Tafluprost API Manufacturers & Suppliers
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Tafluprost | CAS No: 209860-87-7 | GMP-certified suppliers
A medication that reduces elevated intraocular pressure to manage open-angle glaucoma and ocular hypertension, supporting prevention of optic nerve damage in ophthalmic treatments.
Therapeutic categories
Primary indications
- Tafluprost is indicated for reducing elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension
Product Snapshot
- Tafluprost is formulated as an ophthalmic solution or suspension intended for topical ocular administration
- It is primarily indicated for the reduction of elevated intraocular pressure associated with open-angle glaucoma and ocular hypertension
- Tafluprost holds regulatory approval in key markets including the United States and Canada
Clinical Overview
Chemically, tafluprost is a fluorinated derivative of prostaglandin F2-alpha, belonging to the class of prostaglandins. These compounds are unsaturated carboxylic acids based on a 20-carbon arachidonic acid skeleton containing a five-membered ring. Tafluprost specifically acts as a selective agonist of the prostanoid FP receptor (the fluoroprostaglandin receptor), demonstrating a pharmacological affinity approximately twelve times greater than that of latanoprost’s active form, with minimal binding to other receptor types.
The primary mechanism of action involves conversion of tafluprost to its active free acid form in the eye, which then binds to FP receptors on the ciliary muscle. This interaction stimulates remodeling of the extracellular matrix, leading to increased uveoscleral outflow of aqueous humor. Enhanced outflow reduces IOP, thereby mitigating the risk of optic nerve damage associated with glaucoma progression.
Pharmacokinetic data indicate that tafluprost is rapidly hydrolyzed in ocular tissues, with limited systemic absorption. Metabolism primarily occurs in the eye, and the compound displays a short systemic half-life. These characteristics support its topical ophthalmic use with a focused local effect.
Safety considerations reflect typical prostaglandin analog adverse events, including conjunctival hyperemia, eyelash growth, and potential ocular irritation. Tafluprost has a tolerability profile consistent with its class, and careful monitoring is advised during treatment.
Tafluprost was approved for clinical use in the United States in 2012 and is marketed under several brand names globally. From a sourcing perspective, procurement of tafluprost API requires strict adherence to regulatory standards for purity, stereochemistry, and stability. Quality control should ensure the integrity of the ester prodrug, absence of fluorinated impurities, and compliance with ophthalmic-grade specifications. Reliable supply chains with validated manufacturing processes are essential for consistent pharmaceutical formulation.
Identification & chemistry
| Generic name | Tafluprost |
|---|---|
| Molecule type | Small molecule |
| CAS | 209860-87-7 |
| UNII | 1O6WQ6T7G3 |
| DrugBank ID | DB08819 |
Pharmacology
| Summary | Tafluprost acid is a selective agonist of the prostaglandin F2-alpha (FP) receptor, primarily increasing uveoscleral outflow to lower intraocular pressure. It exhibits high receptor affinity with minimal off-target activity. Tafluprost is utilized for reducing elevated intraocular pressure in open-angle glaucoma and ocular hypertension. |
|---|---|
| Mechanism of action | Tafluprost acid is a prostanoid selective FP receptor agonist that is believed to reduce the intraocular pressure (IOP) by increasing the outflow of aqueous humor. Studies in animals and humans suggest that the main mechanism of action is increased uveoscleral outflow. |
| Pharmacodynamics | Tafluprost is a novel prostaglandin analog with a high affinity for the fluoroprostaglandin (FP) receptor PGF2α. Tafluprost has an affinity for the FP receptor that is approximately 12 times higher than that of the carboxylic acid of latanoprost, but with almost no potential to bind to other receptors. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Prostaglandin F2-alpha receptor | Humans | agonist |
ADME / PK
| Absorption | Following instillation, tafluprost is absorbed through the cornea and is hydrolyzed to the biologically active acid metabolite, tafluprost acid. Tafluprost is an ester which makes the drug lipophillic enough to be quickly absorbed through. When administered to the eye, the peak plasma concentration (Cmax) and time to peak plasma concentration (Tmax) of tafluprost acid in healthy subjects was 26 pg/mL and 10 minutes respectively. a AUC, tafluprost acid = 394 pg*min/mL - 432 pg*min/mL. |
|---|---|
| Metabolism | Tafluprost is an ester prodrug which is rapidly hydrolyzed by corneal esterases to form its biologically active acid metabolite. Tafluprost acid is further metabolized via fatty acid β-oxidation and phase II conjugation into 1,2,3,4-tetranor acid. |
| Route of elimination | Mean plasma tafluprost acid concentrations were below the limit of quantification of the bioanalytical assay (10 pg/mL) at 30 minutes following topical ocular administration of tafluprost 0.0015% ophthalmic solution. In male rats, it was observed that tafluprost was excreted into the feces. |
| Volume of distribution | The highest concentration of tafluprost acid was found in the cornea and conjunctiva. |
Formulation & handling
- Tafluprost is a lipophilic small molecule prostaglandin analogue formulated as an ophthalmic solution for topical eye administration.
