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Rufinamide | CAS No: 106308-44-5 | GMP-certified suppliers
A medication that serves as adjunctive therapy for seizures associated with Lennox-Gastaut syndrome, providing seizure control with a tolerable safety profile in severe epileptic conditions.
Therapeutic categories
Primary indications
- Adjunct therapy for treatment of seizures associated with Lennox-Gastaut syndrome
Product Snapshot
- Rufinamide is available as oral tablets and suspensions
- It is used as adjunct therapy for the treatment of seizures associated with Lennox-Gastaut syndrome
- The product is approved in key regulatory markets including the US, Canada, and the EU
Clinical Overview
Pharmacodynamically, rufinamide acts by stabilizing neuronal membranes. It prolongs the inactive state of voltage-gated sodium channels, thereby reducing the ability of neurons to fire repetitive action potentials that propagate seizure activity. At higher concentrations, rufinamide additionally inhibits metabotropic glutamate receptor subtype 5 (mGluR5), decreasing glutamate release and excitatory neurotransmission, which may contribute to its anticonvulsant effect.
Absorption, distribution, metabolism, and excretion (ADME) parameters highlight that rufinamide is metabolized primarily via hydrolysis rather than cytochrome P450 oxidative pathways, minimizing potential for extensive CYP-mediated drug-drug interactions. Notably, it has weak inhibitory effects on CYP2E1 and acts as a weak inducer of CYP3A4 enzymes. This enzymatic profile should be considered when co-administering with other substrates metabolized by these pathways.
Safety and toxicity profiles indicate tolerance consistent with central nervous system depressants. Common adverse effects include somnolence, dizziness, and fatigue. Caution is advised in patients with impaired hepatic function due to altered metabolism and clearance.
Rufinamide is marketed under multiple brand names globally for control of refractory seizures in Lennox-Gastaut syndrome, frequently in combination with other anticonvulsants.
For API sourcing, ensure compliance with pharmacopeial standards and confirm the absence of related impurities or degradation products given its chemical class. Verification of manufacturing processes supporting consistent purity and stability profiles is critical to support formulation and regulatory requirements.
Identification & chemistry
| Generic name | Rufinamide |
|---|---|
| Molecule type | Small molecule |
| CAS | 106308-44-5 |
| UNII | WFW942PR79 |
| DrugBank ID | DB06201 |
Pharmacology
| Summary | Rufinamide is an antiepileptic agent that modulates neuronal excitability by prolonging the inactive state of voltage-gated sodium channels, thereby stabilizing neuronal membranes and inhibiting seizure propagation. At higher concentrations, it also inhibits metabotropic glutamate receptor 5 (mGluR5), reducing glutamate-mediated excitatory neurotransmission. Its primary targets include the sodium channel protein type 9 subunit alpha and mGluR5 receptors. |
|---|---|
| Mechanism of action | Rufinamide is a triazole derivative antiepileptic that prolongs the inactive state of voltage gated sodium channels thus stabilizing membranes, ultimately blocking the spread of partial seizure activity. |
| Pharmacodynamics | At high concentrations will inhibit action of mGluR5 subtype receptors thus preventing the production of glutamate. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Sodium channel protein type 9 subunit alpha | Humans | modulator |
| Metabotropic glutamate receptor 5 | Humans | inhibitor |
ADME / PK
| Absorption | The oral suspension and tablet are bioequivalent on a mg per mg basis. Rufinamide is well absorbed but the rate is slow and the extent of absorption decreases as dose is increases. Based on urinary excretion, the extent of absorption was at least 85% following oral administration of a single dose of 600 mg rufinamide tablet under fed conditions. Bioavailability= 70%-85% (decreases with increasing doses); Tmax, fed and fasted states= 4-6 hours; Cmax, 10 mg/kg/day= 4.01 µL/mL; Cmax, 30mg/kg/day= 8.68 µL/mL; AUC (0h-12h), 10mg/kg/day= 37.8±47 µg·h/mL; AUC (0h-12h), 30mg/kg/day= 89.3±59 µg·h/mL. |
|---|---|
| Half-life | Elimination half-life, healthy subjects and patients with epilepsy = 6-10 hours. |
| Protein binding | 26.3% - 34.8% with 90% binding to albumin (27%). |
| Metabolism | Rufinamide is extensively metabolized but has no active metabolites. Metabolism by carboxyesterases into inactive metabolite CGP 47292, a carboxylic acid derivative, via hydrolysis is the primary biotransformation pathway. A few minor additional metabolites were detected in urine, which appeared to be acyl-glucuronides of CGP 47292. The cytochrome P450 enzyme system or glutathiones are not involved with the metabolism of rufinamide. Rufinamide is a weak inhibitor of CYP 2E1. Rufinamide is a weak inducer of CYP 3A4 enzymes. |
| Route of elimination | Renally (91%; 66% as CGP 47292, 2% as unchanged drug) and fecally (9%) eliminated. |
| Volume of distribution | Rufinamide was evenly distributed between erythrocytes and plasma. The apparent volume of distribution is dependent upon dose and varies with body surface area. The apparent volume of distribution was about 50 L at 3200 mg/day. Volume of distribution is similar between adults and children and is non-linear. |
Formulation & handling
- Rufinamide is a small molecule drug formulated primarily for oral administration in tablet and suspension forms.
