Vilanterol Trifenatate is a long-acting selective β2-adrenergic receptor agonist used as an active pharmaceutical ingredient in inhalation formulations for the management of respiratory conditions including chronic obstructive pulmonary disease (COPD) and asthma. It is the trifenatate salt of vilanterol and is primarily developed for use in dry-powder inhalation pharmaceutical products.
Vilanterol belongs to the long-acting beta-2 adrenergic agonist (LABA) class of bronchodilators. It provides prolonged bronchodilation following inhalation and is particularly suitable for once-daily respiratory formulations. It has been used in combination products containing inhaled corticosteroids and other long-acting bronchodilators.
Vilanterol Trifenatate has the CAS Number 503070-58-4, molecular formula C44H49Cl2NO7, and molecular weight of approximately 774.78 g/mol. The substance consists of vilanterol associated with one equivalent of triphenylacetic acid. Regulatory documentation identifies the active pharmaceutical ingredient as a white powder with practical insolubility in water.
Vilanterol Trifenatate contains one stereogenic center and the pharmaceutical active substance is controlled for its required stereochemical form. Enantiomeric purity is an important quality attribute because vilanterol has defined stereochemistry. Regulatory assessment documentation describes the drug substance as the R-isomer and indicates routine control of enantiomeric purity by chiral HPLC.
The substance is generally described as a white to off-white powder. It is practically insoluble in water and demonstrates higher solubility in selected organic solvents. Regulatory information describes it as practically insoluble in water and heptane, very slightly soluble in toluene and tert-amyl methyl ether, slightly soluble in acetonitrile, ethanol and 2-propanol, soluble in methanol, and freely soluble in dichloromethane and dimethyl sulfoxide.
Public chemical data report a melting point of approximately 131.9–134.2°C.
Vilanterol Trifenatate is primarily used in inhalation pharmaceutical development and manufacturing. Its principal applications include:
Vilanterol has been incorporated into combination inhalation products with fluticasone furoate and umeclidinium, where it contributes long-acting bronchodilator activity. Current regulatory product information continues to list vilanterol trifenatate among the active substances in combination inhalation products.
Vilanterol is a selective long-acting β2-adrenergic receptor agonist. After inhalation, the active molecule interacts with β2-adrenergic receptors present on airway smooth muscle.
Activation of these receptors increases intracellular cyclic AMP signaling, which promotes relaxation of bronchial smooth muscle. The resulting bronchodilation improves airway caliber and facilitates airflow.
The long duration of pharmacological activity makes vilanterol suitable for once-daily inhaled treatment regimens. Its use in dry-powder inhalers also makes the physical characteristics of the API important during pharmaceutical formulation.
Vilanterol Trifenatate is particularly relevant to dry-powder inhalation systems. For inhalation APIs, particle size and particle-size distribution can influence aerosolization, dispersion and delivery of the active ingredient to the respiratory tract.
Regulatory documentation specifically identifies particle-size distribution as a controlled quality attribute for vilanterol trifenatate drug substance. Micronized material is used in inhalation products, and particle-size parameters such as X10, X50 and X90 may therefore be important for formulation and manufacturing control.
A publicly disclosed pharmaceutical specification for vilanterol trifenatate includes particle-size controls around the micron range, demonstrating the importance of particle engineering for inhalation applications.
For pharmaceutical manufacturing, Vilanterol Trifenatate is evaluated using analytical procedures designed to confirm identity, assay, impurity profile and physical quality.
Important quality attributes include:
The FDA chemistry review confirms that the vilanterol trifenatate drug substance is controlled for appearance, identification, assay, impurities, enantiomer, residual solvents, water content, residue on ignition and particle-size distribution.
Vilanterol Trifenatate API is intended for pharmaceutical companies involved in respiratory drug formulation, inhalation product development and commercial manufacturing.
Because the material is intended for inhalation applications, control of particle size, purity, stereochemical composition and physical properties is particularly important. Micronized Vilanterol Trifenatate can be incorporated into dry-powder inhalation systems together with suitable excipients such as lactose and magnesium stearate.
The API is also relevant to combination respiratory formulations containing corticosteroids or other bronchodilators.
Swapnroop Drugs & Pharmaceuticals provides Vilanterol Trifenatate API for pharmaceutical development, formulation and manufacturing requirements, subject to applicable quality and regulatory specifications.
Vilanterol Trifenatate should be stored in appropriately sealed pharmaceutical containers and protected from moisture. Publicly available chemical information describes the material as hygroscopic, while regulatory information identifies appropriate stability controls for the drug substance.
For commercial pharmaceutical use, actual storage conditions, retest period and packaging configuration should be established according to the approved drug-substance specification and stability data.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 2.0% |
| Residue on Ignition | NMT 0.1% |
| Heavy Metals | NMT 10 ppm |
| Individual Impurity | NMT 0.10% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 0.3% |
| Melting Point | 131.9–134.2°C |