Pramipexole

Summary

Pramipexole (CHEMBL301265) is an approved small-molecule antiparkinson drug (ATC N04BC05) targeting DRD2 and DRD3; indicated across 18 conditions including parkinson disease and tourette syndrome.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N04BC05
• Targets: 2 (DRD2, DRD3)
• Indications: 18 conditions
• Clinical trials: 75
• Chemistry: 211.33 Da · C10H17N3S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL301265
Name	Pramipexole
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	119570
ChEBI	CHEBI:8356
ATC	N04BC05
Molecular formula	C10H17N3S
Molecular weight	211.33
InChIKey	FASDKYOPVNHBLU-ZETCQYMHSA-N

SMILES: CCCN[C@H]1CCC2=C(C1)SC(=N2)N

IUPAC name: (6S)-6-N-propyl-4,5,6,7-tetrahydro-1,3-benzothiazole-2,6-diamine

ChEBI definition: A member of the class of benzothiazoles that is 4,5,6,7-tetrahydro-1,3-benzothiazole in which the hydrogens at the 2 and 6-pro-S-positions are substituted by amino and propylamino groups, respectively.

Pharmacological roles (ChEBI): antiparkinson drug, dopamine agonist, antidyskinesia agent, radical scavenger.

Also known as: Ctc-501, Neliprax, NSC-760426, Pipexus, Pramipexol, Pramipexole, SUD-919CL2Y, SUD919CL2Y, U-98528E, pramipexole, SID50112695, PRAMIPEXOLE

Parent form; salt/anhydrous children: CHEMBL542257, CHEMBL3143955, CHEMBL3182733

Patent coverage: 6,751 distinct patent families (24,026 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
DRD2	D2 receptor	Full agonist	7.4	0%	P14416
DRD3	D3 receptor	Full agonist	8.7	0%	P35462

Broader ChEMBL bioactivity targets: 21 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, 5-hydroxytryptamine receptor 1B, Alpha-2C adrenergic receptor, Histamine H2 receptor, Alpha-2B adrenergic receptor, Beta-2 adrenergic receptor, Dopamine receptor D2 and D3, 5-hydroxytryptamine receptor 1A, D(2) dopamine receptor.

Bioactivity

ChEMBL activities: 101 potent at pChembl ≥ 5 of 110 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DRD2	10.83	Kd	0.01	nM	CHEMBL_ACT_24865270
DRD2	10.83	Kd	0.01	nM	CHEMBL_ACT_24865285
DRD3	10.59	Kd	0.03	nM	CHEMBL_ACT_24865313
P19020	9.68	EC50	0.21	nM	CHEMBL_ACT_991480
P19020	9.35	Ki	0.45	nM	CHEMBL_ACT_12171444
DRD4	9.31	Ki	0.49	nM	CHEMBL_ACT_991475
DRD3	9.18	Ki	0.66	nM	CHEMBL_ACT_24865299
DRD3	9.14	Ki	0.72	nM	CHEMBL_ACT_1500421
P19020	9.11	Ki	0.78	nM	CHEMBL_ACT_12040571
P19020	9.11	Ki	0.78	nM	CHEMBL_ACT_2363557
DRD3	9.09	EC50	0.81	nM	CHEMBL_ACT_24865484
DRD3	9.06	Ki	0.88	nM	CHEMBL_ACT_1500436
DRD3	9.06	Ki	0.88	nM	CHEMBL_ACT_1607243
DRD3	9.06	Ki	0.87	nM	CHEMBL_ACT_765776
DRD3	9.05	Ki	0.9	nM	CHEMBL_ACT_19270677
DRD3	9.03	Ki	0.94	nM	CHEMBL_ACT_19270543
DRD3	9	EC50	1	nM	CHEMBL_ACT_2053271
DRD3	8.96	Ki	1.1	nM	CHEMBL_ACT_19270541
DRD3	8.88	Ki	1.32	nM	CHEMBL_ACT_19069756
DRD3	8.82	EC50	1.5	nM	CHEMBL_ACT_1500427
DRD3	8.82	EC50	1.5	nM	CHEMBL_ACT_1607246
DRD3	8.82	EC50	1.5	nM	CHEMBL_ACT_765781
P20288	8.8	Kd	1.6	nM	CHEMBL_ACT_765778
P61169	8.77	EC50	1.7	nM	CHEMBL_ACT_991478
P19020	8.7	EC50	1.98	nM	CHEMBL_ACT_12456195
DRD4	8.68	Ki	2.07	nM	CHEMBL_ACT_991474
DRD3	8.56	Ki	2.78	nM	CHEMBL_ACT_991472
DRD4	8.56	Ki	2.76	nM	CHEMBL_ACT_991476
P61169	8.51	Ki	3.1	nM	CHEMBL_ACT_2363558
DRD3	8.43	ED50	3.7	nM	CHEMBL_ACT_14662480

Target pathways

Aggregated over 2 target gene(s): DRD2, DRD3.

