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Terfenadine acid metabolite (Fexofenadine) API Manufacturers & Suppliers
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Fexofenadine | CAS No: 83799-24-0 | GMP-certified suppliers
A medication that provides reliable relief of allergic rhinitis and chronic idiopathic urticaria symptoms for key regulated markets, supporting consistent supply needs for formulation development.
Therapeutic categories
Primary indications
- In the United States, fexofenadine is indicated for the symptomatic treatment of allergic rhinitis in patients ≥2 years old and chronic idiopathic urticaria in patients ≥6 months old
- In Canada, fexofenadine carries the same indications but is approved only for patients ≥12 years old
- Fexofenadine is also available in combination with [pseudoephedrine] for the symptomatic treatment of season allergic rhinitis in patients ≥12 years old
Product Snapshot
- Fexofenadine is an oral small‑molecule antihistamine available in multiple solid and liquid dosage forms
- Its primary uses are for allergic rhinitis and chronic idiopathic urticaria, including availability in combinations such as with pseudoephedrine for seasonal allergy symptoms
- It is approved in the United States and Canada, with additional investigational listings in some regulatory references
Clinical Overview
The molecule is the primary active metabolite of terfenadine and is administered as a racemic mixture, with both enantiomers contributing similar antihistamine activity. Structurally it belongs to the diphenylmethane class, characterized by a diphenylmethane core with two phenyl substitutions.
Pharmacologically, fexofenadine acts as a selective inverse agonist at the H1 histamine receptor. By stabilizing the inactive receptor conformation, it prevents histamine-mediated activation of downstream inflammatory pathways. This reduces pruritus, rhinorrhea, sneezing, and ocular symptoms associated with allergen-triggered mast cell and basophil degranulation. It shows minimal affinity for dopaminergic, serotonergic, cholinergic, or adrenergic receptors and demonstrates limited central nervous system penetration.
After oral administration, absorption is rapid with symptom relief typically beginning within one to three hours. Fruit juices can decrease absorption through effects on intestinal transporters. The duration of action is approximately 24 hours, enabling once-daily or twice-daily regimens depending on clinical needs. Fexofenadine is a substrate for several transporters, including P-glycoprotein, OATP1B1, OATP1B3, OATP2B1, and OAT3, which influence its distribution and clearance. It undergoes minimal hepatic metabolism and is primarily eliminated unchanged.
Safety considerations include its generally low sedative potential due to negligible blood‑brain barrier penetration and lack of notable off‑target receptor activity. Clinically relevant drug interactions mainly involve transporter modulation rather than cytochrome P450 pathways.
For API procurement, sourcing should focus on verifying enantiomeric consistency, transporter interaction data, and compliance with global pharmacopeial specifications to ensure suitability for regulated markets.
Identification & chemistry
| Generic name | Fexofenadine |
|---|---|
| Molecule type | Small molecule |
| CAS | 83799-24-0 |
| UNII | E6582LOH6V |
| DrugBank ID | DB00950 |
Pharmacology
| Summary | Fexofenadine is an inverse agonist of the H1 histamine receptor that stabilizes the receptor’s inactive state and blocks histamine‑mediated inflammatory signaling. By preventing activation of H1 receptors on mast cells and basophils, it reduces downstream cytokine release associated with allergic symptoms. It is peripherally selective and shows minimal central nervous system penetration. |
|---|---|
| Mechanism of action | The H<sub>1</sub> histamine receptor is responsible for mediating hypersensitivity and allergic reactions. Exposure to an allergen results in degranulation of mast cells and basophils, which then release histamine and other inflammatory mediators. Histamine binds to, and activates, H<sub>1</sub> receptors, which results in the further release of pro-inflammatory cytokines, such as interleukins, from basophils and mast cells. These downstream effects of histamine binding are responsible for a wide variety of allergic symptoms, such as pruritus, rhinorrhea, and watery eyes. Fexofenadine is considered an “inverse agonist” of the H<sub>1</sub> receptor because it binds to and stabilizes the inactive form of the receptor, preventing its activation and subsequent downstream effects.It has a potent and selective affinity for H<sub>1</sub> receptors, and there is no evidence that it carries antidopaminergic, antiserotonergic, anticholinergic, sedative, or adrenergic blocking activity.Fexofenadine does not cross the blood-brain barrier and thus is unlikely to cause significant CNS effects. |
| Pharmacodynamics | Fexofenadine relieves allergy symptoms by antagonizing the actions of histamine, an endogenous compound predominantly responsible for allergic symptomatology.The relatively long duration of action of fexofenadine (approximately 24 hours)allows for once or twice daily dosing, and its rapid absorption allows for an onset of action within 1-3 hours. Fexofenadine should not be taken with fruit juice, as this may impair its absorption. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Histamine H1 receptor | Humans | antagonist |
ADME / PK
| Absorption | Fexofenadine is rapidly absorbed following oral administration and its absolute bioavailability is approximately 33%.The T<sub>max</sub> following oral administration is approximately 1-3 hours.The steady-state AUC<sub>ss(0-12h)</sub> and C<sub>max</sub> following twice daily dosing of 60mg are 1367 ng/mL.h and 299 ng/mL, respectively. Fexofenadine AUC is decreased by >20% when coadministered with fruit juices (e.g. apple, orange, grapefruit) due to their inhibition of OATP transporters - for this reason, prescribing information recommends administering fexofenadine only with water.Similarly, coadministration of fexofenadine with a high-fat meal appears to decrease AUC and C<sub>max</sub> by >20%. |
|---|---|
| Half-life | The terminal elimination half-life is approximately 11-15 hours. |
| Protein binding | Fexofenadine is 60-70% bound to plasma proteins,primarily to albumin and α<sub>1</sub>-acid glycoprotein. The extent of protein binding is decreased to 56-68% and 56-75% in patients with renal and hepatic impairment, respectively. |
| Metabolism | Fexofenadine is very minimally metabolized, with only 5% of an ingested dose undergoing hepatic metabolism.The only identified metabolites are a methyl ester of fexofenadine (3.6% of the total dose) and MDL 4829 (1.5% of the total dose).The enzymes responsible for this metabolism have not been elucidated. |
| Route of elimination | Approximately 80% of an ingested dose is eliminated in the feces, likely largely unchanged due to fexofenadine's limited metabolism, and 11% is eliminated in the urine.The principal pathways of fexofenadine elimination are biliary and renal. |
| Volume of distribution | The volume of distribution is approximately 5.4-5.8 L/kg. |
| Clearance | The oral clearance of fexofenadine is approximately 50.6 L/h and the renal clearance is approximately 4.32 L/h. |
Formulation & handling
- Low aqueous solubility and moderate lipophilicity support use in solid oral dosage forms, with attention to dissolution enhancement for consistent exposure.
