Drug Database
RO

ropinirole (Requip CR / ropinirole 24hr / Requip LP)

✓ Approved

SkyePharma PLC · DRD2 · Small Molecule

What is ropinirole?

ropinirole is a small molecule developed by SkyePharma PLC. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesRequip CR, ropinirole 24hr, Requip LP
CompanySkyePharma PLC
Drug ClassSmall Molecule
Molecular TargetDRD2, DRD3
RouteOral (PO)
StatusApproved

Mechanism of Action

Molecular Targets

ropinirole acts on 2 molecular targets:

DRD2dopamine receptor D2 (D2DR, D2R)
DRD3dopamine receptor D3 (D3DR, FET1)
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Therapeutic Indications

ropinirole is developed for 2 unique indications across 1 therapeutic area.

Therapeutic AreaConditionPhase
Nervous system disordersParkinson's disease✓ Approved
Nervous system disordersRestless legs syndromePhase II

Related Research Articles

PubMedEuropean child & adolescent psychiatry2026-08-25

Ropinirole adjunct to methylphenidate versus placebo adjunct to methylphenidate for attention-deficit/hyperactivity disorder: a randomized, double-blind, placebo-controlled trial.

Farahvash Aidin A, Naseh Ehsan E, Morovvati Mahdis M, Shamabadi Ahmad A et al.

Current therapeutics for attention-deficit/hyperactivity disorder (ADHD) have significant limitations, necessitating innovative therapies. This study aimed to investigate the efficacy and safety of ropinirole, a dopamine agonist with anti-inflammatory and neuroprotective properties, as an add-on to methylphenidate for children with ADHD. In this eight-week, randomized, double-blind trial, 66 outpatients aged 6-17 with a diagnosis of ADHD were randomized to receive methylphenidate plus either ropinirole 0.25 mg or a matching placebo twice daily. ADHD-related symptoms were assessed using the ADHD Rating Scale-IV (ADHD-RS-IV) reported by teachers and parents at baseline and weeks 4 and 8. Inattention and hyperactivity-impulsivity subscale scores were also recorded. Additionally, adverse effects were monitored throughout the study. Data from 65 participants were used for analyses. Baseline demographic and clinical characteristics were comparable between the arms. Significant time-by-treatment interaction was observed for the ADHD-RS-IV total scores as rated by teachers ([Formula: see text]= 0.051) and parents ([Formula: see text]= 0.153). The ropinirole group demonstrated significantly greater reductions in ADHD-RS-IV total scores from baseline to the endpoint as reported by teachers (Cohen's d = 0.530) and parents (Cohen's d = 0.504). Also, the ropinirole group achieved higher rates of response to treatment (69.7% versus 34.4%) and robust improvement (60.6% versus 25.0%). The incidence of adverse effects was comparable. In conclusion, methylphenidate + ropinirole was safe and beneficial compared to methylphenidate + placebo for reducing inattentive, hyperactive-impulsive, and total symptoms in children with ADHD. Further studies are required.

PubMedRegenerative therapy2026-08-08

From neural development to regenerative medicine: A research journey in stem cell biology, spinal cord repair, and iPSC-based drug discovery.

Okano Hideyuki H

This commemorative article reflects on a research journey spanning neural development, stem cell biology, regenerative medicine, and iPSC-based drug discovery. My early work focused on RNA-mediated regulation in the nervous system, including studies on myelin basic protein gene regulation and the identification and functional characterization of the RNA-binding protein Musashi. These studies contributed to the conceptual foundation of neural stem cell biology and helped establish methods for identifying and isolating neural stem/progenitor cells, including those present in the adult human brain. Building on this foundation, my colleagues and I pursued translational research in spinal cord injury, ranging from analyses of injury pathophysiology and molecular interventions to preclinical studies using rodent and non-human primate models. These efforts ultimately led to the first-in-human clinical study of induced pluripotent stem cell-derived neural stem/progenitor cell transplantation for subacute spinal cord injury. In parallel, we developed patient-derived iPSC platforms for neurological disease modeling and drug discovery, particularly for amyotrophic lateral sclerosis, where iPSC-based screening identified Ropinirole as a therapeutic candidate and enabled reverse translational research linking cellular phenotypes with clinical responses. Looking ahead, I argue that the future of regenerative therapy will depend on the continued integration of developmental biology, stem cell science, disease modeling, rehabilitation, and clinical translation to address unmet medical needs in disorders of the central nervous system.

