Zolpidem

Summary

Zolpidem (CHEMBL911) is an approved small-molecule central nervous system depressant (ATC N05CF02) targeting GABRA1, GABRA2, and GABRA3; indicated across 15 conditions including attention deficit-hyperactivity disorder and insomnia.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N05CF02
• Targets: 3 (GABRA1, GABRA2, GABRA3)
• Indications: 15 conditions
• Clinical trials: 83
• Chemistry: 307.4 Da · C19H21N3O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL911
Name	Zolpidem
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5732
ChEBI	CHEBI:10125
ATC	N05CF02
Molecular formula	C19H21N3O
Molecular weight	307.4
InChIKey	ZAFYATHCZYHLPB-UHFFFAOYSA-N

SMILES: CC1=CC=C(C=C1)C2=C(N3C=C(C=CC3=N2)C)CC(=O)N(C)C

IUPAC name: N,N-dimethyl-2-[6-methyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin-3-yl]acetamide

ChEBI definition: An imidazo[1,2-a]pyridine compound having a 4-tolyl group at the 2-position, an N,N-dimethylcarbamoylmethyl group at the 3-position and a methyl substituent at the 6-position.

Pharmacological roles (ChEBI): central nervous system depressant, GABA agonist, sedative.

Also known as: Sanval, Zolpidem, Zolpidem civ, zolpidem, SID26749064, SID144205024, ZOLPIDEM, SID170465242

Parent form; salt/anhydrous children: CHEMBL1723343, CHEMBL3989820

Patent coverage: 5,077 distinct patent families (17,821 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
GABRA1	GABAA receptor α1 subunit	Positive	7.68	0%	P14867
GABRA2	GABAA receptor α2 subunit	Positive	6.12	0%	P47869
GABRA3	GABAA receptor α3 subunit	Positive	5.67	0%	P34903

Broader ChEMBL bioactivity targets: 31 (assay-derived). Sample: Lysine-specific demethylase 4E, Prelamin-A/C, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], 5-hydroxytryptamine receptor 2B, GABA-A receptor; anion channel, Gamma-aminobutyric acid receptor subunit alpha-1, GABA-A receptor; alpha-3/beta-3/gamma-2, GABA-A receptor; alpha-1/beta-3/gamma-2, GABA-A receptor; alpha-2/beta-3/gamma-2, GABA-A receptor; alpha-1/beta-2/gamma-2.

Bioactivity

ChEMBL activities: 68 potent at pChembl ≥ 5 of 77 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
GABRA1	7.85	IC50	14	nM	CHEMBL_ACT_574081
P18508	7.72	Ki	19	nM	CHEMBL_ACT_331765
GABRA1	7.7	Ki	20	nM	CHEMBL_ACT_19306676
O09028	7.6	Ki	25	nM	CHEMBL_ACT_1038572
GABRA1	7.57	Ki	27	nM	CHEMBL_ACT_1412600
P62813	7.57	Ki	26.7	nM	CHEMBL_ACT_17966218
GABRA1	7.57	Ki	27	nM	CHEMBL_ACT_1844041
GABRA1	7.57	Ki	26.7	nM	CHEMBL_ACT_3519533
GABRA1	7.57	Ki	27	nM	CHEMBL_ACT_595754
GABRA1	7.57	Ki	26.7	nM	CHEMBL_ACT_618407
P18508	7.57	Ki	26.7	nM	CHEMBL_ACT_793338
P18508	7.57	Ki	26.7	nM	CHEMBL_ACT_810275
GABRA1	7.57	Ki	26.7	nM	CHEMBL_ACT_886261
P18508	7.46	Ki	35	nM	CHEMBL_ACT_2633992
P62813	7.33	AC50	46.3	nM	CHEMBL_ACT_25131017
GABRA1	7.33	IC50	46.3	nM	CHEMBL_ACT_574083
O09028	7.32	IC50	48	nM	CHEMBL_ACT_1106753
O09028	7.32	Ki	48	nM	CHEMBL_ACT_346463
P18508	7.3	Ki	50	nM	CHEMBL_ACT_1505242
P18508	7.3	Ki	50	nM	CHEMBL_ACT_1700832
P18508	7.3	Ki	50	nM	CHEMBL_ACT_1825760
P18508	7.3	Ki	50	nM	CHEMBL_ACT_2633955
P18508	7.3	Ki	50	nM	CHEMBL_ACT_908901
GABRA1	7.28	Ki	53	nM	CHEMBL_ACT_1701378
GABRA1	7.28	Ki	52.1	nM	CHEMBL_ACT_662350
GABRA1	7.21	Ki	61.9	nM	CHEMBL_ACT_2401379
O09028	7.18	Ki	66.07	nM	CHEMBL_ACT_29089182
GABRG2	6.99	Ki	103	nM	CHEMBL_ACT_1412601
GABRA1	6.89	IC50	130	nM	CHEMBL_ACT_574082
P23576	6.81	Ki	156	nM	CHEMBL_ACT_17966221