- Due to low aqueous solubility and sensitivity to light, formulations require appropriate solubilizers and light-protective packaging to maintain stability.
- Stable handling includes avoiding exposure to extreme temperatures and ensuring sterile conditions for ophthalmic use.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is marketed in the US and Canada, with its earliest patent expired in 2017 and additional patents protecting the product in the US until 2029, indicating partial market maturity with ongoing patent coverage. |
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| Markets | Canada, US |
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Supply Chain
| Supply chain summary | Tafluprost is produced by a limited number of originator companies, primarily supplying branded products in the US and Canadian markets. The presence of multiple brand formulations indicates established market penetration in North America. Existing patents valid until 2029 suggest that generic competition is currently limited but may increase following patent expirations. |
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Safety
| Toxicity | Most common ocular adverse reaction is conjunctival hyperemia (range 4% – 20%). |
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- Exposure may cause conjunctival hyperemia
- Observed incidence ranges from 4% to 20%
- Handle with appropriate protective equipment to avoid ocular contact
Tafluprost is a type of Prostaglandin Analogues
Prostaglandin analogues are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in the field of medicine. These synthetic compounds mimic the effects of natural prostaglandins, which are hormone-like substances found in the body.
Prostaglandin analogues have gained significant attention in medical research due to their diverse therapeutic applications. They exhibit a wide range of physiological activities, such as regulating inflammation, blood flow, and hormone levels. These compounds are commonly used in the treatment of various conditions, including glaucoma, ocular hypertension, and certain types of cancer.
One notable application of prostaglandin analogues is in ophthalmology. These compounds effectively reduce intraocular pressure by increasing the outflow of aqueous humor, providing an effective treatment for glaucoma patients. Moreover, prostaglandin analogues offer the advantage of once-daily dosing, enhancing patient compliance and convenience.
In the field of oncology, prostaglandin analogues have shown promise as anticancer agents. They exert anti-proliferative effects on cancer cells and can induce apoptosis, making them valuable in the treatment of certain malignancies.
Overall, prostaglandin analogues represent a significant class of pharmaceutical APIs with diverse therapeutic applications. Continued research and development in this area hold great potential for the advancement of medicine and the improvement of patient care.
Tafluprost (Prostaglandin Analogues), classified under Anti-inflammatory Agents
Anti-inflammatory agents are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used to treat various inflammatory conditions. These agents play a vital role in alleviating pain, reducing swelling, and controlling inflammation in the body. They are widely employed in the management of diverse medical conditions, including arthritis, autoimmune disorders, asthma, and skin conditions like dermatitis.
Anti-inflammatory APIs primarily function by inhibiting the production of specific enzymes called cyclooxygenases (COX) and lipoxygenases (LOX). These enzymes are responsible for the synthesis of pro-inflammatory molecules known as prostaglandins and leukotrienes, respectively. By suppressing the activity of COX and LOX, anti-inflammatory agents effectively curtail the production of these inflammatory mediators, thereby mitigating inflammation.
Common examples of anti-inflammatory APIs include non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen, aspirin, and naproxen. These agents exhibit analgesic, antipyretic, and anti-inflammatory properties. Another group of anti-inflammatory APIs includes corticosteroids, such as prednisone and dexamethasone, which are synthetic hormones that modulate the body's immune response to control inflammation.
In conclusion, anti-inflammatory agents are a vital category of pharmaceutical APIs widely used to manage inflammation-related disorders. They target enzymes involved in the synthesis of pro-inflammatory molecules, effectively reducing pain and swelling. NSAIDs and corticosteroids are commonly prescribed anti-inflammatory APIs due to their efficacy in controlling inflammation.
Tafluprost API manufacturers & distributors
Compare qualified Tafluprost API suppliers worldwide. We currently have 4 companies offering Tafluprost API, with manufacturing taking place in 4 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 |
|---|---|---|---|---|---|
| AXXO GmbH | Distributor | Germany | European Union | CoA, EDMF/ASMF, GMP, GDP, MSDS, USDMF | 243 products |
| Chirogate International | Producer | Taiwan | Taiwan | CoA, EDMF/ASMF, FDA, GMP, JDMF, KDMF, USDMF | 17 products |
| MSN Labs. | Producer | India | India | CoA, GMP, USDMF, WC | 119 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, GMP, ISO9001, MSDS, USDMF | 757 products |
When sending a request, specify which Tafluprost 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.).
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