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Olopatadine | CAS No: 113806-05-6 | GMP-certified suppliers
A medication that provides symptomatic relief of ocular itching from allergic conjunctivitis and nasal congestion from seasonal allergic rhinitis in patients aged 12 and older.
Therapeutic categories
Primary indications
- Olopatadine is indicated for the symptomatic treatment of ocular itching associated with allergic conjunctivitis as ophthalmic solution
- As a nasal spray, as a monotherapy or in combination with [mometasone furoate], olopatadine is indicated for the symptomatic relief of seasonal allergic rhinitis in patients 12 years of age and older
Product Snapshot
- Olopatadine is available primarily as ophthalmic and nasal solutions, including sprays, for topical administration
- It is used for symptomatic treatment of ocular itching related to allergic conjunctivitis and for relief of seasonal allergic rhinitis
- Olopatadine is approved for use in regulated markets including the US, EU, and Canada
Clinical Overview
Clinically, olopatadine is indicated for symptomatic relief of ocular itching associated with allergic conjunctivitis when administered as an ophthalmic solution. Additionally, as an intranasal spray—either as monotherapy or combined with mometasone furoate—it is used for symptomatic management of seasonal allergic rhinitis in patients aged 12 years and older.
Pharmacodynamically, olopatadine inhibits type 1 immediate hypersensitivity reactions by blocking H1 receptor-mediated histamine effects and stabilizing mast cells to prevent degranulation. This dual activity reduces inflammatory manifestations such as ocular itching, hyperemia, chemosis, and nasal congestion. Olopatadine demonstrates rapid onset of action, with antihistaminic effects evident within 5 minutes and sustained for up to 24 hours. It exhibits minimal affinity for alpha-adrenergic, dopamine, muscarinic, or serotonin receptors, indicating low off-target activity.
The mechanism involves highly selective antagonism at histamine H1 receptors, preventing receptor activation and downstream signaling cascades involving intracellular calcium, protein kinase C, and pathways leading to cytokine and inflammatory mediator release. Olopatadine also inhibits eosinophil activation and expression of intercellular adhesion molecules, contributing to its anti-inflammatory profile.
Regarding absorption, distribution, metabolism, and excretion (ADME), specific pharmacokinetic parameters vary by formulation; however, systemic exposure following ophthalmic or intranasal administration is low, minimizing systemic side effects. Nonetheless, ophthalmic use may cause transient blurred vision or visual disturbances in some patients. Nasal administration has occasionally been associated with somnolence. No clinically significant QT interval prolongations have been reported.
Olopatadine is marketed under various brand names including Pazeo, Patanase, and Opatanol, reflecting its use in diverse allergic conditions affecting ocular and nasal tissues.
For active pharmaceutical ingredient (API) sourcing, stringent quality control is essential to ensure batch-to-batch consistency and purity, given the drug’s high receptor selectivity and clinical safety profile. API suppliers must comply with current good manufacturing practices (cGMP) and provide comprehensive documentation, including impurity profiles and stability data, to support regulatory submissions across international markets.
