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Open AccessJournal ArticleDOI

Fluticasone furoate, a novel inhaled corticosteroid, demonstrates prolonged lung absorption kinetics in man compared with inhaled fluticasone propionate.

Ann Allen, +2 more
- 01 Jan 2013 - 
- Vol. 52, Iss: 1, pp 37-42
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TLDR
In comparison with inhaled FP, inhaled FF (independent of formulation) demonstrated prolonged absorption from the lung into the systemic circulation, indicating a longer lung retention time and suggesting the potential for maintained efficacy with once-daily administration.
Abstract
Background Fluticasone furoate (FF; GW685698) is a novel inhaled corticosteroid that is active at 24 h and under development for once-daily administration in combination with the long-acting β2-adrenoceptor agonist vilanterol (GW642444) for chronic obstructive pulmonary disease and asthma. In vitro studies examining the respiratory tissue-binding properties of corticosteroids showed FF to have the largest cellular accumulation and slowest rate of efflux compared with other clinically used inhaled corticosteroids, consistent with greater tissue retention. The enhanced affinity of the glucocorticoid receptor binding of FF, coupled with its extended tissue association, may be expected to lead to greater and more prolonged anti-inflammatory effects and should provide relevant once-daily efficacy.

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Citations
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Journal ArticleDOI

Inhaled Corticosteroids in Lung Diseases

TL;DR: Although several new drugs are being developed and evaluated, it is unlikely that any of these new medications will replace ICSs as the preferred initial long-term controller therapy for asthma, but more effective initial controller therapy could be developed for COPD.
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Scientific rationale for the possible inhaled corticosteroid intraclass difference in the risk of pneumonia in COPD.

TL;DR: It is suggested that the higher pneumonia risk with fluticasone propionate treatment is caused by greater and more protracted immunosuppressive effects locally in the airways/lungs.
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Current approaches to the discovery of novel inhaled medicines.

TL;DR: Opportunities for novel inhaled drugs, and the key challenges and uncertainties hampering progress are addressed.
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In Vitro Testing for Orally Inhaled Products: Developments in Science-Based Regulatory Approaches

TL;DR: An integrated perspective of case studies and discussion related to in vitro testing of orally inhaled products, including in vitro-in vivo correlations and requirements for in vitro data and statistical analysis that support quality or bioequivalence for regulatory applications are provided.
Journal ArticleDOI

The effect of fluticasone furoate/umeclidinium in adult patients with asthma: a randomized, dose-ranging study.

TL;DR: FF/UMEC may be a viable treatment for patients with asthma symptomatic on ICS; benefit may be most prominent in those with fixed obstruction, and the carryover effect suggests future UMEC studies should use an alternative design.
References
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Journal ArticleDOI

New Method for Calculating the Intrinsic Absorption Rate of Drugs

TL;DR: It is shown that methods based on the single-compartment concept do not result in acceptable estimates of the absorption rates, and a new equation is presented, presuming the drug distributes between a central and one peripheral compartment, which results in an accurate estimate of the known rates of infusion (absorption) for the drugs studied to date.
Journal ArticleDOI

Inhaled corticosteroids: past lessons and future issues

TL;DR: This journal supplement will review what has been learned about the safety of inhaled cortico-steroids during the past decade, discussing some of the questions that remain and considering the characteristics of an "ideal" inhale corticosteroid: one with high local activity in the lung and minimal or no adverse systemic effects.
Journal ArticleDOI

Pharmacological properties of the enhanced-affinity glucocorticoid fluticasone furoate in vitro and in an in vivo model of respiratory inflammatory disease.

TL;DR: The potent and selective pharmacological profile of FF described here could deliver an effective, safe, and sustained topical treatment of respiratory inflammatory diseases such as allergic rhinitis and asthma.
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