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Tofisopam | CAS No: 22345-47-7 | GMP-certified suppliers
A medication that provides anxiolytic effects and supports treatment of anxiety and alcohol withdrawal without typical benzodiazepine sedation or muscle relaxation effects.
Therapeutic categories
Primary indications
- For the treatment of anxiety and alcohol withdrawal
Product Snapshot
- Tofisopam is an oral small molecule formulation
- It is primarily indicated for the treatment of anxiety and managing alcohol withdrawal symptoms
- The compound is currently in an experimental approval status with no established regulatory approvals
Clinical Overview
Unlike traditional benzodiazepines, tofisopam does not bind to the benzodiazepine binding site of the gamma-aminobutyric acid type A (GABA_A) receptor. Consequently, it lacks typical benzodiazepine-associated effects such as sedation, anticonvulsant activity, muscle relaxation, motor impairment, and amnesia. However, it retains anxiolytic properties and can enhance the anticonvulsant activity of 1,4-benzodiazepines like diazepam, without similar potentiation of other anticonvulsant drugs such as sodium valproate or carbamazepine.
The mechanism of action involves selective inhibition of certain phosphodiesterase (PDE) isoenzymes. Tofisopam demonstrates highest affinity for PDE-4A1, followed by PDE-10A1, PDE-3, and PDE-2A3, suggesting modulation of intracellular signaling pathways potentially relevant to its anxiolytic effects.
Pharmacokinetic properties, including absorption, distribution, metabolism, and excretion, have not been extensively characterized in the literature available. Tofisopam exhibits inhibitory activity on cytochrome P450 enzymes, including CYP3A4, which may influence drug-drug interaction profiles.
Safety considerations include the absence of classic benzodiazepine sedative and muscle relaxant toxicities, but comprehensive toxicological data remain limited due to regional availability and restricted approval status. Notably, the D-enantiomer of tofisopam (dextofisopam) is under clinical investigation in the United States for irritable bowel syndrome, indicating expanding potential therapeutic applications.
From a sourcing and quality perspective, procurement of tofisopam API requires verification of compliance with appropriate pharmacopeial standards and regulatory frameworks in jurisdictions where the compound is authorized. Due to its unique pharmacology and limited approval regions, secure supply chains with documented purity, enantiomeric composition, and stability data are essential for formulation and regulatory use.
Identification & chemistry
| Generic name | Tofisopam |
|---|---|
| Molecule type | Small molecule |
| CAS | 22345-47-7 |
| UNII | UZC80HAU42 |
| DrugBank ID | DB08811 |
Pharmacology
| Summary | Tofisopam is a selective phosphodiesterase (PDE) inhibitor with highest affinity for PDE-4A1, PDE-10A1, PDE-3, and PDE-2A3 isoenzymes. It exhibits anxiolytic effects without typical benzodiazepine-associated sedation or muscle relaxation by modulating intracellular cAMP and cGMP signaling pathways. Tofisopam enhances the anticonvulsant activity of certain 1,4-benzodiazepines but does not directly bind the benzodiazepine site of the GABA receptor. |
|---|---|
| Mechanism of action | Tofisopam does not bind to the benzodiazepine binding site of the gamma-aminobutyric acid receptor. One study (Rundfeldt C. et al.) has shown that tofisopam acts as an isoenzyme-selective inhibitor of phosphodiesterases (PDEs) with highest affinity to PDE-4A1 (0.42 μM) followed by PDE-10A1 (0.92 μM), PDE-3 (1.98 μM) and PDE-2A3 (2.11 μM). |
| Pharmacodynamics | Like other benzodiazepines, tofisopam possesses anxiolytic properties but unlike other benzodiazepines it does not have anticonvulsant, sedative, skeletal muscle relaxant, motor skill-impairing or amnestic properties. It enhances the anticonvulsant activity of 1,4-benzodiazepines like diazepam but not sodium valproate, carbamazepine, phenobarbital, or phenytoin. |
Targets
| Target | Organism | Actions |
|---|---|---|
| cAMP-specific 3',5'-cyclic phosphodiesterase 4A | Humans | inhibitor |
| cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A | Humans | inhibitor |
| cGMP-inhibited 3',5'-cyclic phosphodiesterase A | Humans | inhibitor |
ADME / PK
| Half-life | 6-8 hours |
|---|---|
| Metabolism | Hepatic. |
Formulation & handling
- Tofisopam is a small molecule benzodiazepine intended for oral administration due to its physicochemical properties.
- Low water solubility necessitates formulation strategies to enhance bioavailability for oral dosage forms.
- Stability and handling should consider protection from moisture and light to maintain compound integrity.
Regulatory status
Safety
| Toxicity | The onset of impairment of consciousness is relatively rapid in benzodiazepine poisoning. Onset is more rapid following larger doses and with agents of shorter duration of action. The most common and initial symptom is somnolence. This may progress to coma (Grade I or Grade II) following very large ingestions. Oral, rat LD50 is 825 mg/kg. |
|---|
- 1
- Rapid onset of central nervous system depression observed, with somnolence progressing to coma at high exposure levels
- 2
Tofisopam is a type of Anxiolytics
Anxiolytics, belonging to the pharmaceutical API (Active Pharmaceutical Ingredient) category, are substances utilized in the development of drugs aimed at treating anxiety disorders. Anxiety disorders are prevalent mental health conditions characterized by excessive worry, fear, and unease. Anxiolytics work by modulating certain neurotransmitters in the brain, such as gamma-aminobutyric acid (GABA), which plays a crucial role in reducing neuronal excitability and inducing a calming effect.
These pharmaceutical APIs have revolutionized the management of anxiety disorders, providing relief to millions of individuals worldwide. Anxiolytics can be further classified into various subcategories based on their mechanism of action, including benzodiazepines, selective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), and others.
Benzodiazepines, the most commonly prescribed anxiolytics, enhance the activity of GABA receptors, thereby producing sedative and hypnotic effects. SSRIs and SNRIs, on the other hand, primarily work by increasing the availability of serotonin and norepinephrine, respectively, in the brain, leading to a positive impact on mood and anxiety.
The development and production of anxiolytics involve stringent quality control measures to ensure their safety and efficacy. Pharmaceutical companies adhere to Good Manufacturing Practices (GMP) guidelines and conduct thorough preclinical and clinical trials to evaluate the compound's pharmacokinetics, efficacy, and adverse effects.
In conclusion, anxiolytics are a crucial category of pharmaceutical APIs used to address anxiety disorders. Through their modulation of neurotransmitters and receptors in the brain, these medications effectively alleviate symptoms and improve the quality of life for individuals affected by anxiety.
Tofisopam API manufacturers & distributors
Compare qualified Tofisopam API suppliers worldwide. We currently have 3 companies offering Tofisopam 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 |
|---|---|---|---|---|---|
| Alps Pharmaceutical | Producer | Japan | Japan | CoA, JDMF | 8 products |
| Samhwa Biopharm co.,ltd | Producer | South Korea | South Korea | BSE/TSE, CoA, GMP, MSDS | 17 products |
| Symed Labs | Producer | India | India | CoA, GMP | 28 products |
When sending a request, specify which Tofisopam 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 Tofisopam 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.
