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Rotigotine

Rotigotine is a non-ergolinic dopamine agonist formulated as a transdermal patch for continuous delivery, primarily used to treat the signs and symptoms of idiopathic Parkinson's disease (PD) and moderate-to-severe primary restless legs syndrome (RLS).^[1]^[2] Developed in the early 2000s as an alternative to oral dopamine agonists, rotigotine provides stable plasma concentrations over 24 hours, mimicking physiological dopamine levels and reducing fluctuations associated with intermittent dosing.^[3] Its chemical structure, (S)-6-(propyl(2-(thiophen-2-yl)ethyl)amino)-5,6,7,8-tetrahydronaphthalen-1-ol, with a molecular formula of C₁₉H₂₅NOS and molecular weight of 315.47 g/mol, allows for effective skin permeation without first-pass metabolism.^[1] Marketed under the brand name Neupro, it was first approved by the U.S. FDA in 2007 for early-stage PD, with approval expanded in 2012 to include advanced-stage PD and moderate-to-severe primary RLS (after a temporary U.S. market withdrawal from 2008 to 2012 due to manufacturing concerns), with dosing strengths ranging from 1 mg/24 hours to 8 mg/24 hours depending on the indication.^[2]^[4] As a selective agonist for dopamine D3 receptors (with affinity for D1, D2, and D5 subtypes), rotigotine stimulates central dopamine receptors to alleviate motor symptoms in PD, such as bradykinesia, rigidity, and tremors, and to reduce sensory disturbances and urge to move in RLS, though its precise mechanism in these conditions remains partially understood.^[5]^[3] It can be used as monotherapy in early PD or adjunctive therapy with levodopa in advanced stages, and as standalone treatment for RLS, with clinical trials demonstrating significant improvements in Unified Parkinson's Disease Rating Scale (UPDRS) scores and International Restless Legs Syndrome Study Group Rating Scale (IRLS) outcomes.^[6]^[3] Pharmacokinetically, rotigotine exhibits dose-proportional absorption with 37% bioavailability, reaching steady-state levels in 1–2 days, and is primarily metabolized via cytochrome P450 enzymes (CYP3A4 and others) with elimination through urine (71%) and feces (23%).^[3] Common adverse effects include application site reactions (e.g., erythema, pruritus), nausea, somnolence, and dizziness, occurring in ≥5% of patients, while serious risks encompass hallucinations, impulse control disorders (e.g., pathological gambling), orthostatic hypotension, and potential melanoma monitoring in PD patients.^[2]^[5] The patch is applied once daily to clean, dry skin on areas like the abdomen or thigh, with site rotation every 14 days to minimize irritation, and abrupt discontinuation should be avoided to prevent withdrawal symptoms.^[7]

Medical uses

Parkinson's disease

Rotigotine, a non-ergoline dopamine agonist, is approved for the treatment of Parkinson's disease (PD) through transdermal patch delivery, providing continuous dopaminergic stimulation to address motor symptoms across disease stages. In the US, maximum recommended doses are 6 mg/24 hours for early-stage PD and 8 mg/24 hours for advanced-stage PD; higher doses up to 16 mg/24 hours may be approved in other regions such as the EU.^[8]^[9] In early-stage PD, rotigotine serves as monotherapy to alleviate motor symptoms including bradykinesia, rigidity, and tremor. A randomized, double-blind, placebo-controlled trial (SP513) involving patients with early PD demonstrated that rotigotine treatment resulted in a mean absolute difference of 5.28 points lower in combined Unified Parkinson's Disease Rating Scale (UPDRS) parts II (activities of daily living) and III (motor examination) scores compared to placebo after 24 weeks.^[10] This improvement reflects clinically meaningful enhancements in daily functioning and motor control, as confirmed by a systematic review of multiple trials showing consistent reductions in UPDRS motor scores with rotigotine monotherapy.^[11] For advanced-stage PD, rotigotine is used as adjunctive therapy with levodopa to mitigate motor fluctuations, particularly by reducing "off" time when symptoms re-emerge due to waning medication effects. Pooled data from two double-blind, placebo-controlled phase III trials (SP790 and SP792) indicated that rotigotine at 8 mg/24 hours reduced absolute daily "off" time by up to 2.7 hours compared to a 0.9-hour reduction with placebo over 24-28 weeks.^[12] These findings highlight rotigotine's role in stabilizing symptom control for patients experiencing unpredictable motor variations. Dosing begins with an initial 2 mg/24 hours patch for early-stage PD or 4 mg/24 hours for advanced-stage PD, applied once daily to clean, dry skin and replaced after 24 hours. Titration occurs in 2 mg/24 hours increments weekly based on clinical response and tolerability, up to a maximum of 6 mg/24 hours in early PD or 8 mg/24 hours in advanced PD.^[13] Rotigotine is particularly suitable for patients with motor fluctuations or end-of-dose dyskinesia, as its transdermal formulation maintains stable plasma concentrations that approximate physiological dopamine delivery, minimizing pulsatile stimulation.^[13]