Identification & chemistry
| Generic name | Olopatadine |
|---|---|
| Molecule type | Small molecule |
| CAS | 113806-05-6 |
| UNII | D27V6190PM |
| DrugBank ID | DB00768 |
Pharmacology
| Summary | Olopatadine is a selective histamine H1 receptor antagonist and mast cell stabilizer that inhibits histamine release and downstream inflammatory mediator production, including prostaglandins, cytokines, and tryptase. It modulates inflammatory responses by blocking H1 receptor signaling pathways and reducing eosinophil activation and chemotaxis. Olopatadine is primarily indicated for the symptomatic relief of allergic conjunctivitis and seasonal allergic rhinitis. |
|---|---|
| Mechanism of action | Histamine is a biogenic vasoactive amine that binds to its receptors, which are G-protein coupled receptors. Signaling through the histamine H1 receptor is thought to primarily promote the activation of inflammatory reactions, such as allergy, asthma, and autoimmune diseases. H1 receptor signaling activates the intracellular transcription factors, such as IP3, PLC, PKC, DAG, and intracellular calcium ions, which all work to activate further downstream cascades. Activated downstream cascades lead to the production of cytokines, the release of mast cell inflammatory mediators, synthesis of prostacyclins, activation of platelet factor, as well as the synthesis of nitric oxide, arachidonic acid, and thromboxane, which all contribute to inflammatory reactions. Olopatadine is an anti-allergic molecule that works via several mechanisms. As a mast cell stabilizer, it stabilizes rodent basophils and human conjunctival mast cells and inhibits the immunologically-stimulated release of histamine. Olopatadine acts as an antagonist at the histamine H1 receptors with high selectivity, which is explained by a unique receptor binding pocket that consists of the aspartate residue in the third transmembrane helix and other sites in the H1 receptor. Upon binding, olopatadine blocks the H1 receptor signaling pathway, inhibiting the release of inflammatory mediators, such as tryptase, prostaglandin D2, TNF-alpha, as well as pro-inflammatory cytokines. It also decreases chemotaxis and inhibits eosinophil activation. _In vitro_, olopatadine was shown to inhibit epithelial cell intercellular adhesion molecule-1 (ICAM-1), which promotes the recruitment of migrating pro-inflammatory mediators. |
| Pharmacodynamics | Inflammatory reactions in response to various stimuli are mediated by endogenous mediators and other pro-inflammatory factors. Histamine receptor activation and mast cell degranulation are primary mechanisms that cause inflammatory reactions such as ocular itching, hyperemia, chemosis, eyelid swelling, and tearing of seasonal allergic conjunctivitis. Olopatadine is an anti-allergenic molecule and mast cell stabilizer that inhibits the _in vivo_ type 1 immediate hypersensitivity reaction. By blocking the effects of histamine, olopatadine works to reduce the symptoms of allergies and inflammation at various sites of administration, including the eyes and nose. It has shown to exert antihistaminic effects in isolated tissues, animal models, and humans. Olopatadine also demonstrated dose-dependent inhibition of immunologically-stimulated release of histamine from rat basophilic leukemia cells and human conjunctival mast cells _in vitro_. Olopatadine has a relatively rapid onset of action and prolonged duration, where it was shown to mediate anti-histaminic effects at 5 minutes to 24 hours post-administration. While olopatadine is a non-sedating antihistamine agent, there have been reports of somnolence in some patients taking nasal olopatadine during clinical trials. Temporary blurred vision or other visual disturbances were observed following ophthalmic administration. Olopatadine has negligible effects on alpha-adrenergic, dopamine, muscarinic type 1 and 2, and serotonin receptors. In clinical trials, there was no evidence of any effect of olopatadine on QT prolongation was observed following intranasal administration. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Histamine H1 receptor | Humans | antagonist |
| Histamine H2 receptor | Humans | antagonist |
| Histamine H3 receptor | Humans | antagonist |
ADME / PK
| Absorption | Ocular administration of olopatadine in healthy subjects resulted in the Cmax of 1.6 ± 0.9 ng/mL, which was reached after about 2.0 hours. The AUC was 9.7 ± 4.4 ngxh/mL. The average absolute bioavaiability of intranasal olopatadine is about 57%. Following intranasal administration in healthy subjects, the Cmax of 6.0 ± 8.99 ng/mL at steady-state was reached between 30 minutes to 1 hour after twice daily intranasal administration. The average AUC was 66.0 ± 26.8 ng·h/mL. In patients with seasonal allergic rhinitis, the Cmax of 23.3 ± 6.2 ng/mL at steady-state was reached between 15 minutes and 2 hours post-dosing and the average AUC was 78.0 ± 13.9 ng·h/mL. |
|---|---|
| Half-life | Following ocular administration, the elimination half-life of olopatadine was 3.4 ± 1.2 hours. In oral pharmacokinetics study, the elimination half-life was reported to be 8 to 12 hours. |
| Protein binding | About 55% of total olopatadine is bound to human serum proteins, with serum albumin being the primary protein of binding. |
| Metabolism | Olopatadine undergoes hepatic metabolism in a non-extensive manner. Based on oral pharmacokinetic studies, there are at least 6 circulating metabolites in human plasma. Following topical ocular application of olopatadine, olopatadine N-oxide is formed by metabolism catalyzed by flavin-containing monooxygenase (FMO) 1 and 3 and was detected in the plasma after 4 hours post-dosing in less than 10% of the total plasma in half of the patients. Mono-desmethyl olopatadine, or N-desmethyl olopatadine, is formed by CYP3A4 and may be detected in minimal levels. |
| Route of elimination | Olopatadine is mainly eliminated through urinary excretion. Following oral administration, about 70% and 17% of the total dose was recovered in the urine and feces, respectively. |
| Volume of distribution | In an open-label study consisting of healthy Chinese subjects receiving oral administration of olopatadine, the mean apparent volume of distribution was 133.83 L. |
| Clearance | In an open-label study consisting of healthy Chinese subjects receiving oral administration of olopatadine, the mean apparent oral clearance (CL/F) was 23.45 L/h. |
Formulation & handling
- Olopatadine is a small molecule primarily formulated as ophthalmic solutions and nasal sprays, with additional oral tablet forms.
