Ropinirole
drugOn this page
Also known as NSC-758917RopinirolRopitorSK&F 101468SK&F-101468SID11111741SID26750081SID90341563SID104171231SID144203807SID170465139
Summary
Ropinirole (CHEMBL589) is an approved small-molecule dopamine agonist (ATC N04BC04) targeting DRD2 and DRD3; indicated across 7 conditions including parkinson disease and restless legs syndrome.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: N04BC04
- Targets: 2 (DRD2, DRD3)
- Indications: 7 conditions
- Clinical trials: 30
- Chemistry: 260.37 Da · C16H24N2O
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL589 |
| Name | Ropinirole |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 5095 |
| ChEBI | CHEBI:8888 |
| ATC | N04BC04 |
| Molecular formula | C16H24N2O |
| Molecular weight | 260.37 |
| InChIKey | UHSKFQJFRQCDBE-UHFFFAOYSA-N |
SMILES: CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1
IUPAC name: 4-[2-(dipropylamino)ethyl]-1,3-dihydroindol-2-one
Pharmacological roles (ChEBI): dopamine agonist, antiparkinson drug, central nervous system drug, antidyskinesia agent.
Also known as: NSC-758917, Ropinirol, Ropinirole, Ropitor, SK&F 101468, SK&F-101468, ropinirole, SID11111741, SID26750081, SID90341563, ROPINIROLE, SID104171231
Parent form; salt/anhydrous children: CHEMBL1200411
Patent coverage: 5,494 distinct patent families (21,493 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 20,835 (97%) 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
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 | Agonist | 8.14 | 0% | P14416 |
| DRD3 | D3 receptor | Agonist | 7.72 | 0% | P35462 |
Broader ChEMBL bioactivity targets: 30 (assay-derived). Sample: Lysine-specific demethylase 4E, Prelamin-A/C, 5-hydroxytryptamine receptor 2B, D(1B) dopamine receptor, Alpha-2A adrenergic receptor, Alpha-2B adrenergic receptor, D(1A) dopamine receptor, Dopamine receptor, Muscarinic acetylcholine receptor M2, Dopamine receptor D2 and D3.
Bioactivity
ChEMBL activities: 52 potent at pChembl ≥ 5 of 70 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| DRD3 | 8.54 | Ki | 2.9 | nM | CHEMBL_ACT_15623837 |
| DRD2 | 8.43 | Ki | 3.7 | nM | CHEMBL_ACT_15623836 |
| P19020 | 8.41 | EC50 | 3.89 | nM | CHEMBL_ACT_12456194 |
| DRD3 | 8.4 | EC50 | 4 | nM | CHEMBL_ACT_2053270 |
| DRD2 | 8.19 | EC50 | 6.46 | nM | CHEMBL_ACT_16879806 |
| DRD2 | 8.14 | Ki | 7.2 | nM | CHEMBL_ACT_136461 |
| DRD4 | 8.11 | Ki | 7.8 | nM | CHEMBL_ACT_15623838 |
| DRD3 | 7.99 | EC50 | 10.3 | nM | CHEMBL_ACT_3122237 |
| DRD3 | 7.99 | EC50 | 10.3 | nM | CHEMBL_ACT_3465789 |
| DRD3 | 7.72 | Ki | 19 | nM | CHEMBL_ACT_136462 |
| DRD3 | 7.72 | EC50 | 19.2 | nM | CHEMBL_ACT_2983137 |
| P19020 | 7.53 | Ki | 29.3 | nM | CHEMBL_ACT_13318763 |
| P19020 | 7.53 | Ki | 29.3 | nM | CHEMBL_ACT_3465757 |
| DRD2 | 7.52 | EC50 | 30 | nM | CHEMBL_ACT_18073509 |
| DRD3 | 7.44 | Ki | 36.31 | nM | CHEMBL_ACT_2527804 |
| P19020 | 7.25 | IC50 | 56.1 | nM | CHEMBL_ACT_12456233 |
| DRD3 | 7.21 | Ki | 61 | nM | CHEMBL_ACT_13466681 |
| P61169 | 7.12 | EC50 | 75.5 | nM | CHEMBL_ACT_12456204 |
| DRD2 | 7.08 | EC50 | 83 | nM | CHEMBL_ACT_2053267 |
