUSTAT | ChEMBL | Phase 4 (approved) | MGAM |
| VOGLIBOSE | ChEMBL | Phase 4 (approved) | MGAM |
| LUCERASTAT | ChEMBL | Phase 3 | MGAM |
| QUERCETIN | ChEMBL | Phase 3 | MGAM |
| THIAZOLIDINEDIONE | ChEMBL | Phase 3 | MGAM |
| DUVOGLUSTAT | ChEMBL | Phase 2 | MGAM |
| GENISTEIN | ChEMBL | Phase 2 | MGAM |
| ascorbic acid | PubChem | Approved | AMY2A |
Related Atlas pages
- Genes: AMY2A, MGAM
- Diseases: diabetes mellitus, type 2 diabetes mellitus, metabolic syndrome X, gestational diabetes, hypertensive disorder, atherosclerosis, metabolic disease, coronary artery disorder
- Drugs: Migalastat, Miglitol, Miglustat, Voglibose, Lucerastat, Quercetin, Thiazolidinedione, ascorbic acid