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Ropinirole | CAS No: 91374-21-9 | GMP-certified suppliers
A medication that treats Parkinson's disease and moderate to severe restless legs syndrome by modulating dopamine pathways to improve motor control and sensory symptoms.
Therapeutic categories
Primary indications
- For the treatment of the signs and symptoms of Parkinson's disease and for the treatment of primary moderate-severe restless legs syndrome
Product Snapshot
- Ropinirole is an oral small molecule formulated primarily as film-coated and extended-release tablets
- It is indicated for managing signs and symptoms of Parkinson’s disease and moderate to severe primary restless legs syndrome
- Ropinirole is approved for use in the US and Canada, with both approved and investigational statuses noted
Clinical Overview
Pharmacologically, ropinirole acts primarily through selective stimulation of dopamine receptors, notably exhibiting the highest affinity for D3 receptors concentrated in limbic brain areas and significant activity at D2 receptors located in the caudate-putamen system, a key region in movement regulation. The precise mechanisms by which ropinirole alleviates Parkinsonian symptoms and RLS remain incompletely characterized but are understood to involve dopaminergic modulation of neural pathways governing motor control and sensory-motor integration.
Ropinirole belongs chemically to the indoline class, featuring an indole moiety with a fused pyrrolidine and benzene ring. It exhibits negligible affinity for peripheral α2-adrenergic and 5-HT1 receptors, and no activity at D1-like, benzodiazepine, or GABA receptors.
Key ADME attributes include metabolism primarily via CYP1A2 enzymes. Ropinirole has shown no dose-related effects on ECG parameters or QT intervals at doses up to 4 mg/day in healthy volunteers. However, dopamine agonist-associated orthostatic hypotension is a relevant safety consideration, attributed to D2-mediated impairment of noradrenergic vascular responses upon standing. This can be accompanied by bradycardia, syncope, and nausea, especially during dose escalation. Suppression of serum prolactin has been observed at low oral doses.
Ropinirole is commercialized under the brand name ReQuip by GlaxoSmithKline Pharmaceuticals. Regulatory and procurement teams should consider the importance of consistent CYP1A2 substrate activity and the need for API quality assurance regarding impurity profiles and polymorphic forms to ensure bioequivalence. Reliable sourcing aligned with pharmacopeial standards is critical to maintain clinical efficacy and safety in finished products.
Identification & chemistry
| Generic name | Ropinirole |
|---|---|
| Molecule type | Small molecule |
| CAS | 91374-21-9 |
| UNII | 030PYR8953 |
| DrugBank ID | DB00268 |
Pharmacology
| Summary | Ropinirole is a dopamine agonist with high affinity for D3 receptors and selective stimulation of D2 receptors in the caudate-putamen, contributing to its effects on motor control in Parkinson's disease. Its therapeutic actions in Parkinson’s and restless legs syndrome are believed to result from dopamine receptor activation, modulating neural pathways involved in movement regulation. Ropinirole’s pharmacodynamic profile includes effects on prolactin secretion and potential cardiovascular responses such as orthostatic hypotension, mediated by dopaminergic modulation of noradrenergic pathways. |
|---|---|
| Mechanism of action | Ropinirole is a non-ergoline dopamine agonist. Ropinirole has the highest affinity at the D3 receptors, which are concentrated in the limbic areas of the brain and may be responsible for some of the neuropsychiatric effects . The exact mechanism of action of ropinirole as a treatment for Parkinson’s disease is unknown, however, it is believed to be related to its ability to selectively stimulate dopamine D2 receptors within the caudate-putamen system in the brain. This system affects body movement. Negligible affinity is seen for ropinirole at α2 adrenoreceptors in the periphery and 5HT-1 receptor. Ropinirole has no affinity at the D1-like receptors, benzodiazepine or GABA receptors . The precise mechanism of action of ropinirole as a treatment for Restless Legs Syndrome is unknown, however, it is believed to be related to its ability to stimulate dopamine receptors. |
