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Ketotifen | CAS No: 34580-13-7 | GMP-certified suppliers
A medication that provides anti-allergic and anti-asthmatic benefits for mild atopic asthma in children and temporary relief of ocular itching due to allergic conjunctivitis.
Therapeutic categories
Primary indications
- Administered orally, ketotifen is indicated as an add-on medication in the chronic treatment of mild atopic asthma in children
- It is also available as an over-the-counter ophthalmic solution which is indicated for the temporary prevention of itching of the eye due to allergic conjunctivitis
Product Snapshot
- Ketotifen is available in multiple oral and ophthalmic formulations including tablets, syrups, capsules, gels, and ophthalmic solutions/drops
- It is primarily used as an add-on treatment for mild atopic asthma in children and for temporary relief of allergic conjunctivitis-related eye itching
- Ketotifen is approved for use in regulatory markets including the US and Canada
Clinical Overview
Clinically, ketotifen is utilized for its anti-allergic and anti-asthmatic effects. Orally administered ketotifen serves as an add-on therapy for mild atopic asthma in pediatric populations, primarily in Canada and Europe. The therapeutic benefit in asthma arises from its non-bronchodilator activity reducing inflammatory mediator effects. It is also available as an over-the-counter ophthalmic formulation in the United States for temporary relief of itching associated with allergic conjunctivitis.
Pharmacodynamically, ketotifen functions as a potent, non-competitive antagonist at histamine H1 receptors and stabilizes mast cells. This dual mechanism inhibits the release of allergic and inflammatory mediators such as histamine, leukotrienes C4 and D4, and platelet-activating factor. Additional effects observed in vivo include reduction of airway hyperreactivity, suppression of eosinophil priming, and mitigation of leukotriene-induced bronchoconstriction. Therapeutic effects in asthma may require 6 to 12 weeks of treatment to become evident.
Pharmacokinetic data indicate that ketotifen undergoes metabolism involving UGT1A3 and UGT1A4 enzymes, although detailed absorption, distribution, metabolism, and excretion parameters are limited in publicly available sources.
Safety considerations warrant attention to known antihistaminic class effects, including potential sedation and anticholinergic side effects. Ketotifen's systemic use in asthma and allergy necessitates monitoring for tolerability especially in pediatric patients.
Notable brands and markets for ketotifen include oral prescription formulations in Canada and Europe, and ophthalmic OTC products in the United States. Its use is extended to various allergic conditions including urticaria, mastocytosis, and food allergy management in select regions.
For API procurement, ketotifen requires strict adherence to quality standards specifying purity, residual solvents, and residual sulfur-containing impurities consistent with global regulatory requirements. Suppliers should provide comprehensive certificates of analysis and support compliance with relevant pharmacopeial monographs to ensure reproducible performance in formulation development.
Identification & chemistry
| Generic name | Ketotifen |
|---|---|
| Molecule type | Small molecule |
| CAS | 34580-13-7 |
| UNII | X49220T18G |
| DrugBank ID | DB00920 |
Pharmacology
| Summary | Ketotifen acts primarily as a non-competitive antagonist of histamine H1 receptors and a mast cell stabilizer, inhibiting the release of allergic and inflammatory mediators such as histamine, leukotrienes, and platelet-activating factor. Its pharmacodynamic effects include suppression of airway hyperreactivity, eosinophil activation, and prevention of leukotriene-induced bronchoconstriction. These actions contribute to its therapeutic use in managing allergic conditions and mild atopic asthma. |
|---|---|
| Mechanism of action | The precise mechanism(s) through which ketotifen exerts its therapeutic effects are unclear. Ketotifen is a potent and non-competitive antagonist of H1 histamine receptors, which is likely to be a significant contributor to its anti-allergic activity. In addition, ketotifen stabilizes mast cells and has demonstrated _in vitro_ the ability to inhibit the release of allergic and inflammatory mediators such as histamine, leukotrienes C<sub>4</sub> and D<sub>4</sub> (i.e. SRS-A), and platelet-activating factor (PAF). Other _in vivo_ observations thought to contribute to ketotifen's efficacy in asthma include the inhibition of various PAF-mediated processes (e.g. airway hyperreactivity, eosinophil and platelet accumulation in the airways), prevention of leukotriene-induced bronchoconstriction, and suppression of eosinophil priming. |