Restless legs syndrome

Rotigotine is indicated for the treatment of moderate-to-severe primary restless legs syndrome (RLS) in adults, a neurological disorder characterized by an irresistible urge to move the legs often accompanied by uncomfortable sensations, primarily occurring in the evening or at rest.^[8] It is not approved or recommended for secondary RLS stemming from underlying conditions such as iron deficiency anemia or end-stage renal disease, where addressing the root cause takes precedence.^[14] In randomized controlled trials, rotigotine has shown robust efficacy in alleviating RLS symptoms, with mean reductions in the International Restless Legs Syndrome Study Group Rating Scale (IRLS) scores of 11 to 13 points from baseline at effective doses (2-3 mg/24 hours), compared to 4-6 points with placebo.^[15]^[16] These improvements translate to enhanced sleep quality, as measured by the Medical Outcomes Study Sleep Scale, and better overall quality of life, with responder rates (≥50% IRLS reduction) reaching 60-70% in maintenance phases up to 6 months.^[15] Long-term open-label extensions confirm sustained benefits over 1-5 years in adherent patients.^[17] Treatment typically begins with a 1 mg/24 hours transdermal patch applied once daily in the evening, with upward titration by 1 mg/24 hours at weekly intervals based on clinical response and tolerability, to a maximum of 3 mg/24 hours.^[8] If no meaningful improvement occurs after 2-3 weeks at the optimal dose, discontinuation is recommended to avoid unnecessary exposure.^[8] The patch formulation ensures continuous drug delivery, providing stable plasma concentrations that effectively target evening and nocturnal symptom peaks.^[18] Rotigotine's agonism at D3 dopamine receptors may confer additional therapeutic value for RLS patients with comorbid mood disturbances, potentially mitigating depressive symptoms through modulation of reward and motivational pathways.^[19] Nonetheless, as with other dopamine agonists, there is a risk of augmentation—characterized by earlier onset, increased severity, or spread of RLS symptoms—with long-term incidence around 10-13% over multiple years for rotigotine, lower than oral agonists; periodic symptom monitoring and dose adjustments are recommended.^[20]

Adverse effects

Common adverse effects

Common adverse effects of rotigotine, administered as a transdermal patch, are typically mild to moderate and occur more frequently than with placebo in clinical trials for both Parkinson's disease and restless legs syndrome.^[8] These effects often diminish with continued use and dose titration.^[21] Gastrointestinal effects include nausea, reported in 21-48% of patients depending on dose and indication, vomiting in 10-20%, and constipation in 5-9%.^[8] These are frequently dose-related, with higher incidences in early-stage Parkinson's disease at 6 mg/24 hours.^[8] Management involves slow dose titration to reduce onset, and antiemetics may be used for persistent nausea under medical supervision.^[21] Nervous system effects encompass somnolence in 10-32% of patients, dizziness in 22-23%, and headache in up to 16%, particularly in restless legs syndrome trials.^[8]^[16] Insomnia or disturbances in initiating and maintaining sleep affect 10-14%.^[8] These symptoms can be mitigated by gradual dose adjustment and avoiding activities requiring alertness until tolerance develops.^[22] Application site reactions, such as erythema, pruritus, or edema, occur in 32-43% of users and are linked to the transdermal delivery method.^[8] These are mostly mild and resolve without discontinuation.^[11] To minimize them, rotate application sites daily, avoiding the same area for at least 14 days, and apply to clean, dry, intact skin away from oily or irritated areas.^[21] Other common effects include fatigue or asthenic conditions in 6-12% and hyperhidrosis in up to 11%.^[8] Overall incidence data derive from placebo-controlled trials across indications, with withdrawal rates due to adverse events around 10-15%.^[11]

