Bilastine’s Key Specifications & Technical Data
- CAS Number：202189-78-4
- Molecular Formula：C28H37N3O3
- Molecular Weight：463.62 g/mol
- Assay (Purity)：≥ 99% (HPLC)
- Appearance：White to Off-White Crystalline Powder
- Grade：Pharmaceutical Grade / Compounding Grade
- Standard Compliance：GMP, ICH Q7, USP/EP/BP
What is Bilastine?
Bilastine (CAS: 202189-78-4) is a chemically synthesized active pharmaceutical ingredient.It is an API used to produce bilastine tablets and other formulations.It can be used for the treatment of allergic diseases, such as urticaria and allergic rhinitis/rhinoconjunctivitis.
Bilastine is a second-generation, long-acting, non-sedating antihistamine.Compared to first-generation antihistamines (chlorpheniramine, diphenhydramine, promethazine and etc.),it possesses three core advantages: higher selectivity for H1 receptors, inability to cross the blood-brain barrier, and an absence of cardiotoxicity.It has currently been incorporated into allergy treatment guidelines in over 20 countries worldwide.
Why choose Highassay?
Highassay is a China-based supplier of Bilastine APIs. We provide high-purity Bilastine APIs (≥99%) that comply with multiple pharmacopoeias (EP/USP/CP). Our production facilities adhere to GMP standards, ensuring the quality and safety of our products.
Stable Supply：Our manufacturing process for Bilastine API is mature, and we possess the capability to ensure a stable, long-term supply.We commit to shipping within 7–15 days, for your product production schedule remains unaffected.
Flexible Packaging：
We offer many kinds of packaging options to meet maximum convenience for your needs:
– Small-Batch / Sample Orders: Aluminum foil bags + light-shielding bags (1 kg, 5 kg, etc.)
– Bulk Orders: Cardboard drums + double-layer PE liners (25 kg — standard packaging)
– Customized packaging is also available.
After-Sales Service：Each batch of Bilastine powder is accompanied by a COA and MSDS. All products are fully traceable; in the event of any quality issues, we offer return and exchange services (subject to the terms and conditions stipulated in the contract).
For bulk purchases of Bilastine API, choose Highassay. Contact us to obtain free samples and the latest quotes for Bilastine.
Mechanism of Action of Bilastine
Bilastine is a highly selective peripheral H1 receptor antagonist that competitively blocks the binding of histamine to H1 receptors, thereby inhibiting histamine-mediated allergic reactions such as sneezing, rhinorrhea, and edema;
Due to its high selectivity for peripheral H1 receptors and its negligible penetration of the blood-brain barrier into the central nervous system, it effectively avoids central sedative effects, thereby offering superior clinical safety;
It does not block cardiac potassium channels and is a new generation of Bilastine antihistamine API.
Bilastine ‘s Key Pharmacological Data
- Onset of Action: Peak plasma concentration is reached 1 hour after administration on an empty stomach.
- Half-life: Approximately 14.5 hours.
- Metabolic Pathway: Independent of the CYP450 enzyme system.
- Central Sedation: Negligible.
- Cardiac Safety: No clinically significant prolongation of the QT interval.
Note: Bilastine significantly reduces the side effects associated with traditional antihistamines while maintaining therapeutic efficacy.
Yes, they can be used together. Combining bilastine with montelukast (an anti-leukotriene anti-inflammatory agent) creates a dual-pathway anti-allergic approach, which is effective against stubborn and recurrent allergies.
All four are second-generation antihistamines. Bilastine’s advantages lie in its non-sedating profile, independence from hepatic metabolism, and lack of cardiac risk. Clinical data also show it is more effective at relieving nasal congestion.
Bilastine is characterized by its rapid onset of action (1-2 hours) and long half-life (14.5 hours), allowing for once-daily dosing without significant weight gain or drowsiness.
We can provide a complete set of registration documents; please contact us directly for confirmation.
Standard minimum order quantity is 1 kg; sample orders are supported.
Yes. Bilastine eye drops are already available on the market in Canada, while the nasal drops are currently still in the R&D phase; however, the raw materials are available to support the development of these related dosage forms.
The price of Bilastine API fluctuates based on order quantity, procurement cycle, and market conditions. Please contact us for a real-time quote.
Indications and Formulations of Bilastine
Formulation Type | Common Strength | Main Indications |
| Tablets | 20 mg | Seasonal / perennial allergic rhinitis, chronic idiopathic urticaria |
| Orally Disintegrating Tablets | 10 mg / 20 mg | For patients with swallowing difficulties; can be taken without water |
| Oral Solution | 2.5 mg/mL | Pediatric and geriatric patients; flexible dose adjustment |
| Eye Drops | 6 mg/mL | Allergic conjunctivitis (approved in Canada) |
| Nasal Drops | Under development | Local administration for allergic rhinitis (not yet marketed) |
Specifications of Bilastine
| Test Item | Specification |
| Description | White to almost white crystalline powder |
| Assay (HPLC) | ≥ 99.0% |
| Individual Impurity | ≤ 0.1% |
| Total Impurities | ≤ 0.5% |
| Loss on Drying | ≤ 0.5% |
| Residual Solvents | Complies with ICH Q3C |
| Heavy Metals | ≤ 10 ppm |
Note：It can simultaneously comply with the EP (European Pharmacopoeia) or internal corporate standards; specific terms are subject to the contract.