| DRD2 | 7.05 | EC50 | 89 | nM | CHEMBL_ACT_18073455 |
| DRD2 | 7.05 | EC50 | 89 | nM | CHEMBL_ACT_18217133 |
| DRD2 | 7 | EC50 | 100 | nM | CHEMBL_ACT_243490 |
| P19020 | 6.97 | IC50 | 107 | nM | CHEMBL_ACT_12456209 |
| HTR2A | 6.85 | EC50 | 141.2 | nM | CHEMBL_ACT_16879798 |
| DRD3 | 6.75 | AC50 | 179.8 | nM | CHEMBL_ACT_25193702 |
| DRD2 | 6.52 | EC50 | 304 | nM | CHEMBL_ACT_15150972 |
| DRD2 | 6.52 | EC50 | 302 | nM | CHEMBL_ACT_15151000 |
| DRD2 | 6.52 | EC50 | 304 | nM | CHEMBL_ACT_2983129 |
| DRD2 | 6.52 | EC50 | 304 | nM | CHEMBL_ACT_3122233 |
| DRD2 | 6.52 | EC50 | 304 | nM | CHEMBL_ACT_3465786 |
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
7 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 |
| restless legs syndrome | 3 | MONDO:0005391 | EFO:0004270 |
| stroke disorder | 2 | MONDO:0005098 | EFO:0000712 |
| cocaine dependence | 2 | MONDO:0005186 | EFO:0002610 |
| fibromyalgia | 2 | MONDO:0005546 | EFO:0005687 |
| Unverricht-Lundborg syndrome | 2 | MONDO:0009698 | MONDO:0009698 |
| hyperprolactinemia | 1 | MONDO:0005804 | EFO:0007319 |
Clinical trials
Total trials: 30.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 9 |
| PHASE4 | 8 |
| PHASE2 | 5 |
| PHASE1 | 5 |
| PHASE1/PHASE2 | 2 |
| Not specified | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00314821 | PHASE4 | COMPLETED | Ropinirole in the Treatment of Bipolar Depression |
| NCT00329602 | PHASE4 | COMPLETED | Long-term Study Of Ropinirole In Restless Legs Syndrome |
| NCT00334048 | PHASE4 | COMPLETED | Treating Sexual Dysfunction From Selective Serotonin Reuptake Inhibitor (SSRI) Medication: a Study Comparing Requip CR to Placebo |
| NCT00335205 | PHASE4 | UNKNOWN | A Placebo Controlled Trial of the Dopamine D-2 Receptor Agonist Ropinirole in Treatment of 60 Patients With Refractory Bipolar Depression. |
| NCT00373542 | PHASE4 | COMPLETED | 12-week Polysomnography Study of Ropinirole Controlled Release for Restless Legs Syndrome |
| NCT01485172 | PHASE4 | COMPLETED | A Fixed Dose, Dose Response Study for Ropinirole Prolonged Release in Patients With Early Stage Parkinson’s Disease |
| NCT01494532 | PHASE4 | COMPLETED | A Fixed Dose Study of Ropinirole Prolonged Release as Adjunctive Treatment in Patients With Advanced Parkinson’s Disease |
| NCT03176966 | PHASE4 | COMPLETED | Ropinirole for the Treatment of Muscle Cramps in Patients With Cirrhosis |
| NCT00036218 | PHASE3 | COMPLETED | Study Evaluating Sumanirole for the Treatment of the Signs and Symptoms of Early Parkinson’s Disease. |
| NCT00225862 | PHASE3 | COMPLETED | A Clinical Research Study Evaluating Ropinirole Treatment For Restless Legs Syndrome (RLS) |
| NCT00357097 | PHASE3 | COMPLETED | The Effects Of Ropinirole On Mood Or Mild Depression In Patients With Moderate To Severe Restless Legs Syndrome |
| NCT00363857 | PHASE3 | COMPLETED | A Clinical Research Study Testing Ropinirole Treatment for Restless Legs Syndrome |
| NCT00367822 | PHASE3 | COMPLETED | Transdermal Lisuride: a Trial for the Treatment of Patients With Restless Legs Syndrome (RLS) |
| NCT00381472 | PHASE3 | COMPLETED | Investigational Parkinson’s Disease In Patients Not Well Controlled On L-dopa |
