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Bilastine | CAS No: 202189-78-4 | GMP-certified suppliers
A medication that provides symptomatic relief for seasonal allergic rhinitis in adolescents and adults and helps manage chronic spontaneous urticaria symptoms in adult patients.
Therapeutic categories
Primary indications
- For symptomatic relief of nasal and non-nasal symptoms of seasonal rhinitis in patients 12 years of age and older and for symptomatic relief in chronic spontaneous urticaria in patients 18 years of age and older [FDA Label]
Product Snapshot
- Bilastine is supplied as an oral small‑molecule antihistamine with available tablet, orally disintegrating tablet, solution, and ophthalmic solution formulations
- It is used for symptomatic control of seasonal allergic rhinitis and chronic spontaneous urticaria
- It is marketed in Canada with approved and investigational status across different formulations
Clinical Overview
Bilastine exhibits high selectivity for the histamine H1 receptor, with reported affinity in the nanomolar range. By competitively inhibiting H1 receptor activation during mast cell degranulation, it mitigates the cascade of histamine‑mediated effects underlying nasal congestion, pruritus, and urticarial wheals. Its pharmacodynamic profile aligns with a low potential for central nervous system penetration, supporting its classification as a non-sedating antihistamine.
Absorption is generally rapid when administered in the fasting state, and food or certain fruit juices may reduce bioavailability due to interactions with intestinal transporters such as OATP2B1. Bilastine is minimally metabolized, with most of the administered dose excreted unchanged, primarily in feces and to a lesser extent in urine. The elimination half-life supports once‑daily dosing in clinical use.
Safety considerations include dose‑related risks of somnolence in susceptible individuals and potential QTc interval prolongation, although clinically meaningful events remain uncommon when used at approved doses. Bilastine does not undergo significant hepatic metabolism, reducing the likelihood of metabolic drug–drug interactions, though transporter-mediated interactions remain relevant. Use in younger pediatric populations or special populations should follow local regulatory guidance.
Bilastine is marketed in multiple regions under various brand names, often as oral tablets or solutions. For API procurement, sourcing should prioritize manufacturers adhering to Good Manufacturing Practice, with attention to impurity profiles, particle characteristics, and transporter‑interaction data requirements relevant to regulatory submissions.
Identification & chemistry
| Generic name | Bilastine |
|---|---|
| Molecule type | Small molecule |
| CAS | 202189-78-4 |
| UNII | PA1123N395 |
| DrugBank ID | DB11591 |
Pharmacology
| Summary | Bilastine is a selective histamine H1‑receptor antagonist that blocks histamine‑mediated signaling released during mast‑cell degranulation. By preventing H1‑receptor activation, it reduces downstream pathways that drive allergic symptoms. Its pharmacodynamic effect is characterized by antihistaminic activity relevant to seasonal allergic rhinitis and chronic spontaneous urticaria. |
|---|---|
| Mechanism of action | Bilastine is a selective histamine H1 receptor antagonist (Ki = 64nM) [FDA Label]. During allergic response mast cells undergo degranulation which releases histamine and other subastances. By binding to and preventing activation of the H1 receptor, bilastine reduces the development of allergic symptoms due to the release of histamine from mast cells. |
| Pharmacodynamics | Bilastine is an antiallergenic and acts to reduce allergic symptoms such as nasal congestion and urticaria [FDA Label]. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Histamine H1 receptor | Humans | antagonist |
ADME / PK
| Absorption | Bilastine has a Tmax of 1.13 h [FDA Label]. The absolute bioavailability is 61%. No accumulation observed with daily dosing of 20-100 mg after 14 days. Cmax decreased by 25 % and 33% when taken with a low fat and high fat meal compared to fasted state. Administration with grapefruit juice decreased Cmax by 30%. |
|---|---|
| Half-life | The mean half life of elimination is 14.5h [FDA Label]. |
| Protein binding | Bilastine is 84-90% bound to human plasma proteins [FDA Label]. |
| Metabolism | Bilastine does not interact with the cytochrome P450 system and does not undergo significant metabolism in humans [FDA Label]. |
| Route of elimination | Bilastine is mainly excreted in the feces (66.5%) with some excreted in the urine (28.3%) [FDA Label]. Nearly all is excreted as the parent compound. |
| Clearance | Bilastine has a total clearance is 9.20 L/h and a renal clearance of 8.7 L/h [FDA Label]. |
Formulation & handling
- Oral formulations must address very low aqueous solubility; absorption is food‑sensitive, so designs often avoid high‑fat or fruit‑juice coadministration contexts.
- As a small‑molecule benzimidazole derivative in solid form, it is suitable for conventional tablet and ODT processing with standard stability profiles.
- Ophthalmic solutions require solubilization strategies and pH/osmolality control due to limited intrinsic water solubility.
Regulatory status
| Lifecycle | Patent expiry information was not provided, so the lifecycle can only be described in general terms. In Canada, the API’s lifecycle position depends on its patent status, with products typically transitioning to a mature, competitive market once key protections expire. |
|---|
| Markets | Canada |
|---|
Supply Chain
| Supply chain summary | Bilastine is produced globally from a single originator developer, with manufacturing supported by multiple regional licensees for finished‑dose distribution. Branded products are marketed across the EU and many international markets, while the drug is not approved in the United States and is sold in Canada under the Blexten brand. Core patent protections have largely expired, indicating that generic competition is present or emerging in several regions. |
|---|
Safety
| Toxicity | The most common adverse effects experienced during clinical trials were abdominal pain, dizziness, headache, and somnolence [FDA Label]. Bilastine is associated with Q/T prolongation. The no observed adverse effect level of bilastine is 1200 mg/kg/day in rats and 125 mg/kg/day in dogs . |
|---|
- Clinical data note frequent CNS and GI adverse effects (e
- G
- , somnolence, dizziness, headache, abdominal discomfort), indicating a need to control exposure during handling to limit operator contact with aerosolized or powdered material
Certificate of Analysis
A CoA is a document issued by a companies’ QA/QC-department that confirms that a product meets its product specification and is part of the quality control of a product batch. The CoA commonly contains results obtained from laboratory tests of an individual batch of a product. There are different international standards to which a product can be tested, for example: Ph. Eur. | EP – (European Pharmacopoeia) USP – (United States Pharmacopeia)
Bilastine 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.
Bilastine (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.
Bilastine API manufacturers & distributors
Compare qualified Bilastine API suppliers worldwide. We currently have 11 companies offering Bilastine API, with manufacturing taking place in 6 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 |
|---|---|---|---|---|---|
| ACE Japan | Producer | Japan | Japan | CoA | 76 products |
| AXXO GmbH | Distributor | Germany | World | CoA, GMP, GDP, MSDS, USDMF | 243 products |
| Faes Farma | Producer | Spain | Spain | CoA, GMP | 2 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| MSN Life Sciences | Producer | India | India | CoA, WC | 46 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Symed Labs | Producer | India | India | CoA, GMP | 28 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
| Valence Labs | Producer | India | India | CoA, GMP | 32 products |
| Veeprho Group | Producer | Czech Republic | Czech Republic | CoA | 144 products |
| Zhejiang Hengkang Pharmac... | Producer | China | China | BSE/TSE, CoA, MSDS, USDMF | 31 products |
When sending a request, specify which Bilastine 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 Bilastine 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.
Frequently asked questions about Bilastine API
Sourcing
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Technical
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Regulatory
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Pharmaoffer
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