Vilanterol trifenatate is a white powder with a molecular weight of 774.8, and the empirical formula is C24H33Cl2NO5.C20H16O2. It insoluble in water and slightly soluble in methanol, ethanol, acetonitrile and propan-2-ol. It is slightly hygroscopic. It is provided in a micronized form.
Vilanterol Trifenatate is a long-acting β2 adrenergic receptor Agonist with alonger than 24-hour activity in humans, and is being developed to be used in combination with FF. It is also highly selective for the β2-receptor, with over 1000-fold greater selectivity compared to β1-receptors. It demonstrates prolonged bronchodilation in subjects with asthma and COPD.
Vilanterol trifenatate is synthesized by incorporation of an oxygen atom at the homobenzylic position of the right-hand side phenyl ring of (R)-salmeterol and has suitable chemical properties for inhaled administration. The combination in fluticasone furoate (FF) and vilanterol trifenatate (VI) in a single inhaler is the first once daily combination available on the market for the treatment of stable COPD.
ChEBI: Vilanterol Trifenatate is a triphenylacetate salt obtained by combining vilanterol with one equivalent of triphenylacetic acid. Used in combination with fluticasone furoate for treatment of bronchospasm associated with chronic obstructive pulmonary disease. It has a role as a beta-adrenergic agonist and a bronchodilator agent. It contains a vilanterol(1+).
vilanterol trifenatate is a novel and selective agonist of β2-ar with a pec50 value of 10.37±0.05 [1].vilanterol trifenatate is a novel long-acting β2-ar agonist (laba) with 24h activity in development for inhaled once daily treatment. in the radioligand binding studies, vilanterol trifenatate has shown the binding affinity in the one-affinity site model with pkd values of 9.44±0.07 and 10.82±0.12 in the presence gpp(nh)p and absence gpp(nh)p, respectively. in dissociation studies, vilanterol trifenatate has been reported to bind from the β2-ar with a dissociation t1/2 value of 3.5 min in the presence of gpp(nh)p. vilanterol trifenatate has been found to have a good selectivity for β2-ar over the other β-ar receptor subtypes(β1and β3) with pec50 values of 10.37±0.05, 6.98±0.03 and 7.36±0.03, respectively. vilanterol trifenatate has exhibited at least 1000-fold selectivity over both β1-and β3-ar subtypes [1].
The recommended and maximum dose is one inhalation of vilanterol trifenatate 25 micrograms once daily either morning or evening but at the same time every day.
Vilanterol Trifenatate is a selective long-acting beta2-receptor agonist (also referred to as a LABA). The pharmacologic effects of beta2-adrenoceptor agonist drugs, including vilanterol trifenatate, are at least in part attributable to stimulation of intracellular adenylate cyclase, the enzyme that catalyses the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells.
[1] slack rj1, barrett vj, morrison vs, sturton rg, emmons aj, ford aj, knowles rg.in vitro pharmacological characterization of vilanterol, a novel long-acting β2-adrenoceptor agonist with 24-hour duration of action.j pharmacol exp ther. 2013 jan; 344(1):218-30.