Serious adverse effects

Rotigotine, a dopamine agonist, is associated with impulse control disorders, including pathological gambling, hypersexuality, compulsive shopping, and binge eating, which occur in approximately 9% of patients with Parkinson's disease during long-term treatment.^[23] These behaviors represent a class effect of dopamine agonists and are generally reversible upon dose reduction or discontinuation.^[24] The risk may be linked to rotigotine's strong affinity for D3 receptors, which can contribute to dysregulated reward pathways.^[25] Psychiatric adverse effects, such as hallucinations, psychotic episodes, confusion, and delirium, have been reported in approximately 7% of patients in advanced Parkinson's disease trials (4% greater than placebo), with higher incidence in patients over 65 years old.^[8] These effects are more common in elderly patients and may require dose adjustment or temporary discontinuation.^[25] Cardiovascular risks include orthostatic hypotension and syncope, particularly during dose initiation or escalation, with incidences of significant systolic blood pressure drops (≥20 mmHg) of 16% in early Parkinson's disease, 32% in advanced stages, and 13% in restless legs syndrome (treatment differences of 18%, 4%, and 1% over placebo, respectively).^[8] Sudden onset of sleep, or "sleep attacks," occurs in 0.5-2% of patients, including those with restless legs syndrome, and can lead to hazardous situations without warning.^[8]^[25] Other serious risks encompass a potential increased melanoma incidence in Parkinson's disease patients treated with dopamine agonists, necessitating regular dermatologic monitoring.^[8] Postmarketing reports include rhabdomyolysis.^[8] Abrupt discontinuation can precipitate withdrawal symptoms, including rebound restless legs syndrome, anxiety, fatigue, hyperpyrexia, and confusion, potentially mimicking neuroleptic malignant syndrome.^[25] Gradual dose tapering, such as reducing by 1 mg/24 hours every other day for restless legs syndrome, is recommended to mitigate these effects.^[25] Monitoring for serious adverse effects involves screening patients and caregivers for impulse control behaviors at baseline, during dose increases, and at regular follow-ups, with prompt intervention if symptoms emerge.^[8] Blood pressure should be assessed regularly, especially in early treatment phases, and patients advised against driving or operating machinery due to sudden sleep risk.^[8] Annual skin examinations are advised for melanoma surveillance in Parkinson's patients.^[8]

Pharmacology

Pharmacodynamics

Rotigotine is a non-ergoline dopamine agonist that acts as a full agonist at the D1, D2, D3, D4, and D5 dopamine receptor subtypes, exhibiting the highest binding affinity for the D3 receptor (Ki = 0.71 nM), followed by D2 (Ki = 13.5 nM) and D1 (Ki = 83 nM).^[26] It displays moderate affinity and full agonist activity at D4 and D5 receptors (Ki values ranging from 3.9 to 15 nM for D4 subtypes and 5.4 nM for D5).^[26]^[27] By stimulating dopamine receptors in key brain regions such as the substantia nigra and striatum, rotigotine enhances dopaminergic signaling to alleviate motor symptoms associated with Parkinson's disease.^[28] Its potent D3 receptor agonism may also contribute to potential antidepressant effects, as observed with other dopamine agonists targeting this subtype.^[29] Additionally, D3 activation has been linked to anti-inflammatory properties in preclinical models of neurodegeneration.^[30] Rotigotine exhibits additional binding at non-dopaminergic sites, acting as an antagonist at the α2B-adrenergic receptor (Ki = 27 nM) and as a weak agonist at the 5-HT1A serotonin receptor (Ki = 30 nM).^[26] The transdermal delivery system of rotigotine provides continuous drug release, achieving steady-state plasma levels that mimic physiological continuous dopaminergic stimulation rather than the pulsatile release seen with intermittent oral dosing.^[31]

