Glimepiride

Summary

Glimepiride (CHEMBL1481) is an approved small-molecule hypoglycemic agent (ATC A10BB12); indicated across 7 conditions including diabetes mellitus and type 2 diabetes mellitus.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A10BB12
• Indications: 7 conditions
• Clinical trials: 183
• Chemistry: 490.6 Da · C24H34N4O5S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1481
Name	Glimepiride
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	3476
ChEBI	CHEBI:5383
ATC	A10BB12
Molecular formula	C24H34N4O5S
Molecular weight	490.6
InChIKey	WIGIZIANZCJQQY-UHFFFAOYSA-N

SMILES: CCC1=C(CN(C1=O)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCC(CC3)C)C

IUPAC name: 4-ethyl-3-methyl-N-[2-[4-[(4-methylcyclohexyl)carbamoylsulfamoyl]phenyl]ethyl]-5-oxo-2H-pyrrole-1-carboxamide

Pharmacological roles (ChEBI): hypoglycemic agent, insulin secretagogue.

Also known as: Amaryl, Glimepirida, Glimepiride, Glimepiride component of avandaryl, Glimepiride component of duetact, HOE 490, HOE-490, Niddaryl, NSC-759809, glimepiride, SID26755029, GLIMEPIRIDE

Patent coverage: 8,319 distinct patent families (33,335 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

Broader ChEMBL bioactivity targets: 10 (assay-derived). Sample: Nuclear receptor ROR-gamma, Fructose-bisphosphate aldolase, ATP-binding cassette sub-family C member 4, Thromboxane A2 receptor, Menin/Histone-lysine N-methyltransferase MLL, Aldo-keto reductase family 1 member C3, Nuclear receptor subfamily 1 group I member 3, Aldo-keto reductase family 1 member C1, ATP-binding cassette sub-family C member 3, Bile salt export pump.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 13 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
AKR1C3	6.07	IC50	850	nM	CHEMBL_ACT_22396349
ABCC3	5.19	IC50	6390	nM	CHEMBL_ACT_18130190
AKR1C1	5.16	IC50	6860	nM	CHEMBL_ACT_22396353
P51450	5	Potency	10000	nM	CHEMBL_ACT_4802352

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

7 indications (3 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	Orphanet:552
hypertensive disorder	3	MONDO:0005044	EFO:0000537
atherosclerosis	3	MONDO:0005311	EFO:0003914
coronary artery disorder	3	MONDO:0005010	EFO:0001645

2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 183.

Phase distribution

Phase	Trials
PHASE3	71
PHASE4	61
Not specified	20
PHASE1	19
PHASE2	9
PHASE2/PHASE3	3