| Pharmacodynamics | **Effects on Parkinson's and restless leg syndrome** This drug promotes the relief or improvement of symptoms of Parkinson's or restless leg syndrome by stimulatory actions on dopamine receptors, which regulate movement. **Effects on blood pressure** Clinical experience with dopamine agonists, including ropinirole, suggests an association with impaired abilities in regulating blood pressure with resulting orthostatic hypotension, especially with patients undergoing dose escalation. In some patients in clinical studies, blood pressure changes were associated with orthostatic symptoms, bradycardia, and, in one case in a healthy volunteer, transient sinus arrest accompanied by syncope. The mechanism of orthostatic hypotension caused by ropinirole is assumed to be due to a D2-mediated blunting of noradrenergic response to a standing position, followed by a decrease in peripheral vascular resistance. Nausea is also a frequent symptom which accompanies orthostatic signs and symptoms. **Effects on prolactin** At oral doses as low as 0.2 mg, ropinirole suppressed serum prolactin concentrations in healthy male volunteers. Ropinirole had no dose-related effect on ECG wave form and rhythm in young, healthy, male volunteers in the range of 0.01 to 2.5 mg. **Effects on QT interval** Ropinirole had no dose- or exposure-related effect on average QT intervals in healthy male and female volunteers at doses up to 4 mg/day. The effect of ropinirole on QTc intervals at higher exposures reached either due to drug interactions, hepatic dysfunction, or at higher doses has not been adequately evaluated. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Dopamine D3 receptor | Humans | agonist |
| Dopamine D2 receptor | Humans | agonist |
| Dopamine D4 receptor | Humans | agonist |
ADME / PK
| Absorption | Ropinirole is rapidly absorbed after oral administration, reaching peak concentration in approximately 1 to 2 hours, . Absolute bioavailability was 45% to 55%, suggesting approximately 50% hepatic first-pass effect. The bioavailability of ropinirole prolonged release compared to the immediate release tablets is about 100% . Ingestion of food does not affect the absorption of ropinirole, although its Tmax was increased by 2.5 hours and its Cmax was reduced by approximately 25% when the drug is taken with a high-fat meal. |
|---|---|
| Half-life | Approximately 6 hours, . |
| Protein binding | 40% bound to plasma proteins with a blood-to-plasma ratio of 1:1. |
| Metabolism | Ropinirole is heavily metabolized by the liver. The most important metabolic pathways are N despropylation and hydroxylation to form the _N-despropyl_ metabolite and _hydroxy_ metabolites, both of which are inactive . The _N-despropyl_ metabolite is then converted to _carbamyl glucuronide_, carboxylic acid, and _N-despropyl hydroxy_ metabolites. Following this process, the _hydroxy_ metabolite of ropinirole is glucuronidated at a rapid rate. _In vitro_ studies show that the major cytochrome P450 enzyme involved in the metabolism of ropinirole is CYP1A2, . |
| Route of elimination | The majority of the absorbed dose is cleared by the liver . In clinical trials, more than 88% of a radiolabeled dose was recovered in urine. Less than 10% of the administered dose is excreted as unchanged drug in urine. _N-despropyl ropinirole_ is the major metabolite found in the urine (40%), followed by the _carboxylic acid_ metabolite (10%), and the _glucuronide_ of the hydroxy metabolite (10%). |
| Volume of distribution | Ropinirole is found to be widely distributed throughout the body, with an apparent volume of distribution of **7.5 L/kg**. |
| Clearance | The clearance of ropinirole after oral administration is 47 L/h. |
Formulation & handling
- Ropinirole is formulated exclusively for oral administration, primarily as film-coated and extended-release tablets.
- As a small molecule indoline compound with moderate water solubility and LogP of 3.06, it exhibits good permeability characteristics for oral absorption.
- It can be administered with or without food, though food intake may be advised to reduce gastrointestinal discomfort such as nausea.