PubMedClinical neuropharmacology2026-07-01

Pre-Existing Peak-Dose Dyskinesia and Light Body Weight as Predictors of Ropinirole Patch Dose Modification in Parkinson Disease: A Multicenter Retrospective Study.

Tohge Rie R, Kaneko Satoshi S, Kouda Katsuyasu K, Oki Mitsuaki M et al.

A ropinirole patch provides continuous dopaminergic stimulation, permitting its increasing use in clinical practice. Inappropriate dose conversion after switching from other dopamine agonists may cause insufficient efficacy or dose-limiting adverse effects. Moreover, factors influencing dose modification remain unclear. Thus, this study aimed to identify factors associated with the need for dose modification in patients with Parkinson disease who switched from another dopamine agonist to a ropinirole patch. In this multicenter, retrospective study, dose trajectories over 3 months were categorized as dose reduction, maintenance, or escalation. Clinical characteristics associated with dose changes were assessed using univariate analyses, followed by ordinal logistic regression to identify independent predictors. Correlations among candidate variables were examined for potential dependency. Of the 110 patients screened, 95 were analyzed. Twenty-two patients required dose reduction or discontinuation, primarily because of dyskinesia, hallucinations, or somnolence, whereas 19 required dose escalation because of insufficient efficacy. Univariate analysis identified female sex, lower body weight, and pre-existing peak-dose dyskinesia as significant factors. In multivariate analysis, lower body weight [odds ratio (OR)=1.04; 95% CI=1.00-1.09] and pre-existing peak-dose dyskinesia (OR=0.38; 95% CI=0.15-0.94) independently predicted dose modification. Model comparisons suggested potential dependency between body weight and female sex. Pre-existing peak-dose dyskinesia and lower body weight independently influence the need for ropinirole patch dose modification after switching. Individualized dose titration is recommended, particularly in light-weight patients or those with dyskinesia, and prospective studies are warranted to refine dose conversion strategies.

PubMedInternational journal of biological macromolecules2026-06-30

Quality by design-based development of transferrin-functionalized nanostructured lipid carriers for targeted Co-delivery of ropinirole and mangiferin for improved drug-delivery to the brain.

Adil Mohammad M, Jiba Umme U, Zaidi Syed Amir Azam SAA, Iqbal M D Azhar MDA et al.

Ischemic stroke (IS) persists as a major contributor of mortality and functional impairment globally, because of limited conventional drug delivery system and restrictive properties of the blood-brain barrier (BBB). In recent years, Ligand-conjugated nanomaterial-based drug delivery systems have emerged as effective techniques to improve brain-targeted therapy through multimodal approach. In this context, the present study proposes an innovative nanotechnology based Transferrin (Tf)-conjugated Nanostructured Lipid carrier (NLC) co-loaded Ropinirole (RP), and Mangiferin (MF) to facilitate targeted and effective delivery across the BBB. The characterization of developed Transferrin-conjugated Ropinirole-Mangiferin-Nanostructured Lipid carrier (Tf-RP-MF-NLC) demonstrated a mean particle size of 163.9 ± 2.97 nm, a polydispersity index (PDI) of 0.31 ± 0.04, zeta potential of -8.589 ± 3.63 mV and spherical morphology as shown by Transmission Electron Microscopy (TEM) Analysis. The entrapment efficiency (EE) of RP and MF was found to be >85%, while Tf conjugation efficiency was estimated to be >60%. The % cumulative drug release was found to be >80% for RP and > 65% for MF over 24 h from Tf-RP-MF-NLC. The antioxidant effect and biocompatibility of the Tf-RP-MF-NLC were confirmed by the DPPH assay and haemolysis testing, respectively. Furthermore, results obtained from gamma scintigraphy study revealed that Tf-RP-MF-NLC had enhanced brain targeting and increased drug accumulation as compared to RP-MF-NLC following intraperitoneal (i.p.) administration. Overall, these findings highlights Tf-RP-MF-NLC as a promising brain targeted nanocarrier system with improved drug delivery, suggesting its potential as an effective therapeutic strategy for improved drug delivery to the brain.