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07365358	PHASE4	NOT_YET_RECRUITING	Evaluate the Efficacy and Safety of Empagliflozin or Glimepiride Combination Therapy in Type 2 Diabetes Mellitus Patients
NCT00318656	PHASE4	COMPLETED	24-Hour Glycemia: Rosiglitazone Versus Glimepiride In Type 2 Diabetes
NCT00360698	PHASE4	COMPLETED	Insulin Glulisine in Type 2 Diabetic Patients
NCT00469092	PHASE4	COMPLETED	Comparison of Biphasic Insulin Aspart 30 Versus Insulin Glargine Both in Combination With Metformin and Glimepiride in Subjects With Type 2 Diabetes
NCT00562172	PHASE4	COMPLETED	Insulin Glargine (Lantus) vs Sulfonylurea (SU) for BETA Cell Function (BETA Study)
NCT00576784	PHASE4	COMPLETED	Metabolic Effects of Pioglitazone in Type II Diabetic Patients Previously Treated With Insulin
NCT00612144	PHASE4	COMPLETED	Study Comparing Efficacy and Safety of Amaryl M and Metformin Uptitraion to Type 2 DM
NCT00619697	PHASE4	COMPLETED	Efficacy and Safety of Biphasic Insulin Aspart 30 in Combination With Metformin in Type 2 Diabetes
NCT00633425	PHASE4	COMPLETED	Continuous Glucose Monitoring System (CGMS) in Type 2 Diabetic Patients Inadequately Controlled by Metformine Monotherapy; Analyze of Glycemic Profile Before and After Association of Glimepiride
NCT00642915	PHASE4	COMPLETED	Insulin Glargine Benefits in Japanese Pts Outside of Japan (US or Brazil)
NCT00699322	PHASE4	UNKNOWN	Effect of Dipeptidyl Peptidase-IV Inhibitor and Sulfonylurea on Glucose Variability and Oxidative Stress
NCT00708578	PHASE4	COMPLETED	Optimal Oral Hypoglycaemic Agents (OHA) for Combination With Insulin Glargine (Sulfonylurea vs. Metformin)
NCT00858013	PHASE4	COMPLETED	Study of the Durability of Glycemic Control With Nateglinide
NCT00908921	PHASE4	COMPLETED	Efficacy and Safety of Glimepiride as Oral Anti-Diabetic (OAD) Initiation Mono-therapy in Chinese Type 2 Diabetes Mellitus (T2DM)
NCT00913367	PHASE4	COMPLETED	Efficacy/Safety Study of Amaryl®M 1/500 mg Twice Daily Versus Amaryl® 4 mg Both in Combination With Lantus® in Type 2 Diabetes Mellitus
NCT00939939	PHASE4	TERMINATED	Effect of Sitagliptin on Postprandial Lipoprotein Metabolism
NCT00941161	PHASE4	COMPLETED	Effect of Oral Combination Therapy in a Single Dosage Form in Patients With Type 2 Diabetes Mellitus
NCT00949442	PHASE4	COMPLETED	Lantus Versus NPH: Comparison in Insulin Naive People Not Adequately Controlled With at Least One Oral Anti Diabetics (OAD) Treatment
NCT00957060	PHASE4	COMPLETED	Superiority of Glimepiride Over Sitagliptin in Naive Type 2 Diabetes Patients
NCT00993187	PHASE4	COMPLETED	Efficacy and Safety of Sitagliptin/Metformin Fixed-Dose Combination (FDC) Compared to Glimepiride in Participants With Type 2 Diabetes Mellitus (MK-0431A-202)
NCT01006603	PHASE4	COMPLETED	Saxagliptin Compared to Glimepiride in Elderly Type 2 Diabetes Patients, With Inadequate Glycemic Control on Metformin
NCT01123980	PHASE4	COMPLETED	Comparison of the Blood Sugar Lowering Effect of Biphasic Insulin Aspart 30 and Insulin Glargine Both Combined With Metformin and Glimepiride in Chinese and Japanese Subjects With Type 2 Diabetes New to Insulin Treatment
NCT01144728	PHASE4	COMPLETED	Initiation and Titration of Amaryl
NCT01204580	PHASE4	COMPLETED	ADIponectin and Asymmetric Dimethylarginine (ADMA) Level in Type-2 Diabetes Patients After 12 Weeks of Treatment With GlimepiRide And Metformin Fixed Dose Combination
NCT01341717	PHASE4	COMPLETED	Effects of Sitagliptin on Type 2 Diabetes Mellitus Patients on Treatment With Metformin and Insulin
NCT01429818	PHASE4	COMPLETED	Endothelial Disfunction Treatment With Glimepiride/Metformin Combination (Glimetal) in Type 2 Diabetes Patients
NCT01444248	PHASE4	COMPLETED	Compare the Compliance of Patients Treated With Once-daily (od) or Twice-daily (Bid) Glimepiride and Metformin Fixed Combination Therapy
NCT01509001	PHASE4	COMPLETED	Study of Metabolic and Haemodynamic Effects of Metformin and Glimepiride in Patients With Type 2 Diabetes Mellitus
NCT01547104	PHASE4	UNKNOWN	Effect of Linagliptin in Comparison With Glimepiride as Add on to Metformin on Postprandial Beta Cell Function, Postprandial Metabolism and Oxidative Stress in Patients With Type 2 Diabetes Mellitus
NCT01565096	PHASE4	UNKNOWN	Effect of Adding Vildagliptin on Beta Cell Function and Cardiovascular Risk Markers in Patients With Moderate Metabolic Control During Metformin Monotherapy
NCT01593137	PHASE4	WITHDRAWN	A Long-term Trial to Compare the Effects of Liraglutide and Sulphonylurea (Glimepiride) Both in Combination With Metformin on Clinical, Endothelial and Image Markers of Cardiovascular Risk in Patients With Type 2 Diabetes
NCT01660386	PHASE4	UNKNOWN	Study of Comparing the Different Effect of DPP-4 Inhibitors and Sulfonylurea by Using Biphase-Hyperglycemic Clamp
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)
NCT01812122	PHASE4	COMPLETED	Effects of Vildagliptine and Glimepiride on Glucose Variability
NCT01910441	PHASE4	TERMINATED	Comparison of Vildagliptin vs. Glimepiride on Glucose Variability in Metformin Uncontrolled Type 2 Diabetic Patients
NCT02007278	PHASE4	COMPLETED	Glycemic Excursions in Type 2 Diabetic Patients With Vildagliptin and Metformin Versus Vildagliptin and Glimepiride
NCT02072096	PHASE4	TERMINATED	A Comparison of Two Treatment Strategies in Older Participants With Type 2 Diabetes Mellitus (T2DM)
NCT02142309	PHASE4	UNKNOWN	Glycemic Durability After Metformin Failure
NCT02280486	PHASE4	COMPLETED	Efficacy and Safety of Saxagliptin VS. Glimepiride in Chinese T2DM Patients Controlled Inadequately With Metformin
NCT02301806	PHASE4	UNKNOWN	Effects of Sitaglpitin on Endothelial Function During the OGTT in T2DM

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (2) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of DPWG Guideline for glimepiride and CYP2C9	DPWG	CYP2C9
Annotation of CPIC Guideline for chlorpropamide, dabrafenib, gliclazid	CPIC	G6PD

PharmGKB also curates 1 clinical and 32 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).