Top Reactome pathways

2 total, by targets touching each:

Pathway	Targets	Genes
Dopamine receptors	2	DRD2, DRD3
G alpha (i) signalling events	1	DRD3

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor internalization	2
intracellular calcium ion homeostasis	2
adenylate cyclase-inhibiting dopamine receptor signaling pathway	2
locomotory behavior	2
visual learning	2
response to xenobiotic stimulus	2
regulation of dopamine secretion	2
positive regulation of cytokinesis	2
circadian regulation of gene expression	2
response to histamine	2
response to cocaine	2
dopamine metabolic process	2
regulation of potassium ion transport	2
response to morphine	2
negative regulation of blood pressure	2

Indications & clinical

Indications

18 indications (1 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
Parkinson disease	4	MONDO:0005180	MONDO:0005180
Tourette syndrome	3	MONDO:0007661	EFO:0004895
restless legs syndrome	3	MONDO:0005391	EFO:0004270
essential tremor	3	MONDO:0003233	EFO:0003108
eating disorder	3	MONDO:0005451	EFO:0005203
schizoaffective disorder	3	MONDO:0005487	EFO:0005411
depressive disorder	3	MONDO:0002050	MONDO:0002050
fibromyalgia	2	MONDO:0005546	EFO:0005687
obsessive-compulsive disorder	2	MONDO:0008114	EFO:0004242
Alzheimer disease	2	MONDO:0004975	MONDO:0004975
major depressive disorder	2	MONDO:0002009	MONDO:0002009
bipolar disorder	2	MONDO:0004985	MONDO:0004985
substance-related disorder	1	MONDO:0002494	MONDO:0002491
amyotrophic lateral sclerosis	1	MONDO:0004976	MONDO:0004976

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

Clinical trials

Total trials: 75.

Phase distribution

Phase	Trials
PHASE4	22
PHASE3	19
Not specified	14
PHASE2	10
PHASE1	6
EARLY_PHASE1	2
PHASE2/PHASE3	1
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05003648	PHASE4	ACTIVE_NOT_RECRUITING	Treating Leg Symptoms in Women With X-linked Adrenoleukodystrophy
NCT06580041	PHASE4	ENROLLING_BY_INVITATION	Precision Care for Major Depressive Disorder
NCT00102856	PHASE4	SUSPENDED	Neuromodulation and Language Acquisition (Stage Ib)
NCT00231959	PHASE4	COMPLETED	Effectiveness of Pramipexole for Treatment-Resistant Depression
NCT00297778	PHASE4	COMPLETED	Pramipexole Versus Placebo in Parkinson’s Disease (PD) Patients With Depressive Symptoms
NCT00321854	PHASE4	COMPLETED	Study of (Mirapex) Pramipexole for the Early Treatment of Parkinsons Disease (PD)
NCT00344994	PHASE4	COMPLETED	SWITCH:Restless Legs Patients Switched to Ropinirole From Pramipexole
NCT00349531	PHASE4	COMPLETED	A Phase IV Trial With Pramipexole to Investigate the Effects on RLS Symptoms and Sleep Disturbance in Patients With RLS
NCT00356096	PHASE4	COMPLETED	Phase IV Trial With Pramipexole to Evaluate Safety and Efficacy in Patients With RLS Associated With Mood Disturbances
NCT00375284	PHASE4	COMPLETED	A 6 Week Trial to Study the Efficacy and Safety of a Starting Dose 0.25 mg Pramipexole (Mirapex) in Patients With RLS
NCT00402233	PHASE4	COMPLETED	A Randomized, Double-blind, Active (Pramipexole 0.5 mg Tid) and Placebo Controlled, Study of Pramipexole Given 0.5 mg and 0.75 mg Bid Over 12-week Treatment in Early Parkinson’s Disease (PD) Patients
NCT00472199	PHASE4	COMPLETED	Long-term Efficacy, Safety and Tolerability of Pramipexole in Patients With Idiopathic Moderate to Severe Restless Legs Syndrome (RLS)
NCT00597896	PHASE4	COMPLETED	Cognitive Enhancement in Bipolar Disorder
NCT01048229	PHASE4	TERMINATED	Evaluation of the Tolerance and Acceptability of Rasagiline in the Treatment of Early-stage Parkinson’s Disease
NCT01066897	PHASE4	TERMINATED	Imaging the Nucleus Accumbens in Major Depressed Patients ‘Treated With Pramipexole
NCT01673724	PHASE4	COMPLETED	Pramipexole and Bromocriptine on Nonmotor Symptoms of Early Parkinson’s Disease
NCT02025608	PHASE4	COMPLETED	Autonomic Function and Cardiovascular Risk in Restless Legs Syndrome
NCT02033369	PHASE4	COMPLETED	Imaging Dopamine Release in Depression
NCT02233023	PHASE4	COMPLETED	Ophthalmologic Safety of Long Term Treatment With Pramipexole Compared to Bromocriptine or Other Dopamine Agonists in Patients With Parkinson’s Disease
NCT02397837	PHASE4	COMPLETED	Targeting Cognition in Bipolar Disorder With Pramipexole
NCT03817554	PHASE4	TERMINATED	Pramipexole for Restless Leg Syndrome in Peritoneal Dialysis Patients
NCT04936126	PHASE4	UNKNOWN	Comparison of Antidepressant Augmentation With Amantadine vs Pramipexole vs Quetiapine in Treatment Resistant Depression
NCT00133198	PHASE3	COMPLETED	Efficacy and Safety of Pramipexole Compared to Placebo in the Treatment of Restless Legs Syndrome (RLS)
NCT00144209	PHASE3	COMPLETED	Assess Efficacy and Safety of the Dopamine Agonist Pramipexole Versus Levodopa / Benserazide (Madopar® DR) in Patients With Restless Legs Syndrome
NCT00152958	PHASE3	COMPLETED	A Study in Patients Suffering From Idiopathic Restless Legs Syndrome Who Responded to a Preceding, 6-month Treatment With Open-label Pramipexole Including Titration (0.125, 0.25, 0.5, 0.75 mg Orally q.n.)
NCT00240409	PHASE3	COMPLETED	Randomized Single-blind Placebo Controlled Comparative Trial of Pramipexole and Bromocriptine in Parkinson’s Disease
NCT00275457	PHASE3	COMPLETED	Efficacy and Safety of Pramipexole (PPX) in Moderate to Severe Idiopathic Restless Legs Syndrome (RLS) Patients
NCT00335166	PHASE3	COMPLETED	SLV 308 and Pramipexole for Treatment of Patients With Early Parkinson Disease
NCT00577460	PHASE3	COMPLETED	Long-term Safety Study of Open-label Pramipexole ER in Patients With Advanced PD
NCT00601523	PHASE3	COMPLETED	Long-term Safety Study of Open-label Pramipexole Extended Release (ER) in Patients With Early Parkinson´s Disease (PD).
NCT00654498	PHASE3	COMPLETED	Pramipexole in Out-patients With Idiopathic Restless Legs Syndrome (IRLS)
NCT00806026	PHASE3	COMPLETED	Long Term Study Of Pregabalin In Idiopathic Restless Legs Syndrome Patients
NCT00991276	PHASE3	COMPLETED	Polysomnography Study Of Pregabalin And Pramipexole Versus Placebo In Patients With Restless Legs Syndrome And Associated Sleep Disturbance
NCT01106053	PHASE3	WITHDRAWN	Pramipexole for Binge Eating Disorder
NCT01320982	PHASE3	UNKNOWN	Minocycline, Acetylsalicylic Acid or Pramipexole vs Placebo in Patients With Schizophrenia or Schizoaffective Disorder
NCT01441284	PHASE3	WITHDRAWN	Efficacy of Pramipexole Extended Release in the Treatment of Essential Tremor
NCT02172573	PHASE3	COMPLETED	Safety and Efficacy of Pramipexole and Bromocriptine Combined With L-dopa in Parkinson’s Disease
NCT02177357	PHASE3	COMPLETED	Pramipexole in Untreated and Levodopa-treated Parkinson’s Disease Patients
NCT03329508	PHASE3	COMPLETED	A Phase 3 Study With P2B001 in Subjects With Early Parkinson’s
NCT04759703	PHASE2/PHASE3	TERMINATED	Treatment of Restless Legs Symptoms With Pramipexole to Improve the Outcomes of Protracted Opioid Withdrawal in OUD