Pharmacokinetics

Rotigotine is administered via transdermal patch, providing continuous release over 24 hours with an absolute bioavailability of approximately 37% of the applied dose. Steady-state plasma concentrations are reached within 2–3 days of daily application, exhibiting linear pharmacokinetics across therapeutic doses. Plasma levels remain stable throughout the day, with average maximum concentrations (C_max) ranging from 0.4 to 1.1 ng/mL at doses of 2–8 mg/24 hours used for Parkinson's disease.^[31]^[8]^[3] Following absorption, rotigotine is widely distributed, with an apparent volume of distribution of approximately 84 L/kg, indicating extensive tissue penetration, including efficient crossing of the blood-brain barrier. It is highly bound to plasma proteins, approximately 92%, primarily to albumin and α₁-acid glycoprotein.^[8]^[29]^[3] Metabolism occurs primarily in the liver through conjugation (sulfation and glucuronidation), producing inactive metabolites, with a minor contribution from N-dealkylation mediated by cytochrome P450 enzymes, including CYP3A4 as the major isoform and CYP2D6 as a minor one. At least eight metabolites have been identified, none of which are pharmacologically active. The transdermal route avoids first-pass metabolism.^[3]^[25]^[29] Elimination of rotigotine follows a biphasic pattern, with an initial half-life of about 3 hours and a terminal half-life of 5–7 hours after patch removal. Approximately 71% is excreted in the urine and 23% in the feces, predominantly as inactive conjugates, with less than 1% as unchanged drug. No dose adjustment is required for patients with mild to moderate hepatic impairment or mild to severe renal impairment, including those requiring dialysis. Use in severe hepatic impairment has not been studied and should only be considered if the anticipated benefits outweigh the risks.^[13]^[8]^[3] In special populations, pharmacokinetics are similar between elderly and younger adults, with no clinically significant differences in clearance. Food does not affect absorption due to the transdermal delivery. The stable plasma levels achieved help minimize fluctuations beneficial in conditions like Parkinson's disease.^[32]^[8]^[3]

History

Development

Rotigotine, originally designated as N-0437, was synthesized in 1985 at the University of Groningen in the Netherlands as part of efforts to develop novel dopamine receptor agonists within the 2-aminotetralin class. The compound was designed to exhibit high potency with preference for D3 dopamine receptors over D2 (Ki values of 0.71 nM for D3 and 13.5 nM for D2), addressing limitations of existing agonists by offering improved receptor binding affinity, as demonstrated through radioreceptor assays. This synthesis marked an early step toward non-ergoline structures, which were prioritized to mitigate risks associated with ergot-derived compounds, such as cardiac valvulopathy.^[33] Preclinical evaluation in animal models, including rodents and primates, confirmed rotigotine's potent agonism at D2 and D3 dopamine receptors, with binding affinities several times higher than dopamine itself at these sites. Studies highlighted its efficacy in improving motor function in models of Parkinson's disease, such as 6-hydroxydopamine-lesioned rats and MPTP-treated primates, where it reduced akinesia and improved locomotion without the pronounced emetic side effects observed with ergoline agonists like bromocriptine, due to its non-ergoline profile and avoidance of gastrointestinal first-pass metabolism. The emphasis on transdermal delivery emerged early, as rotigotine's high lipophilicity (logP ≈ 4.5) supported patch formulations using a silicone-based matrix for sustained release, bypassing gastrointestinal absorption issues and providing stable plasma levels over 24 hours in preclinical pharmacokinetic models.^[34]^[33]^[28] Early clinical development in the 1990s involved Phase I and II trials that assessed safety, tolerability, and preliminary efficacy in healthy volunteers and Parkinson's disease patients. These studies, comprising over 17 protocols, demonstrated good tolerability with minimal nausea compared to oral agonists, attributed to the transdermal route, and confirmed motor benefits such as reduced "off" time in small cohorts of early-stage patients through Unified Parkinson's Disease Rating Scale assessments. The non-ergoline structure was further validated as reducing risks of fibrotic complications like valvulopathy, with no such events reported in initial safety monitoring. Key milestones included the licensing of rotigotine in 1998 from Aderis Pharmaceuticals to Schwarz Pharma, which advanced the transdermal patch technology using a silicone adhesive matrix for controlled, zero-order release kinetics, achieving approximately 45% in vitro drug delivery over 24 hours. Schwarz Pharma was acquired by UCB in 2006. This partnership facilitated progression to larger Phase III trials by the early 2000s, building on the compound's promising preclinical and early clinical profile.^[29]^[35]