Regulatory status
| Lifecycle | The API's initial patent expired in the United States in June 2012, with subsequent related patents expiring in 2021. The product is available in both the US and Canadian markets, indicating a mature stage in its lifecycle with potential for generic competition. |
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| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Ropinirole's manufacturing landscape includes multiple originator and generic manufacturers such as GlaxoSmithKline and several generic pharmaceutical companies, reflecting a diverse supplier base. The branded products have a presence primarily in the US and Canadian markets. Patent expirations occurring between 2012 and 2021 suggest that generic competition is currently established and ongoing. |
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Safety
| Toxicity | **Overdose** Symptoms of overdose include agitation, chest pain, confusion, drowsiness, facial muscle movements, grogginess, increased jerkiness of movement, symptoms of low blood pressure (dizziness, light-headedness)upon standing, nausea, and vomiting. **Carcinogenicity** Two-year carcinogenicity studies of ropinirole were performed on animal models at oral doses of 5, 15, and 50 mg/kg/day and in rats at oral doses of 1.5, 15, and 50 mg/kg/day. There was an increase in testicular Leydig cell adenomas at all doses tested in rats. The hormonal mechanisms thought to be involved in the development of these tumors in rats are not considered relevant to humans. In mice, there was an increase in benign uterine endometrial polyps at a dose of 50 mg/kg/day. The highest dose not associated with this observation (15 mg/kg/day) is three times the maximum recommended human dose on a mg/m2 basis. **Mutagenesis** Ropinirole was not found to be mutagenic or clastogenic during in vitro assays, or in the in vivo mouse micronucleus test. **Effects on reproduction** When given to female rats prior to and during mating and throughout pregnancy, ropinirole led to disruption of implantation at oral doses of 20 mg/kg/day (8 times the MRHD on a mg/m2 basis) or higher. This effect in rats is believed to be due to the prolactin-lowering effects of ropinirole. **Use in Pregnancy** Pregnancy Category C. There are no sufficient and well-controlled studies done in pregnant women. In animal reproduction studies, ropinirole has demonstrated adverse effects on embryo-fetal development, including teratogenicity. |
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- Handle with care to avoid exposure, as overdose symptoms may include neurological and cardiovascular effects such as agitation, chest pain, and hypotension
- Toxicology studies indicate species-specific tumorigenic effects at high doses
- Relevance to humans is considered low based on current data
Ropinirole is a type of Dopamine agonists
Dopamine agonists are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that act on the dopamine receptors in the brain. These compounds mimic the effects of dopamine, a neurotransmitter involved in various physiological processes such as movement, cognition, and emotions.
Dopamine agonists are commonly used in the treatment of neurological disorders, particularly Parkinson's disease and restless legs syndrome. They work by binding to dopamine receptors and stimulating them, thereby increasing dopamine activity in the brain. This helps to alleviate the symptoms associated with these conditions, such as tremors, rigidity, and muscle stiffness.
One of the key advantages of dopamine agonists is their ability to provide long-lasting relief compared to other medications. They are available in different formulations, including oral tablets, transdermal patches, and injectable solutions, allowing patients to choose the most suitable administration method.
However, like any medication, dopamine agonists may have side effects. These can include nausea, dizziness, hallucinations, and compulsive behaviors. It is important for healthcare professionals to closely monitor patients using dopamine agonists to minimize the occurrence and severity of these side effects.
In conclusion, dopamine agonists are a vital subcategory of pharmaceutical APIs used to manage Parkinson's disease and restless legs syndrome. They mimic the effects of dopamine in the brain and offer long-lasting relief from symptoms. Although they can have side effects, proper monitoring and dosage adjustments can help optimize their therapeutic benefits.
Ropinirole (Dopamine agonists), classified under Central Nervous System Agents
Central Nervous System (CNS) Agents are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that specifically target the central nervous system. The CNS encompasses the brain and spinal cord, playing a vital role in regulating and controlling various bodily functions, including cognition, movement, emotions, and sensory perception. These agents are designed to interact with specific receptors, enzymes, or ion channels within the CNS to modulate neural activity and restore normal functioning.
CNS agents comprise a diverse range of pharmaceutical APIs, including analgesics, anesthetics, antipsychotics, sedatives, hypnotics, anti-epileptics, and antidepressants. Each subcategory addresses distinct neurological disorders and conditions. For instance, analgesics alleviate pain by targeting receptors in the brain and spinal cord, while antipsychotics are employed to manage psychosis symptoms in mental illnesses such as schizophrenia.
The development of CNS agents involves rigorous research, molecular modeling, and extensive clinical trials to ensure safety, efficacy, and specific target engagement. Pharmaceutical companies invest significant resources in identifying novel drug targets, synthesizing new compounds, and optimizing their pharmacological properties. These agents undergo rigorous regulatory evaluations and must adhere to stringent quality standards and guidelines.
Given the prevalence of CNS disorders globally, the market demand for effective CNS agents is substantial. The development of innovative CNS APIs not only improves patient outcomes but also provides valuable commercial opportunities for pharmaceutical companies. Continued advancements in CNS agent research and development hold the promise of groundbreaking therapies that can improve the quality of life for individuals affected by neurological conditions.
Ropinirole API manufacturers & distributors
Compare qualified Ropinirole API suppliers worldwide. We currently have 7 companies offering Ropinirole API, with manufacturing taking place in 3 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Apollo Healthcare Resourc... | Distributor | Singapore | Singapore | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, ISO9001, JDMF, KDMF, MSDS, USDMF, WC | 200 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Ind-Swift Labs. | Producer | India | India | CoA, GMP, JDMF, USDMF, WC | 27 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Torrent Pharma | Producer | India | India | CoA, USDMF | 34 products |
| USV | Producer | India | India | CoA, GMP, USDMF, WC | 35 products |
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