Rotigotine

Summary

Rotigotine (CHEMBL1303) is an approved small molecule (ATC N04BC09) targeting DRD1, DRD2, and DRD3; indicated across 6 conditions including restless legs syndrome and parkinson disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N04BC09
• Targets: 5 (DRD1, DRD2, DRD3…)
• Indications: 6 conditions
• Clinical trials: 77
• Chemistry: 315.5 Da · C19H25NOS

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1303
Name	Rotigotine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	59227
ATC	N04BC09
Molecular formula	C19H25NOS
Molecular weight	315.5
InChIKey	KFQYTPMOWPVWEJ-INIZCTEOSA-N

SMILES: CCCN(CCC1=CC=CS1)[C@H]2CCC3=C(C2)C=CC=C3O

IUPAC name: (6S)-6-[propyl(2-thiophen-2-ylethyl)amino]-5,6,7,8-tetrahydronaphthalen-1-ol

Also known as: Leganto, Neupro, Rotigotina, Rotigotine, SPM 962, SPM-962, ROTIGOTINE, SID50113269, SID144206180, SID170465204, rotigotine

Patent coverage: 344 distinct patent families (832 SureChEMBL compound mentions), from 2 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
DRD1	D1 receptor	Full agonist	5.6	0%	P21728
DRD2	D2 receptor	Agonist	10.22	0%	P14416
DRD3	D3 receptor	Agonist	8.4	0%	P35462
DRD4	D4 receptor	Agonist	7.26	0%	P21917
DRD5	D5 receptor	Full agonist	6	0%	P21918

Broader ChEMBL bioactivity targets: 27 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, Equilibrative nucleoside transporter 1, D(1A) dopamine receptor, 5-hydroxytryptamine receptor 1A, Muscarinic acetylcholine receptor M1, D(2) dopamine receptor, Cannabinoid receptor 1.

Bioactivity

ChEMBL activities: 30 potent at pChembl ≥ 5 of 38 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DRD2	10.22	Ki	0.06	nM	CHEMBL_ACT_647888
DRD2	10.22	Ki	0.06	nM	CHEMBL_ACT_863324
DRD2	9.15	EC50	0.7	nM	CHEMBL_ACT_13863878
DRD1	9	AC50	1	nM	CHEMBL_ACT_25180169
DRD2	8.49	EC50	3.2	nM	CHEMBL_ACT_18073487
ADRA1A	8.48	AC50	3.3	nM	CHEMBL_ACT_25229533
DRD3	8.4	Ki	4	nM	CHEMBL_ACT_647889
DRD3	8.4	Ki	3.99	nM	CHEMBL_ACT_863322
DRD2	8.39	EC50	4.1	nM	CHEMBL_ACT_18073454
DRD2	8.36	EC50	4.4	nM	CHEMBL_ACT_18073508
DRD3	7.98	AC50	10.5	nM	CHEMBL_ACT_25193172
P20288	7.82	Ki	15	nM	CHEMBL_ACT_720874
DRD2	7.7	Ki	20	nM	CHEMBL_ACT_863321
DRD1	7.55	EC50	28	nM	CHEMBL_ACT_13863911
DRD4	7.26	Ki	55	nM	CHEMBL_ACT_863323
DRD2	6.92	AC50	121.6	nM	CHEMBL_ACT_25139970
ADRA2B	6.89	AC50	130	nM	CHEMBL_ACT_25143348
ADRA2C	6.4	AC50	400	nM	CHEMBL_ACT_25147513
HTR2B	6.37	AC50	430	nM	CHEMBL_ACT_25228364
HTR2A	6.34	AC50	460	nM	CHEMBL_ACT_25225993
Q95136	6.3	Ki	500	nM	CHEMBL_ACT_720873
DRD1	6.26	AC50	550	nM	CHEMBL_ACT_25115842
HTR1A	6.17	AC50	670	nM	CHEMBL_ACT_25215760
SLC6A3	5.89	AC50	1300	nM	CHEMBL_ACT_25123592
ADRA2A	5.43	AC50	3700	nM	CHEMBL_ACT_25220739
KCNH2	5.42	AC50	3800	nM	CHEMBL_ACT_25117323
HRH1	5.37	AC50	4300	nM	CHEMBL_ACT_25212146
SLC6A2	5.29	AC50	5100	nM	CHEMBL_ACT_25144644
SLC6A4	5.11	AC50	7800	nM	CHEMBL_ACT_25149984
OPRM1	5.07	AC50	8600	nM	CHEMBL_ACT_25157210

Target pathways

Aggregated over 5 target gene(s): DRD1, DRD2, DRD3, DRD4, DRD5.