Regulatory history

Rotigotine, marketed as Neupro, received initial marketing authorization from the European Medicines Agency (EMA) on February 15, 2006, for the treatment of early-stage Parkinson's disease as monotherapy or in combination with levodopa in advanced stages. The authorization was extended to include moderate to severe idiopathic restless legs syndrome in August 2008, following a positive CHMP opinion on April 24, 2008. No major changes to the approval status occurred as of the latest procedural update on May 8, 2025.^[9]^[36] In the United States, the Food and Drug Administration (FDA) approved rotigotine transdermal system on May 9, 2007, for the signs and symptoms of early-stage idiopathic Parkinson's disease as monotherapy. The indications were expanded to advanced Parkinson's disease and moderate-to-severe primary restless legs syndrome in November 2008. However, in March 2008, the manufacturer voluntarily recalled all lots due to crystallization of the active ingredient in some patches, which could impair drug delivery and efficacy; the product went out of stock in late April 2008. The issue was resolved through reformulation, leading to reapproval on April 3, 2012, for early- and advanced-stage Parkinson's disease and restless legs syndrome.^[35]^[34]^[37]^[4] Rotigotine was approved in Australia by the Therapeutic Goods Administration on November 14, 2007, for Parkinson's disease, with subsequent inclusion of restless legs syndrome. In Canada, Health Canada granted a Notice of Compliance on March 21, 2013, for both Parkinson's disease and restless legs syndrome. Japan's Ministry of Health, Labour and Welfare approved it on December 27, 2012, for the same indications. No significant new regulatory approvals have occurred in major markets since 2020. In December 2024, UCB filed a lawsuit against the FDA over approval of a generic version of rotigotine.^[38]^[39]^[40]^[41] Post-marketing surveillance includes ongoing monitoring for impulse control disorders, such as pathological gambling and hypersexuality, as highlighted in updated product labels requiring patient counseling. The EMA's pediatric investigation plan for rotigotine was completed following submission of study results in 2016 and 2023, but no extension to pediatric use was granted due to insufficient evidence of safety and efficacy in children and adolescents.^[25]^[42]^[43]

Society and culture

Brand names

Rotigotine is primarily marketed under the brand name Neupro by UCB Pharma as a transdermal patch formulation.^[44] Neupro is available in six dosage strengths: 1 mg/24 hours, 2 mg/24 hours, 3 mg/24 hours, 4 mg/24 hours, 6 mg/24 hours, and 8 mg/24 hours, designed for once-daily application to provide continuous delivery of the drug through the skin.^[13] As of 2025, no generic version of rotigotine is available in the United States due to ongoing patent protections until at least 2032.^[45] In the European Union, however, generic rotigotine patches have been authorized since 2018, with examples including Rotigotine Mylan, following the expiry of key patents.^[46] Additionally, in April 2025, Luye Pharma launched its own generic transdermal patch, branded as Rotigotine Luye, in the United Kingdom, offering comparable strengths in a smaller patch size compared to Neupro. In early 2025, Luye Pharma also launched its generic transdermal patch in Japan.^[47]^[48] Rotigotine is primarily available as a transdermal patch worldwide, with no oral formulations approved or marketed. An extended-release microsphere injection formulation (Jinyouping) is also available in China.^[29]^[49] Minor regional variations exist, but Neupro remains the dominant international brand.^[50]