PubMedRegenerative therapy2026-06-26

Therapeutic frontiers in ALS: iPSC-based drug discovery, cell therapy, and gene therapy-Advances through 2026.

Morimoto Satoru S, Kato Chris C, Takahashi Shinichi S, Okano Hideyuki H

Three converging therapeutic paradigms-iPSC-based drug discovery, cell transplantation, and gene therapy-have substantially expanded the therapeutic pipeline for amyotrophic lateral sclerosis (ALS) between 2020 and 2026. The FDA's accelerated approval of tofersen (Qalsody) in April 2023 marked the first treatment targeting a genetic cause of ALS. iPSC-derived drug candidates, including ropinirole and bosutinib, have completed early-phase clinical trials led by Japanese institutions. Cell therapies targeting neuroinflammation through regulatory T cells are being actively explored as immunomodulatory strategies, although efficacy remains to be established in adequately powered trials. Next-generation gene-silencing approaches-including RNA interference (RNAi) therapeutics and AAV-delivered microRNA-entered first-in-human trials in 2024-2025. The identification of STMN2 as a downstream target of TDP-43 dysfunction has opened a potential TDP-43-downstream nucleic acid therapeutic avenue for sporadic ALS, which constitutes approximately 90% of all cases, with company-reported interim data suggesting target engagement in the ongoing Phase 1/2 ANQUR trial (QRL-201). This review synthesizes the latest evidence across all three therapeutic domains, with attention to the hierarchy of evidence, regulatory milestones, and the pioneering contributions of Japanese research groups.

PubMedAmerican journal of ophthalmology2026-06-24

Dopamine-Enhancing Therapies and Risk of Neovascular AMD Conversion: A Target Trial Emulation.

Fazal Owais O, Loya Asad A, Muayad Jawad J, Alsoudi Amer F AF et al.

Age-related macular degeneration (AMD) is a leading cause of central vision loss worldwide. Emerging evidence suggests that targeting dopaminergic pathways may influence AMD progression. This study evaluates whether levodopa ± carbidopa or dopamine receptor D2 (DRD2) agonists are associated with reduced risk of conversion to neovascular AMD (nAMD). Population-based clinical cohort study. Adults aged ≥18 years diagnosed with non-nAMD between May 2005 and May 2025, within the TriNetX US Collaborative Network, a federated electronic health record database spanning 69 healthcare organizations. This retrospective cohort study emulated four distinct target trials comparing new users of (1) levodopa (± carbidopa) or (2) DRD2 agonists (pramipexole, ropinirole, bromocriptine, rotigotine, or cabergoline) to new users of two comparators (pantoprazole or gabapentin). Patients with prior nAMD or prescriptions of other dopamine-enhancing agents (eg, selegiline, rasagiline, tolcapone) were excluded. Each exposure group was independently matched to comparators using 1:1 propensity score matching for selected demographics, social factors, comorbidities, and AMD stage. The primary outcome was 3-year risk of conversion from non-nAMD to nAMD. Hazard ratios (HRs) with 95% confidence intervals (CIs) were calculated. An α level of 0.05 was used to determine statistical significance. Patients prescribed levodopa ± carbidopa had a reduced 3-year risk of conversion to nAMD relative to their matched counterparts prescribed pantoprazole (levodopa n = 1312, control n = 1312; HR 0.67; 95% CI, 0.45-0.98) and gabapentin (levodopa n = 1675, control n = 1675; HR 0.69; 95% CI, 0.50-0.95). No significant difference was observed in 3-year risk of conversion to nAMD between DRD2 agonists use relative to pantoprazole (DRD2 n = 1603, control n = 1603; HR 0.81; 95% CI, 0.58-1.13) or gabapentin (DRD2 n = 2779, control n = 2779; HR 0.92; 95% CI, 0.72-1.19). In this cohort study, levodopa ± carbidopa use was associated with lower 3-year risk of conversion to nAMD in two independent matched comparisons, whereas DRD2 agonists were not associated with significant differences in risk. These findings suggest dopaminergic signaling may influence AMD progression and warrant further prospective investigation.

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