Target pathways

Aggregated over 3 target gene(s): GABRA1, GABRA2, GABRA3.

Top Reactome pathways

2 total, by targets touching each:

Pathway	Targets	Genes
GABA receptor activation	3	GABRA1, GABRA2, GABRA3
Signaling by ERBB4	1	GABRA1

Dominant GO biological processes

GO term	Targets
gamma-aminobutyric acid signaling pathway	3
synaptic transmission, GABAergic	3
chloride transmembrane transport	3
inhibitory synapse assembly	3
monoatomic ion transport	3
chloride transport	3
monoatomic ion transmembrane transport	3
regulation of postsynaptic membrane potential	3
regulation of presynaptic membrane potential	1

Indications & clinical

Indications

15 indications (0 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
attention deficit-hyperactivity disorder	3	MONDO:0007743	EFO:0003888
insomnia	3	MONDO:0013600	EFO:0004698
anxiety	3	MONDO:0011918	EFO:0005230
dementia	3	MONDO:0001627	HP:0000726
depressive disorder	3	MONDO:0002050	MONDO:0002050
sleep disorder	3	MONDO:0100081	EFO:0008568
drug dependence	2	MONDO:0005303	EFO:0003890
Parkinson disease	2	MONDO:0005180	MONDO:0005180
autism	2	MONDO:0005260	EFO:0003758
prostate adenocarcinoma	1	MONDO:0005082	EFO:0000673
obesity disorder	1	MONDO:0011122	EFO:0001073
cannabis dependence	1	MONDO:0005689	EFO:0007191
dystonic disorder	1	MONDO:0003441	MONDO:0000477

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

Clinical trials

Total trials: 83.