Availability

Rotigotine is available by prescription only worldwide, as it is classified as a controlled medication requiring medical supervision due to its dopaminergic effects.^[9]^[24] It is not a scheduled controlled substance under international drug conventions, though its use is monitored for potential impulse control disorders, such as pathological gambling or compulsive behaviors, which have been reported in up to 50% of patients on dopamine agonists like rotigotine.^[51]^[52] The medication is widely accessible in developed regions, including the European Union, United States, Canada, and Japan, where it is approved for Parkinson's disease and restless legs syndrome.^[9]^[34]^[40] In Canada, it is authorized by Health Canada and available through limited coverage programs for eligible indications.^[53] Availability is more restricted in many developing countries, where regulatory approval may be absent or distribution limited due to healthcare infrastructure challenges, often requiring importation for access.^[54] In approved markets, rotigotine is typically covered by public or private insurance for its indicated uses, though copayments and prior authorization may apply.^[55]^[56] Expanded access in Japan includes generic options launched in 2025.^[48] In the United States, the average retail cost for a 30-day supply of rotigotine transdermal patches (e.g., 4 mg/24 hours strength) is approximately $850 as of 2025, though patient assistance programs can reduce out-of-pocket expenses to as low as $10 per month for eligible individuals.^[57]^[58] In the European Union, generic versions of rotigotine patches, introduced by manufacturers such as Mylan and Vektor Pharma since 2020, have reduced costs by 20-40% compared to the branded Neupro product, enhancing affordability.^[59]^[60]^[61] No supply shortages of rotigotine have been reported globally since its reformulation and reintroduction in 2012, ensuring consistent availability.^[34] The European Medicines Agency's marketing authorization for Neupro remains active as of 2025, with no indications of impending withdrawal.^[9]

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Status date: 2013-12-19. Filter items. Showing 1 to 1 of 1 ... The Summary Basis of Decision explains why the product was approved for sale in Canada.
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Buy Neupro (rotigotine) Online • Price & Costs | Everyone.org
Neupro (rotigotine transdermal system) is a prescription medicine used to treat Parkinson's disease and moderate-to-severe primary Restless Legs Syndrome.
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Eligible for the NEUPRO Patient Savings Card?
Eligible commercial patients may pay as little as $10 per 30-day supply of NEUPRO* · Check your eligibility below · Register to activate your card · Present your ...Missing: 2025 | Show results with:2025
[53]
Limited coverage criteria – rotigotine - Province of British Columbia
Mar 21, 2025 · Limited Coverage Criteria Information for Special Authority coverage of rotigotine (Neupro) for the treatment of Parkinson's disease.Missing: EU | Show results with:EU
[54]
https://everyone.org/neupro-rotigotine-transdermal-system
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Neupro Prices, Coupons, Copay Cards & Patient Assistance
1 mg/24 hr Neupro transdermal film, extended release from $851.81 for 30 films · 2 mg/24 hr Neupro transdermal film, extended release from $851.81 for 30 films ...Missing: monthly | Show results with:monthly
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[PDF] Rotigotine Mylan - European Medicines Agency
The primary pharmacokinetic variables for assessment of bioequivalence are AUCTAU,. CPEAK(SS) and Cτ(SS) for rotigotine. The chosen pharmacokinetic variables ...
[57]
Generic Rotigotine Patches Developed by Vektor Pharma
Jun 12, 2020 · The patches are approved for the treatment of Parkinson's disease in Europe and the United States. Generic medications are designed to work in ...<|separator|>
[58]
https://www.drugs.com/price-guide/neupro