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Bepotastine | CAS No: 125602-71-3 | GMP-certified suppliers
A medication that provides symptomatic relief of itchy eyes caused by allergic conjunctivitis through antihistamine and mast cell stabilization effects.
Therapeutic categories
Primary indications
- For the symptomatic treatment of itchy eyes (caused by IgE-induced mast cell degranulation) due to allergic conjunctivitis
Product Snapshot
- Bepotastine is available as ophthalmic solutions and oral film-coated tablets
- It is indicated for the symptomatic treatment of allergic conjunctivitis-related itchy eyes caused by IgE-mediated mast cell degranulation
- The product is approved for use in the US and Canadian markets
Clinical Overview
This agent acts through multiple mechanisms. It blocks the histamine H1 receptor to prevent histamine-induced symptoms such as pruritus. Additionally, bepotastine stabilizes mast cells, inhibiting further release of inflammatory mediators, and suppresses eosinophil migration to inflamed ocular tissues, thereby mitigating the progression of allergic inflammation. These combined actions contribute to reduction of itching and other allergic conjunctivitis symptoms.
Bepotastine belongs to the second-generation piperidine class of antihistamines, characterized by minimal penetration of the blood-brain barrier, which explains its reduced sedative potential. Pharmacodynamically, onset of action occurs within 15 minutes (0.25 hours), with a duration spanning 12 to 24 hours. The compound demonstrates selectivity, lacking significant interaction with serotonin, muscarinic, benzodiazepine, or beta-adrenergic receptors, which is associated with a lower incidence of anticholinergic side effects such as dry mouth or somnolence.
Metabolically, bepotastine is primarily eliminated via renal excretion, consistent with its classification among drugs mainly renally eliminated. Safety data support its use in approved ocular and oral formulations, though toxicity profiles should be reviewed in special populations, including those with renal impairment.
Bepotastine has been approved since 2000 in Japan for allergic rhinitis and urticaria, with ophthalmic solutions approved by the US FDA in 2009 for allergic conjunctivitis. The compound is marketed by Tanabe Seiyaku Co., Ltd. under the brand name Talion (oral and ophthalmic in Japan) and as Bepreve ophthalmic solution in the United States.
For API sourcing and quality control, practitioners should ensure compliance with pharmacopeial standards and verify purity, stability, and batch-to-batch consistency. As bepotastine is supplied for sensitive ocular applications, strict adherence to GMP and appropriate documentation to support regulatory filings are critical considerations.
Identification & chemistry
| Generic name | Bepotastine |
|---|---|
| Molecule type | Small molecule |
| CAS | 125602-71-3 |
| UNII | HYD2U48IAS |
| DrugBank ID | DB04890 |
Pharmacology
| Summary | Bepotastine is a selective histamine H1 receptor antagonist that inhibits allergen-induced mast cell degranulation responsible for symptoms of allergic conjunctivitis. It also functions as a mast cell stabilizer and reduces eosinophil migration to inflamed conjunctival tissues, mitigating allergic inflammation. This mechanism targets the IgE-mediated hypersensitivity cascade to alleviate ocular itching without significant interaction with other receptor systems. |
|---|---|
| Mechanism of action | Because of a type 1 hypersensitivity reaction cascade that is triggered by antigen exposure, allergic conjunctivitis occurs. Allergen exposure is followed by conjunctival mast cell degranulation and histamine released as a result of the formation of complementary IgE cross-links on the conjunctiva. Due to the release of histamine, symptoms such as itching can be observed. Bepotastine works to relieve itchy eyes by three primary mechanisms of action. It is a non-sedating, selective antagonist of the histamine 1 (H1) receptor, a mast cell stabilizer, and it suppresses the migration of eosinophils into inflamed tissues to prevent tissue damage and worsening of allergic inflammation of the conjunctiva. |
| Pharmacodynamics | Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor. It belongs to the second-generation piperidine chemical class. It is a mast cell stabilizer and suppresses the migration of eosinophils into inflamed tissues. Furthermore, bepotastine does not interact with serotonin, muscarinic, benzodiazepine, and beta-adrenergic receptor that would otherwise result in adverse reactions such as dry mouth or sonmolence. Onset of action = 0.25 hours; Duration of action = 12-24 hours; |
Targets
| Target | Organism | Actions |
|---|---|---|
| Histamine H1 receptor | Humans | antagonist |
ADME / PK
| Absorption | Tmax, after single dose, opthalmic = 1.2 hours; Cmax, 1.5%, opthalmic dose = 7.3 ±1.9 ng/mL; After 24 hours post-installation, levels of bepotastine are below quantifiable limit of 2 ng/mL. Minimal systemic absorption with opthalmic dosage form. |
|---|---|
| Half-life | Elimination half life = 2.5 hours |
| Protein binding | 55.4% mean plasma protein binding with 10 mg oral dose. Extent of protein binding is independent of plasma drug concentration. |
| Metabolism | Minimal metabolism via CYP enzymes |
| Route of elimination | When a oral dose of 2.5 - 40 mg bepotastine is given, 75%-90% of the dose was excreted unchanged in the urine by 24 hours. |
Formulation & handling
- Bepotastine is formulated for both oral administration as film-coated tablets and topical ophthalmic solutions for conjunctival use.