Top Reactome pathways

3 total, by targets touching each:

Pathway	Targets	Genes
Dopamine receptors	5	DRD1, DRD2, DRD3, DRD4, DRD5
G alpha (s) signalling events	2	DRD1, DRD5
G alpha (i) signalling events	2	DRD3, DRD4

Dominant GO biological processes

GO term	Targets
phospholipase C-activating dopamine receptor signaling pathway	5
synaptic transmission, dopaminergic	5
signal transduction	5
G protein-coupled receptor signaling pathway	5
response to amphetamine	4
behavioral response to cocaine	4
response to cocaine	4
intracellular calcium ion homeostasis	4
adenylate cyclase-activating dopamine receptor signaling pathway	3
G protein-coupled dopamine receptor signaling pathway	3
visual learning	3
response to xenobiotic stimulus	3
dopamine metabolic process	3
positive regulation of MAPK cascade	3
regulation of dopamine uptake involved in synaptic transmission	3

Indications & clinical

Indications

6 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
restless legs syndrome	4	MONDO:0005391	EFO:0004270
Parkinson disease	4	MONDO:0005180	MONDO:0005180
fibromyalgia	2	MONDO:0005546	EFO:0005687
stroke disorder	2	MONDO:0005098	EFO:0000712
Alzheimer disease	2	MONDO:0004975	MONDO:0004975
drug dependence	2	MONDO:0005303	EFO:0003890

Clinical trials

Total trials: 77.

Phase distribution

Phase	Trials
PHASE3	31
PHASE2	14
PHASE1	14
PHASE4	13
Not specified	3
PHASE2/PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00594464	PHASE4	COMPLETED	A Trial of Neupro® (Rotigotine Transdermal Patch) in Patients With Parkinson’s Disease Undergoing Surgery
NCT01300819	PHASE4	COMPLETED	Placebo-controlled Study in Patients With Parkinson’s Disease to Evaluate the Effect of Rotigotine on Non-motor Symptoms
NCT01455012	PHASE4	COMPLETED	Effects of Neupro on Cardiovascular Observations in Patients With Restless Legs Syndrome
NCT01519882	PHASE4	TERMINATED	Sleep Efficiency Assessed by Polysomnography (PSG Sleep Lab Testing) in Advanced Parkinson’s Disease
NCT01523301	PHASE4	COMPLETED	Rotigotine Versus Placebo to Evaluate the Efficacy on Depressive Symptoms in Idiopathic Parkinson’s Disease Patients
NCT01711866	PHASE4	COMPLETED	A Phase 4, Open-label Study to Assess the Feasibility and Efficacy on Motor and Non-motor Symptoms of Switching From Pramipexole or Ropinirole to Rotigotine Transdermal Patch in Subjects With Advanced Idiopathic Parkinson’s Disease
NCT01744496	PHASE4	COMPLETED	Study to Evaluate the Efficacy of Rotigotine on Parkinson’s Disease-Associated Pain
NCT01782222	PHASE4	COMPLETED	Trial to Evaluate The Efficacy Of Rotigotine on Parkinson’s Disease-Associated Motor Symptoms And Apathy
NCT01823770	PHASE4	COMPLETED	Effect of Rotigotine Patch Treatment on Cardiovascular Markers in Idiopathic Restless Legs Syndrome
NCT01976871	PHASE4	COMPLETED	Switching From Oral Dopamine Agonists to Rotigotine
NCT02365870	PHASE4	TERMINATED	Anxiety in Parkinson’s: Use of Quantitative Methods to Guide Rational Treatment
NCT03098368	PHASE4	UNKNOWN	Rotigotine Effect on Nocturnal Hypokinesia Compares to Placebo Control: A Quantitative Assessment by Wearable Sensors
NCT03103919	PHASE4	COMPLETED	Study to Evaluate the Impact of Using Wearable Devices in Addition to Standard Clinical Practice on Parkinson´s Subject Symptoms Management
NCT06702124	PHASE3	RECRUITING	A Phase 3 Study of Rotigotine in Combination with Rivastigmine in Mild to Moderate Alzheimer’s Disease
NCT00135993	PHASE3	COMPLETED	Four Different Transdermal Doses of Rotigotine in Subjects With Idiopathic Restless Legs Syndrome
NCT00136045	PHASE3	COMPLETED	Three Different Transdermal Doses of Rotigotine in Subjects With Idiopathic Restless Leg Syndrome
NCT00242008	PHASE3	COMPLETED	A Trial To Assess Switching From Ropinirole, Pramipexole Or Cabergoline To The Rotigotine Transdermal System In Idiopathic Parkinson’s Disease
NCT00243945	PHASE3	COMPLETED	A Trial to Evaluate the Effects of Rotigotine Transdermal Patch on Early Morning Motor Impairment and Sleep Disorders Idiopathic Parkinson’s Disease
NCT00243971	PHASE3	COMPLETED	A Trial to Compare the Efficacy of Rotigotine Transdermal Patch to That of Ropinirole on Early Morning Motor Impairment and Sleep Disorders in Subjects With Early-Stage, Idiopathic Parkinson’s Disease
NCT00244387	PHASE3	COMPLETED	Rotigotine Patch in Subjects With Advanced Stage, Idiopathic Parkinson’s Disease Who Are Not Well Controlled on Levodopa
NCT00263068	PHASE3	COMPLETED	An Extension Trial to Investigate Long-Term Treatment With Transdermal Rotigotine in Idiopathic Restless Legs Syndrome
NCT00275236	PHASE3	COMPLETED	A Sleep Lab Trial to Investigate the Efficacy and Safety of Transdermal Rotigotine in Subjects With Idiopathic Restless Legs Syndrome
NCT00474058	PHASE3	COMPLETED	Randomized Evaluation of the 24-Hour Coverage: Efficacy of Rotigotine
NCT00498108	PHASE3	COMPLETED	Phase 3 Open-label Extension Trial With Rotigotine in Idiopathic Restless Legs Syndrome Subjects
NCT00501969	PHASE3	COMPLETED	An Open-Label Extension Trial to Assess the Safety of Long-Term Treatment of Rotigotine in Advanced-Stage Parkinson’s Disease
NCT00505687	PHASE3	COMPLETED	An Open-Label Extension Trial to Assess the Safety and Tolerability of Long Term Treatment of Rotigotine in Subjects With Idiopathic Parkinson’s Disease
NCT00519532	PHASE3	TERMINATED	Long-term Extension of RECOVER- Long-term Effect of the 24h Transdermal Delivery of Rotigotine in Subjects With Idiopathic Parkinson’s Disease
NCT00522379	PHASE3	COMPLETED	Trial to Assess Parkinson’s Disease (PD) Symptom Control to Four Doses of Rotigotine in a Transdermal Patch
NCT00537485	PHASE2/PHASE3	COMPLETED	A Placebo-controlled Study for SPM 962 in Early Parkinson’s Disease Patients
NCT00593606	PHASE3	COMPLETED	Safety and Tolerability Trial of Switching From Ropinirole to Rotigotine
NCT00594165	PHASE3	COMPLETED	An Open-Label Extension Trial to Assess the Safety of Long-Term Treatment of Rotigotine in Early-Stage Parkinson’s Disease.
NCT00594386	PHASE3	COMPLETED	An Open-Label Extension Trial to Assess the Safety of Long-Term Treatment of Rotigotine in Advance-Stage Parkinson’s Disease
NCT00599196	PHASE3	COMPLETED	An Open-Label Extension Trial to Assess the Safety of Long-Term Treatment of Rotigotine in Early-Stage Parkinson’s Disease
NCT01084551	PHASE3	COMPLETED	Study of SPM 962 in Patients With Restless Legs Syndrome (RLS)
NCT01536015	PHASE3	TERMINATED	Effect of Rotigotine on Motor Symptoms in Patients With Advanced Parkinson’s Disease (PD) With Motor Fluctuations and Symptoms of Gastrointestinal Dysfunction
NCT01537042	PHASE3	COMPLETED	A Sleep Laboratory Study to Investigate the Safety and Efficacy of the Rotigotine Skin Patch in Subjects With Restless Legs Syndrome and End-Stage Renal Disease Requiring Hemodialysis
NCT01569464	PHASE3	COMPLETED	Rotigotine Effect on All-day Functioning and Quality of Life in Subjects With Moderate to Severe Restless Legs Syndrome (RLS)
NCT01628926	PHASE3	COMPLETED	A Placebo- and Ropinirole-Controlled Study for SPM 962 in Advanced Parkinson’s Disease Patients
NCT01628965	PHASE2/PHASE3	COMPLETED	A Long-Term Extension Trial From Phase II/III of SPM 962 in Early Parkinson’s Disease Patients
NCT01631825	PHASE3	COMPLETED	A Long-Term Extension Trial From of SPM 962 in Advanced Parkinson’s Disease Patients