| Pharmacodynamics | Ketotifen is a non-competitive histamine antagonist and mast cell stabilizer. Administered orally, it functions as a non-bronchodilator antiasthmatic drug by inhibiting the effects of endogenous substances known to be inflammatory mediators. While effects can take 6 to 12 weeks to become apparent, the use of ketotifen has been demonstrated to reduce the frequency, severity, and duration of asthma symptoms, and may allow for a reduction in the use of other asthma therapies. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Histamine H1 receptor | Humans | antagonist |
| 6-phosphogluconate dehydrogenase, decarboxylating | Humans | inhibitor |
ADME / PK
| Absorption | Following oral administration, absorption is relatively quick (with a T<sub>max</sub> of ~3 hours) and nearly complete as judged by plasma concentrations and urinary excretion levels - despite this, oral bioavailability is only ~50% due to a significant first-pass effect in the liver. |
|---|---|
| Half-life | Ketotifen clearance is biphasic - the half-life of the distribution phase is approximately 3-5 hours and the half-life of the elimination phase is 22 hours. |
| Protein binding | Ketotifen is 75% protein-bound in plasma, though the specific proteins to which it binds are unclear. |
| Metabolism | Ketotifen is extensively metabolized in humans and three distinct metabolites have been detected in human urine. The main metabolite is the N-glucuronide, comprising roughly 50% of urinary drug product, with the N-demethylated nor-ketotifen and the 10-hydroxyl derivative comprising 2% and <1%, respectively. Nor-ketotifen appears to be equally as active as its parent drug, though the clinical relevance of this is unclear given the relatively small proportion in which nor-ketotifen is found in the plasma. Formation of the N-glucuronide metabolite is carried out by several UGT enzymes, including UGT1A3, UGT1A4, and UGT2B10. |
| Route of elimination | More than 60% of an administered dose is excreted in the urine, primarily as metabolites - of this material, <1% is found as unchanged drug, while the glucuronide and pharmacologically active nor-ketotifen metabolites account for 50% and 10%, respectively. |
Formulation & handling
- Ketotifen is a small molecule API formulated for oral and ophthalmic use, including extended-release oral tablets and ophthalmic solutions or gels.
- The compound exhibits low water solubility (7.87 mg/L) and a moderate logP (3.35), indicating consideration for solubilization strategies in formulation development.
- Ketotifen can be administered with or without food, as food intake does not significantly impact its pharmacokinetics.
Regulatory status
| Lifecycle | The API is currently protected by patents expiring in the United States in 2028 and 2030, with marketed products primarily in the US and Canada. Post-patent expiry, increased generic competition is expected, reflecting a transition toward market maturity. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | The manufacturing landscape for ketotifen includes multiple originator companies involved in both production and packaging, reflecting a diversified supply base. Branded ketotifen products have an established presence primarily in the US and Canadian markets. Patent protection extending into 2028 and 2030 indicates that generic competition is limited or forthcoming rather than currently widespread. |
|---|
Safety
| Toxicity | Oral ingestion of up to 60x the recommended dose has been reported, although no fatal overdoses of ketotifen have been described. Symptoms of ketotifen overdosage may include significant sedation, confusion, disorientation, tachycardia, hypotension, convulsions, hyperexcitability (particularly in children), and/or reversible coma. If ingestion is recent, consider the use of gastric lavage or activated charcoal. Other treatments should be supportive and administered as necessary based on symptoms. Physostigmine may be useful to mitigate anticholinergic effects, and short-acting barbiturates or benzodiazepines may be used if the patient presents with excitation or convulsions. |
|---|
- Ketotifen exhibits central nervous system toxicity at high doses, with symptoms including sedation, confusion, tachycardia, hypotension, convulsions, and reversible coma
- Overdose management is primarily supportive
- Physostigmine may be considered for anticholinergic symptoms, and anticonvulsants for seizure control
Ketotifen 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.
Ketotifen (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.
Ketotifen API manufacturers & distributors
Compare qualified Ketotifen API suppliers worldwide. We currently have 3 companies offering Ketotifen API, with manufacturing taking place in 2 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 |
|---|---|---|---|---|---|
| Quimdis | Distributor | France | Unknown | CoA | 17 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, GMP, ISO9001, MSDS, USDMF | 764 products |
| Zhejiang Supor | Producer | China | China | CoA, GMP, USDMF | 13 products |
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