- As an orally administered small molecule, it is suitable for tablets, capsules, and suspensions without parenteral handling constraints.
- Formulations should avoid co‑administration with fruit juices due to reduced bioavailability, though general food effects are minimal.
Regulatory status
| Lifecycle | Most patent protections in the United States and Canada expired between 2010 and 2018, indicating the API is in a late‑lifecycle stage. With products marketed in both countries, the market is mature and characterized by full generic availability. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Fexofenadine was originally developed by an originator company within the Sanofi‑Aventis group, with a wide range of generic manufacturers now active in production and numerous repackagers participating in U.S. and Canadian distribution. Branded and non‑branded products are established across these markets, indicating mature commercial availability. All listed U.S. and Canadian patents have expired, supporting the presence of broad generic competition. |
|---|
Safety
| Toxicity | No deaths were observed following the oral administration of up to 5000 mg/kg in both mice and rats (equivalent to approximately 100-200x the recommended human dose). Single doses of up to 800 mg and chronic exposure of up to 690 mg twice daily for 1 month in humans did not result in clinically significant adverse events. Symptoms of overdosage are consistent with fexofenadine's adverse effect profile and are likely to include dizziness, drowsiness, and dry mouth. If overdosage occurs, employ symptomatic and supportive treatment. Hemodialysis does not effectively remove fexofenadine from the blood and is therefore of no benefit. |
|---|
- Exhibits low acute oral toxicity in rodents, with no lethality observed at doses up to 5000 mg/kg
- Human single‑ and short‑term repeated‑dose exposures up to 800 mg and 690 mg BID, respectively, showed no clinically significant adverse findings
- Overexposure may manifest as CNS and anticholinergic‑like effects such as dizziness, drowsiness, and dry mouth, consistent with the compound’s known adverse‑effect profile
Fexofenadine 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.
Fexofenadine (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.
Fexofenadine API manufacturers & distributors
Compare qualified Fexofenadine API suppliers worldwide. We currently have 22 companies offering Fexofenadine 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 |
|---|---|---|---|---|---|
| Amino Chemicals | Producer | Malta | Malta | CoA, JDMF | 20 products |
| AXXO GmbH | Distributor | Germany | World | CEP, CoA, GMP, GDP, JDMF, KDMF, MSDS, USDMF | 243 products |
| Cipla | Producer | India | Unknown | CEP, CoA, FDA, GMP, USDMF, WC | 164 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, JDMF, KDMF, MSDS, USDMF, WC | 170 products |
| Excel Industries | Producer | India | India | CoA | 2 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Hari Ganesh Pharma Privat... | Distributor | India | India | CoA, FDA, GMP | 35 products |
| Hetero Drugs | Producer | India | Unknown | CEP, CoA, FDA, GMP, USDMF, WC | 98 products |
| Ind-Swift Labs. | Producer | India | India | CEP, CoA, FDA, GMP, JDMF, USDMF, WC | 27 products |
| Kolon Life Science | Producer | South Korea | South Korea | CoA | 32 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Morepen Laboratories Ltd. | Producer | India | India | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, ISO9001, JDMF, MSDS, USDMF, WC | 22 products |
| Mylan | Producer | India | India | CoA, FDA, GMP, USDMF, WC | 201 products |
| Osaka Synthetic Chemical ... | Producer | Japan | Japan | CoA, JDMF | 16 products |
| Pharm Rx Chemical Corp | Distributor | United States | India | BSE/TSE, CoA, GMP, MSDS, USDMF | 166 products |
| Pharmacostech | Producer | South Korea | South Korea | CoA, JDMF | 3 products |
| PLIVA | Producer | Czech Republic | Czech Republic | CoA, GMP, JDMF | 31 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Sun Pharma | Producer | India | India | CEP, CoA, GMP, WC | 219 products |
| THINQ Pharma | Producer | India | India | CoA, FDA, USDMF | 6 products |
| Valence Labs | Producer | India | India | CoA, GMP | 32 products |
| Vasudha Pharma Chem Ltd. | Producer | India | India | CEP, CoA, FDA, GMP, KDMF, MSDS, USDMF, WC | 37 products |
When sending a request, specify which Fexofenadine 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 Fexofenadine 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.
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