| NCT00823836 | PHASE3 | COMPLETED | Clinical Evaluation of Ropinirole Prolonged Release/Extended Release (PR/XR) Tablet for Adjunctive Therapy to L-dopa in Subjects With Advanced Parkinson’s Disease |
| NCT01628926 | PHASE3 | COMPLETED | A Placebo- and Ropinirole-Controlled Study for SPM 962 in Advanced Parkinson’s Disease Patients |
| NCT03806530 | PHASE3 | COMPLETED | DIalysis Symptom COntrol-Restless Legs Syndrome Trial |
| NCT00256893 | PHASE2 | COMPLETED | Fibromyalgia Study In Adults |
| NCT00460148 | PHASE2 | COMPLETED | Parkinson’s Disease Patient Study On Absorption, Distribution, Metabolism And Excretion Of Ropinirole |
| NCT00639119 | PHASE2 | UNKNOWN | Effect of Ropinirole Hydrochloride in Progressive Myoclonic Epilepsy of Unverricht-Lundborg Type |
| NCT01393457 | PHASE2 | COMPLETED | Cognitive Remediation for Cocaine Dependence |
| NCT03038308 | PHASE1/PHASE2 | COMPLETED | Treatment of Hyperprolactinemia With the Non-ergoline Dopamine Agonist Ropinirole |
| NCT03250117 | PHASE1/PHASE2 | TERMINATED | Relative Bioavailability Study of Ropinirole Implants in Parkinson’s Patients on L-Dopa Switched From Oral Ropinirole |
| NCT03708237 | PHASE2 | TERMINATED | Effectiveness of Ropinirole and Gabapentin for the Treatment of RLS in Patients on Maintenance HD |
| NCT00419692 | PHASE1 | COMPLETED | Restless Legs Patient Study On Absorption, Distribution, Metabolism And Excretion Of Ropinirole And The Effect Of Food |
| NCT01435915 | PHASE1 | COMPLETED | Ropinirole PR Pharmacokinetics Study Among Chinese Healthy Subjects |
| NCT01627834 | PHASE1 | COMPLETED | Bioequivalence Study of Ropinirole Hydrochloride ER Tablets 2 mg Under Fasting Condition |
| NCT01627847 | PHASE1 | COMPLETED | Bioequivalence Study of Ropinirole Hydrochloride ER Tablets 2 mg Under Fed Condition |
| NCT01717235 | PHASE1 | COMPLETED | Bioequivalence Study of Ropinirole Hydrochloride CR 2mg Tablets of Lupin Limited, India, With REQUIP XL of GlaxoSmithKline Research Triangle Park, in Healthy, Adult, Male, Subjects Under Fasting Conditions |
| NCT01327339 | Not specified | COMPLETED | REQUIP RLS Post Marketing Surveillance |
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.
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 |
Related Atlas pages
- Genes: DRD2, DRD3
- Diseases: Parkinson disease, restless legs syndrome
- Drugs: Dihydroergotamine, Acetophenazine, Amiodarone, Amisulpride, Amitriptyline, Amlodipine, Amoxapine, Apomorphine, Aripiprazole, Armodafinil, Asenapine, Astemizole, Azelastine, Bazedoxifene, Benperidol, Benzquinamide, Benztropine, Bepridil, Bosutinib, Brexpiprazole, Bromocriptine, Bromperidol, Buspirone, Butriptyline, Cabergoline, Cariprazine, Carvedilol, Chlorhexidine, Chlorpromazine, Chlorprothixene, Cinacalcet, Cinnarizine, Cisapride, Clemastine, Clomipramine, Clotrimazole, Clozapine, Cyclobenzaprine, Cyproheptadine, Daunorubicin, Desipramine, Desloratadine, Dibenzepin, Diethylstilbestrol, Diphenidol, Disulfiram, Dobutamine, Domperidone, Dopamine, Dothiepin, Doxepin, Droperidol, Duloxetine, Ebastine, Econazole, Epalrestat, Epinephrine, Ergotamine, Fenoldopam