title: Pharmacodynamic and pharmacokinetic assessment of fluticasone furoate + vilanterol for the treatment of asthma.
abstract: The pharmacokinetic (PK) and pharmacodynamic (PD) effects of long-acting β2-agonists and mostly inhaled corticosteroids (ICSs) shape the efficacy and safety of these agents in the treatment of asthma. In fact, the PK and PD characteristics of the drug largely determine the degree of pulmonary targeting Areas covered. In this review, we summarize the PK and PD properties of inhaled fluticasone furoate (FF) and vilanterol trifenatate (VI) and their fixed-dose combination (FDC) for the treatment of asthma Expert opinion. It is difficult to interpret the data that we have described because the preclinical and clinical development of FF/VI FDC was not really based on solid information on quantitative PK/PD approach. Unfortunately, for both FF and VI we only know concentrations in systemic blood, a compartment that is downstream of both target and non-target respiratory tissue. This lack of information does not allow us to understand the temporal relationship between the delivered dose and the drug concentration at the sites of action within the lungs. In addition, all studies performed with FF and VI did not address the fundamental issue that asthma can significantly alter lung deposition, absorption and also clearance of inhaled medicines.
authors.affiliation: a Department of Systems Medicine, Unit of Respiratory Clinical Pharmacology , University of Rome Tor Vergata , Roma , Italy.
authors.forename: Luigino
authors.initials: L
authors.lastname: Calzetta
authors.affiliation: b Department of Experimental Medicine, Section of Pharmacology 'L. Donatelli', Centre of Excellence for Cardiovascular Diseases , Second University of Naples , Naples , Italy.
authors.forename: Barbara
authors.initials: B
authors.lastname: Rinaldi
authors.affiliation: a Department of Systems Medicine, Unit of Respiratory Clinical Pharmacology , University of Rome Tor Vergata , Roma , Italy.
authors.forename: Mario
authors.initials: M
authors.lastname: Cazzola
authors.affiliation: b Department of Experimental Medicine, Section of Pharmacology 'L. Donatelli', Centre of Excellence for Cardiovascular Diseases , Second University of Naples , Naples , Italy.
authors.forename: Maria Gabriella
authors.initials: MG
authors.lastname: Matera
mesh_terms: D000280:Administration, Inhalation; D000730:Androstadienes / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D018927:Anti-Asthmatic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D001249:Asthma / Q000188:drug therapy* / Q000503:physiopathology; D001592:Benzyl Alcohols / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D002722:Chlorobenzenes / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D004338:Drug Combinations; D016503:Drug Delivery Systems; D005938:Glucocorticoids / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D008168:Lung / Q000378:metabolism; D014018:Tissue Distribution
chemical_list: D000730:Androstadienes; D018927:Anti-Asthmatic Agents; D001592:Benzyl Alcohols; D002722:Chlorobenzenes; D004338:Drug Combinations; D005938:Glucocorticoids; C000611924:fluticasone furoate-vilanterol trifenatate
keywords: Asthma; fluticasone furoate; pharmacodynamics; pharmacokinetics; vilanterol trifenatate