Phase distribution

Phase	Trials
PHASE4	24
PHASE1	16
Not specified	16
PHASE3	12
PHASE2	6
EARLY_PHASE1	5
PHASE2/PHASE3	3
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04118387	PHASE4	RECRUITING	Central Sleep Apnea : Physiologic Mechanisms to Inform Treatment
NCT07542756	PHASE4	NOT_YET_RECRUITING	A SMART Approach to Evaluating the Benefits of Common Prescription and OTC Medications for Insomnia
NCT00042146	PHASE4	COMPLETED	Behavioral and Pharmacological Treatment for Insomnia
NCT00156533	PHASE4	COMPLETED	Long Term Treatment With Zolpidem: Nightly and Intermittent Dosing
NCT00177216	PHASE4	COMPLETED	Characteristics of Sleep Patterns in Young Adults With and Without Insomnia
NCT00227942	PHASE4	COMPLETED	Estrogen for Treating Depression in Menopausal Women With Hot Flashes and Insomnia
NCT00286936	PHASE4	TERMINATED	Incidence of Delirium in Hip Fracture Patients Randomized to Regular Hypnotics vs Placebo
NCT00292734	PHASE4	COMPLETED	STILDEP: Zolpidem in Depressive and Dysthimic Patients
NCT00359229	PHASE4	COMPLETED	Stilnox Treatment in Elderly Patients With Insomnia
NCT00432198	PHASE4	COMPLETED	Zolpidem Postmarketing Study in Adolescent Patients With Insomnia
NCT00492232	PHASE4	COMPLETED	Facilitation of Zolpidem (≥10 mg) Discontinuation Through Use of Ramelteon in Subjects With Chronic Insomnia
NCT00530556	PHASE4	COMPLETED	Insomnia and Daytime Function in Osteoarthritis
NCT00653562	PHASE4	COMPLETED	Zolpidem (Myslee) Post Marketing Study in Adolescent Patients With Insomnia - Evaluation With Polysomnography
NCT00781482	PHASE4	WITHDRAWN	Positron Emission Tomography Assessment of the Central Nervous System Effects of Eszopiclone and Zolpidem
NCT01024192	PHASE4	COMPLETED	Efficacy and Safety Assessment of ZOlpidem (Stilnox CR) in Patients With Chronic insomNIA
NCT01097382	PHASE4	COMPLETED	Sleep Satisfaction and Psychomotor Performance of Adults
NCT02353299	PHASE4	COMPLETED	Assess the Effect of Zolpidem, Silenor & Placebo on Arousability, Ataxia/Balance & Cognition in Healthy Volunteers
NCT03526575	PHASE4	COMPLETED	Optimize Astronaut Sleep Medication Efficacy and Individual Effects
NCT03657212	PHASE4	TERMINATED	Enhancing Memory Consolidation in Older Adults
NCT04014387	PHASE4	COMPLETED	Treatment of Disturbed Sleep in Progressive Supranuclear Palsy (PSP)
NCT04468776	PHASE4	COMPLETED	CBT-I or Zolpidem/Trazodone for Insomnia
NCT04720547	PHASE4	COMPLETED	Sleep and Breathing in the General Population - Chemical Stimuli
NCT06084130	PHASE4	UNKNOWN	Zolpidem on CPAP Acclimatization in OSA
NCT06800378	PHASE4	COMPLETED	Zolpidem’s Effects on Road Cycling Performance
NCT06975514	PHASE3	RECRUITING	Safety and Efficacy Study of YZJ-1139 Tablets in Insomnia Disorder
NCT07336277	PHASE3	NOT_YET_RECRUITING	Sleep Quality and the Efficacy of a Multimodal Sleep Pathway in Hospitalized Orthopedic Trauma Patients
NCT00283946	PHASE3	COMPLETED	A Double-blind, Group-comparison Study Using Zolpidem (Myslee) as a Comparative Drug in Patients With Insomnia
NCT00318448	PHASE3	COMPLETED	Efficacy, Safety, and Tolerability of Ambien (Zolpidem) in the Treatment of Children Ages 6 to 17 With Attention Deficit Hyperactivity Disorder (ADHD)-Associated Insomnia
NCT00608985	PHASE3	COMPLETED	Almorexant (ACT 078573) in Adult Subjects With Chronic Primary Insomnia
NCT00630175	PHASE3	COMPLETED	Evaluation of the Hypnotic Properties of Zolpidem-MR 12.5 mg and Zolpidem 10 mg Marketed Product Compared to Placebo in Patients With Primary Insomnia
NCT00999219	PHASE3	COMPLETED	A Study of FK199B to Compare Efficacy With Zolpidem by Polysomnography in Patients With Insomnia
NCT01685073	PHASE2/PHASE3	COMPLETED	The Role of Sleep in the Treatment of Cannabis Use Disorders
NCT01804036	PHASE2/PHASE3	COMPLETED	Two Contrasting Interventions for Sleep Management
NCT02096900	PHASE3	COMPLETED	A Comparison of Midazolam and Zolpidem as Oral Premedication in Children
NCT02139098	PHASE3	TERMINATED	Alternative Dosing Regimens in the Pharmacotherapy of Insomnia
NCT02374567	PHASE3	TERMINATED	Pharmacovigilance in Gerontopsychiatric Patients
NCT03075241	PHASE3	COMPLETED	Z-Drugs for Sleep Disorders in Alzheimer’s Disease
NCT03885141	PHASE2/PHASE3	UNKNOWN	Biolab Zolpidem Orodispersible 1.0 mg, 1.75 mg and 3.5 mg to Treat Maintenance Insomnia Disorder.
NCT05615727	PHASE3	UNKNOWN	Intranasal Dexmedetomidine and Zolpidem for Treatment of Primary Insomnia
NCT05540574	PHASE2	RECRUITING	Trial of Zolpidem for Sleep in Children With Autism

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.

