Glipizide

Summary

Glipizide (CHEMBL1073) is an approved small-molecule hypoglycemic agent (ATC A10BB07); indicated across 5 conditions including diabetes mellitus and type 2 diabetes mellitus.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A10BB07
• Indications: 5 conditions
• Clinical trials: 26
• Chemistry: 445.5 Da · C21H27N5O4S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1073
Name	Glipizide
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	3478
ChEBI	CHEBI:5384
ATC	A10BB07
Molecular formula	C21H27N5O4S
Molecular weight	445.5
InChIKey	ZJJXGWJIGJFDTL-UHFFFAOYSA-N

SMILES: CC1=CN=C(C=N1)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCCCC3

IUPAC name: N-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-5-methylpyrazine-2-carboxamide

ChEBI definition: An N-sulfonylurea that is glyburide in which the (5-chloro-2-methoxybenzoyl group is replaced by a (5-methylpyrazin-2-yl)carbonyl group. An oral hypoglycemic agent, it is used in the treatment of type 2 diabetes mellitus.

Pharmacological roles (ChEBI): hypoglycemic agent, EC 2.7.1.33 (pantothenate kinase) inhibitor, insulin secretagogue.

Also known as: CP-28,720, CP-28720, Glibenese, Glipizida, Glipizide, Glipizide component of metaglip, Glipizide slow release, Glucotrol, Glucotrol xl, K 4024, K-4024, Minodiab 2.5

Patent coverage: 10,725 distinct patent families (42,268 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 42,077 (100%) of the total. 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: 13 (assay-derived). Sample: Microtubule-associated protein tau, Survival motor neuron protein, Prelamin-A/C, RecQ-like DNA helicase BLM, Thyrotropin receptor, Beta-lactamase, 5-hydroxytryptamine receptor 1A, Cannabinoid receptor 1, Alpha-1A adrenergic receptor, Nuclear factor NF-kappa-B p105 subunit.

Bioactivity

ChEMBL activities: 10 potent at pChembl ≥ 5 of 19 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
NFKB1	7.95	Potency	11.2	nM	CHEMBL_ACT_3675762
NFKB1	7.95	Potency	11.2	nM	CHEMBL_ACT_4588944
CNR1	7.73	AC50	18.7	nM	CHEMBL_ACT_25116751
LMNA	7.05	Potency	89.1	nM	CHEMBL_ACT_3667450
CYP2C19	6.3	Potency	501.2	nM	CHEMBL_ACT_4021183
SMN1	5.9	Potency	1259	nM	CHEMBL_ACT_3871335
TSHR	5.4	Potency	3981	nM	CHEMBL_ACT_3918888
CYP3A4	5.13	IC50	7447	nM	CHEMBL_ACT_2686202
CYP2C9	5.1	Potency	7943	nM	CHEMBL_ACT_5029450
CYP2C9	5.1	AC50	7943	nM	CHEMBL_ACT_6019454

Target pathways

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

Indications & clinical

Indications

5 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
atherosclerosis	3	MONDO:0005311	EFO:0003914
chronic kidney disease	3	MONDO:0005300	EFO:0003884
exocrine pancreatic carcinoma	2	MONDO:0005192	EFO:0002618

Clinical trials

Total trials: 26.

Phase distribution

Phase	Trials
PHASE3	12
PHASE4	6
Not specified	5
PHASE2	2
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00347100	PHASE4	COMPLETED	Insulin Glargine in Type 2 Diabetic Patients
NCT00513630	PHASE4	COMPLETED	Study on the Prognosis and Effect of Anti-diabetic Drugs on Type-2 Diabetes Mellitus With Coronary Artery Disease
NCT00732524	PHASE4	COMPLETED	Combination of Sulfonylureas and Insulin Glargine Outpatient Therapy for Unstable Diabetes and Impending DKA
NCT01758471	PHASE4	UNKNOWN	Efficacy of Acarbose on Intestinal Microbiome and Incretins of Type 2 Diabetes
NCT01951651	PHASE4	COMPLETED	Effect of Exenatide on Liver and Heart Fat and Inflammation
NCT02911792	PHASE4	COMPLETED	Effect of Farxiga on Renal Function and Size in Type 2 Diabetic Patients With Hyperfiltration
NCT00086515	PHASE3	COMPLETED	Metformin Add-on Study in Patients With Type 2 Diabetes Mellitus (0431-020)(COMPLETED)
NCT00094770	PHASE3	COMPLETED	An Investigational Drug Study in Patients With Type 2 Diabetes Mellitus (0431-024)
NCT00095056	PHASE3	COMPLETED	An Investigational Drug in Patients With Type 2 Diabetes Mellitus and Chronic Renal Insufficiency (0431-028)(COMPLETED)
NCT00116831	PHASE3	COMPLETED	Rosiglitazone Versus a Sulfonylurea On Progression Of Atherosclerosis In Patients With Heart Disease And Type 2 Diabetes
NCT00350779	PHASE3	COMPLETED	Sitagliptin Metformin/PPARg Agonist Combination Therapy Add-on (0431-052)
NCT00509236	PHASE3	COMPLETED	Sitagliptin Versus Glipizide in Participants With Type 2 Diabetes Mellitus and End-Stage Renal Disease (MK-0431-073 AM1)
NCT00509262	PHASE3	COMPLETED	Sitagliptin Versus Glipizide in Participants With Type 2 Diabetes Mellitus and Chronic Renal Insufficiency (MK-0431-063 AM1)
NCT00660907	PHASE3	COMPLETED	Efficacy and Safety of Dapagliflozin in Combination With Metformin in Type 2 Diabetes Patients
NCT00707993	PHASE3	COMPLETED	Efficacy and Safety of Alogliptin Compared to Glipizide in Elderly Diabetics
NCT00856284	PHASE3	COMPLETED	Efficacy and Safety of Alogliptin Plus Metformin Compared to Glipizide Plus Metformin in Patients With Type 2 Diabetes Mellitus
NCT00885352	PHASE3	COMPLETED	Sitagliptin (MK-0431) vs. Placebo in Patients With Inadequate Glycemic Control on Metformin With Pioglitazone (MK-0431-128)
NCT01698775	PHASE3	COMPLETED	A Study of Omarigliptin (MK-3102) in Participants With Type 2 Diabetes Mellitus With Chronic Kidney Disease or Kidney Failure on Dialysis (MK-3102-019)
NCT06168812	PHASE2	ACTIVE_NOT_RECRUITING	A Study of Glipizide to Treat High Blood Sugar in People With Pancreatic Cancer
NCT01020123	PHASE2	COMPLETED	Evaluate Efficacy, Safety and Tolerability of AZD1656 as Add-on Treatment to Metformin in Type 2 Diabetes Mellitus (TD2M) Patients
NCT01762046	PHASE1	COMPLETED	Study to Understand the Genetics of the Acute Response to Metformin and Glipizide in Humans
NCT06830096	Not specified	RECRUITING	Role of KATP Channel Loss in Type 2 Diabetes
NCT00550329	Not specified	COMPLETED	Bioequivalence Study Of Glucotrol XL 2.5 Mg Tablets
NCT01082796	Not specified	COMPLETED	Cytochrome P450 2C19 Variant is Related to Pharmacokinetics of Glipizide Extended Release Tablet in Chinese Subjects
NCT02608177	Not specified	COMPLETED	Continuous Glucose Monitoring to Assess Glycemia in Chronic Kidney Disease - Changing Glucose Management
NCT05073692	Not specified	COMPLETED	Comparison of Type 2 Diabetes Pharmacotherapy Regimens

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (1) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

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

PharmGKB also curates 1 clinical and 26 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).