- The API exhibits moderate water solubility and a low to moderate logP, influencing formulation strategies for bioavailability enhancement.
- Administration with food is recommended to improve systemic absorption, which should be considered in dosage form design.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is in a mature market phase in the US, Canada, and EU, with key patent protections having expired between 2018 and 2023, allowing for generic competition in these regions. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Rufinamide is supported by a limited number of originator companies supplying branded products primarily across the US, Canada, and EU markets. Multiple patents in the United States have recently expired or are near expiration, indicating the potential presence or forthcoming introduction of generic competition. This landscape suggests an evolving supply environment with opportunities for both branded and generic API sourcing. |
|---|
Safety
| Toxicity | The most commonly observed adverse reactions (≥10% and greater than placebo) were headache, dizziness, fatigue, somnolence, and nausea. |
|---|
- Exposure may cause CNS-related adverse effects including headache, dizziness, somnolence, and fatigue
- Handle with appropriate protective equipment to minimize inhalation or dermal contact
- In case of accidental exposure, monitor for neurological symptoms and implement supportive measures
Good Manufacturing Practices
Active pharmaceutical ingredients are made in GMP-certified manufacturing facilities. GMP stands for Good Manufacturing Practices and is the main standard in the pharmaceutical industry. cGMP or Current GMP means that the company complies with the most recent requirements/version of GMP. The WHO has its own guideline for GMP, the World Health Organization or WHO GMP. The authority that has audited the company can also be from a country like China (Chinese GMP) or from the EU (EU GMP), every authority has different GMP requirements.
Rufinamide is a type of Anticonvulsants
Anticonvulsants are a vital category of pharmaceutical Active Pharmaceutical Ingredients (APIs) used for the treatment of seizures and epilepsy. These APIs play a crucial role in managing and preventing convulsions, which are characterized by abnormal electrical activity in the brain. With a significant demand for effective anticonvulsant medications, these APIs hold immense importance in the pharmaceutical industry.
Anticonvulsant APIs work by stabilizing the excessive electrical activity in the brain, preventing or reducing seizures. They achieve this by targeting specific receptors or channels involved in the regulation of neuronal excitability. Some commonly used anticonvulsant APIs include phenytoin, valproic acid, carbamazepine, and lamotrigine.
Pharmaceutical companies utilize these APIs to formulate various dosage forms, such as tablets, capsules, and oral suspensions, ensuring convenient administration for patients. Additionally, anticonvulsant APIs may also be employed in the development of extended-release formulations, providing sustained and controlled drug release.
The market for anticonvulsant APIs continues to grow due to the rising prevalence of epilepsy and other seizure disorders. Moreover, ongoing research and development efforts aim to enhance the efficacy, safety, and tolerability of these APIs, ensuring better treatment outcomes for patients.
In conclusion, anticonvulsant APIs are a crucial pharmaceutical category used to manage seizures and epilepsy. With their ability to stabilize brain activity, these APIs play a pivotal role in improving the quality of life for individuals living with these conditions. The pharmaceutical industry's continued focus on research and development in this area ensures the availability of advanced and effective anticonvulsant medications for patients in need.
Rufinamide API manufacturers & distributors
Compare qualified Rufinamide API suppliers worldwide. We currently have 6 companies offering Rufinamide API, with manufacturing taking place in 2 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 |
|---|---|---|---|---|---|
| Amino Chemicals | Producer | Malta | Malta | CoA, GMP | 20 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Lupin | Producer | India | India | CoA, USDMF | 155 products |
| MSN Labs. | Producer | India | India | CoA, GMP, USDMF, WC | 119 products |
| MSN Life Sciences | Producer | India | India | CoA, USDMF | 46 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
When sending a request, specify which Rufinamide API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Rufinamide API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