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.

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

Molecule	Source	Status	Shared targets
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	DRD2, DRD3
GENTIAN VIOLET	ChEMBL + PubChem	Phase 4 (approved)	DRD2, DRD3
ACETOPHENAZINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
AMIODARONE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
AMISULPRIDE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
AMLODIPINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
AMOXAPINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
APOMORPHINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
ARMODAFINIL	ChEMBL	Phase 4 (approved)	DRD2, DRD3
ASENAPINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
AZELASTINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BAZEDOXIFENE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BENPERIDOL	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BENZQUINAMIDE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BENZTROPINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BEPRIDIL	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BOSUTINIB	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BROMPERIDOL	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BUSPIRONE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
BUTRIPTYLINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CABERGOLINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CARIPRAZINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CARVEDILOL	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CHLORPROTHIXENE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CINACALCET	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CINNARIZINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CISAPRIDE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CLEMASTINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CLOZAPINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CYCLOBENZAPRINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
CYPROHEPTADINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DAUNORUBICIN	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DESIPRAMINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DESLORATADINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DIBENZEPIN	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DIPHENIDOL	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DISULFIRAM	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DOBUTAMINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DOMPERIDONE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DOPAMINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DOTHIEPIN	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DOXEPIN	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DROPERIDOL	ChEMBL	Phase 4 (approved)	DRD2, DRD3
DULOXETINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
EBASTINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
ECONAZOLE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
EPALRESTAT	ChEMBL	Phase 4 (approved)	DRD2, DRD3
EPINEPHRINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
ERGOTAMINE	ChEMBL	Phase 4 (approved)	DRD2, DRD3
FENOLDOPAM	ChEMBL	Phase 4 (approved)	DRD2, DRD3