75 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
ALPRAZOLAM	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2, GABRA3
APALUTAMIDE	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2, GABRA3
BREXANOLONE	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2, GABRA3
CHLORDIAZEPOXIDE	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2, GABRA3
CLONAZEPAM	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2, GABRA3
DIAZEPAM	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2, GABRA3
ENZALUTAMIDE	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2, GABRA3
ESZOPICLONE	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2, GABRA3
FLUMAZENIL	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2, GABRA3
FLUNITRAZEPAM	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2, GABRA3
GANAXOLONE	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2, GABRA3
LIOTHYRONINE	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2, GABRA3
PROPOFOL	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2, GABRA3
TRIAZOLAM	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2, GABRA3
ALFAXALONE	ChEMBL + PubChem	Phase 2 (approved)	GABRA1, GABRA2, GABRA3
ABECARNIL	ChEMBL	Phase 2	GABRA1, GABRA2, GABRA3
AZD7325	ChEMBL	Phase 2	GABRA1, GABRA2, GABRA3
BAICALEIN	ChEMBL	Phase 2	GABRA1, GABRA2, GABRA3
BASMISANIL	ChEMBL	Phase 2	GABRA1, GABRA2, GABRA3
BRETAZENIL	ChEMBL	Phase 2	GABRA1, GABRA2, GABRA3
DELORAZEPAM	ChEMBL	Phase 2	GABRA1, GABRA2, GABRA3
FLAVONE	ChEMBL	Phase 2	GABRA1, GABRA2, GABRA3
MK-0777	ChEMBL	Phase 2	GABRA1, GABRA2, GABRA3
PROGABIDE	ChEMBL	Phase 2	GABRA1, GABRA2, GABRA3
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	GABRA1, GABRA2
ASENAPINE	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2
AZELASTINE	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2
BENPERIDOL	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2
CHLORAMBUCIL	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2
CLOZAPINE	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2
EPINASTINE	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2
ETOMIDATE	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2
GLAFENINE	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2
SIMVASTATIN	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2
TIPRANAVIR	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2
TROGLITAZONE	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2
ZALEPLON	ChEMBL	Phase 4 (approved)	GABRA1, GABRA2
SURAMIN	ChEMBL	Phase 3	GABRA1, GABRA2
TIRATRICOL	ChEMBL	Phase 3	GABRA1, GABRA2
DARIGABAT	ChEMBL	Phase 2	GABRA1, GABRA3
PANADIPLON	ChEMBL	Phase 2	GABRA1, GABRA3
ZOTEPINE	ChEMBL	Phase 2	GABRA1, GABRA2
Afatinib	PubChem	Approved	GABRA1, GABRA2
Apixaban	PubChem	Approved	GABRA1, GABRA2
Binimetinib	PubChem	Approved	GABRA1, GABRA2
chenodiol	PubChem	Approved	GABRA1, GABRA2
Fulvestrant	PubChem	Approved	GABRA1, GABRA2
gentian violet	PubChem	Approved	GABRA1, GABRA2
Imipenem	PubChem	Approved	GABRA1, GABRA2
Lactulose	PubChem	Approved	GABRA1, GABRA2
levocarnitine	PubChem	Approved	GABRA1, GABRA2
podofilox	PubChem	Approved	GABRA1, GABRA2
Propylene Glycol	PubChem	Approved	GABRA1, GABRA2
Pyrazinamide	PubChem	Approved	GABRA1, GABRA2
Pyridoxine	PubChem	Approved	GABRA1, GABRA2
Riociguat	PubChem	Approved	GABRA1, GABRA2
saxagliptin	PubChem	Approved	GABRA1, GABRA2
Thiamine	PubChem	Approved	GABRA1, GABRA2
Vorapaxar	PubChem	Approved	GABRA1, GABRA2