- As a small molecule with moderate water solubility and low LogP, it is suitable for aqueous ophthalmic formulations and oral delivery.
- Oral bioavailability is not significantly affected by food intake, allowing flexible dosing with regard to meals.
Regulatory status
| Lifecycle | The API's primary patents in the United States expired between 2019 and 2024, indicating that the market, including the US and Canada, has entered a mature phase with potential generic competition. Ongoing product availability in these regions reflects established market adoption post-patent expiry. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Bepotastine is supplied primarily by originator companies with branded products focused on the US and Canadian markets. Multiple US patents have recently expired or are nearing expiration between 2019 and 2024, indicating established or imminent generic competition. The product is available in various formulations, including ophthalmic solutions, reflecting a specialized supply landscape. |
|---|
Bepotastine is a type of Antihistamines
Antihistamines are a vital subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) widely used in the treatment of allergies and allergic reactions. These compounds work by blocking the action of histamines, which are responsible for triggering allergic symptoms such as itching, sneezing, runny nose, and watery eyes.
Antihistamines can be classified into two main categories: first-generation and second-generation antihistamines. First-generation antihistamines, such as diphenhydramine and chlorpheniramine, have been in use for several decades. They are effective in relieving allergy symptoms but are associated with drowsiness and other side effects due to their ability to cross the blood-brain barrier.
On the other hand, second-generation antihistamines, including cetirizine, loratadine, and fexofenadine, offer similar allergy relief with fewer sedative effects. These newer antihistamines are preferred for their improved safety profiles, making them suitable for use during the day without causing significant drowsiness.
Antihistamines are available in various forms, including tablets, capsules, syrups, and topical creams. They are extensively used to manage conditions such as hay fever, hives, allergic rhinitis, and insect bites. Moreover, antihistamines may also be combined with decongestants or other medications to provide relief from nasal congestion and sinus symptoms.
As pharmaceutical APIs, antihistamines are produced through meticulous synthesis and manufacturing processes, adhering to strict quality standards. These APIs serve as the active components in various branded and generic pharmaceutical formulations, making them crucial in the pharmaceutical industry's production of allergy medications.
In conclusion, antihistamines are a significant subcategory of pharmaceutical APIs widely used for alleviating allergy symptoms. Their classification into first- and second-generation antihistamines offers options based on efficacy and sedative effects. By blocking histamines, antihistamines provide relief from common allergic reactions, making them essential in the development of effective allergy medications.
Bepotastine (Antihistamines), 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.
Bepotastine API manufacturers & distributors
Compare qualified Bepotastine API suppliers worldwide. We currently have 5 companies offering Bepotastine API, with manufacturing taking place in 4 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 |
|---|---|---|---|---|---|
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Hanmi Fine Chemical | Producer | South Korea | South Korea | CoA, JDMF | 18 products |
| ICROM | Producer | Italy | Italy | CoA, GMP, USDMF | 19 products |
| MSN Labs. | Producer | India | India | CoA, USDMF | 119 products |
| Osaka Synthetic Chemical ... | Producer | Japan | Japan | CoA, JDMF | 16 products |
When sending a request, specify which Bepotastine 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 Bepotastine 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.