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.

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

Molecule	Source	Status	Shared targets
CLOZAPINE	ChEMBL + PubChem	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
OLANZAPINE	ChEMBL + PubChem	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
PALIPERIDONE	ChEMBL + PubChem	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
Pramipexole	ChEMBL + PubChem	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
AMOXAPINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
APOMORPHINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
CABERGOLINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
CARIPRAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
DOPAMINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
DOXEPIN	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
HALOPERIDOL	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
IMIPRAMINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
LOXAPINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
PROMAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
RISPERIDONE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
ROPINIROLE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
TEGASEROD	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4, DRD5
PENFLURIDOL	ChEMBL	Phase 2	DRD1, DRD2, DRD3, DRD4, DRD5
RACLOPRIDE	ChEMBL	Phase 2	DRD1, DRD2, DRD3, DRD4, DRD5
RITANSERIN	ChEMBL	Phase 2	DRD1, DRD2, DRD3, DRD4, DRD5
DESLORATADINE	ChEMBL + PubChem	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
AMIODARONE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
ASENAPINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
BENPERIDOL	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
CARVEDILOL	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
CHLORPROTHIXENE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
DISULFIRAM	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
DOBUTAMINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
EBASTINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
ECONAZOLE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
ILOPERIDONE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
KETANSERIN	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
KETOTIFEN	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
LOPERAMIDE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
MAPROTILINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD5
MECLIZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
MIANSERIN	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
MICONAZOLE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
NEFAZODONE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
PERGOLIDE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
PIMOZIDE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
PROCHLORPERAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
PROMETHAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
QUETIAPINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
SERTINDOLE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
SILODOSIN	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
SULPIRIDE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
SUNITINIB	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
TAMOXIFEN	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
THIORIDAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4
THIOTHIXENE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, DRD4