- The compound has low water solubility and moderate lipophilicity (LogP 0.75), which may require solubilization strategies in formulation.
- Stable handling considerations should account for its solid state and formulation into aqueous solutions for ocular and nasal administration routes.
Regulatory status
| Lifecycle | The API is in a mature market phase in Canada, with original patents expired by 2016, while key US patents are set to expire between 2022 and 2024, allowing for increased generic competition. The EU market status is not specified but may follow similar patent expiration trends. |
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| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Olopatadine is manufactured primarily by Alcon entities, with multiple packagers supporting distribution across the US, Canada, and EU markets. Several branded products exist, indicating a broad global presence. Patent expirations occurring between 2022 and 2024 suggest the potential for existing or imminent generic competition in these regions. |
|---|
Safety
| Toxicity | Based on the findings of an acute toxicity study in animals, the oral LD<sub>50</sub> of olopatadine was >1150 mg/kg in mice and >3870 mg/kg in rats. The Lowest published toxic dose via the oral route was 20 mg/kg in rat and 0.1 mg/kg in mouse.[MSDS] There are no known reports on overdosage following oral, ophthalmic, or intranasal administration of olopatadine. Likely symptoms of antihistamine overdose may include drowsiness in adults and, initially, agitation and restlessness, followed by drowsiness in children. In case of suspected overdose, supportive and symptomatic treatment is recommended. |
|---|
- 1
- Oral LD50 values in animal studies indicate low acute toxicity, with ›1150 mg/kg in mice and ›3870 mg/kg in rats
- 2
Olopatadine 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.
Olopatadine (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.
Olopatadine API manufacturers & distributors
Compare qualified Olopatadine API suppliers worldwide. We currently have 12 companies offering Olopatadine API, with manufacturing taking place in 7 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 |
|---|---|---|---|---|---|
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, CoA, MSDS, USDMF | 229 products |
| Curia | Producer | United States | Spain | CoA, EDMF/ASMF, GMP, MSDS, USDMF | 106 products |
| Indoco Remedies | Producer | India | India | CoA, GMP, USDMF, WC | 19 products |
| Kolon Life Science | Producer | South Korea | South Korea | CoA, JDMF | 32 products |
| Kyowa Pharma Chem. | Producer | Japan | Unknown | CoA, JDMF, USDMF | 12 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Medigraph Pharma | Producer | India | India | CoA, GMP, WC | 5 products |
| MSN Labs. | Producer | India | India | CoA, GMP, JDMF, USDMF, WC | 119 products |
| PCAS | Producer | France | Unknown | CoA, USDMF | 29 products |
| Sumitomo Chemical | Producer | Japan | Japan | CoA, JDMF | 28 products |
| Sun Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 219 products |
| USV | Producer | India | India | CoA, GMP, USDMF, WC | 35 products |
When sending a request, specify which Olopatadine 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 Olopatadine 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.
