Fluticasone propionate (FP) and fluticasone furoate (FF) are both synthetic glucocorticoid drugs used in the prevention of asthma exacerbations and for the treatment of allergy symptoms and rhinitis. Based on the assigned glucocorticoid nomenclature, both drugs consist of a common steroidal backbone (fluticasone) and the ester substituent (furoate/propionate). This naming convention wrongly suggests that these derivatives could be ester prodrugs of fluticasone. However, fluticasone 17α esters are remarkably stable and remain attached to the fluticasone backbone even during metabolism. Their pharmacological activity is mediated by the entire molecule (backbone + ester) and they share no common metabolites – neither FF nor FP is metabolised to fluticasone. FF and FP are therefore structurally different compounds with distinct properties.
The furoate and propionate moieties help to significantly increase the glucocorticoid activity of fluticasone and neither of the two is metabolised to Fluticasone (note that fluticasone base does not currently exist as a separate drug moiety). The ester group also contributes to the physicochemical characteristics of the molecule which impact solubility, dissolution rate, tissue affinity, and hence pharmacokinetic and pharmacodynamic properties. The ester derived from 2-furoic acid in FF has been shown to confer higher affinity for both nasal and lung tissue compared with FP and this translates to enhanced lung residency and once-daily efficacy for inhaled FF in asthma. The furoate has a quicker onset of action (8-24 hours) compared to the propionate (3-4 days)
Take away
FF and FP are distinct glucocorticoids and the practice of abbreviating them to fluticasone should be discouraged.
Key differences between FP & FF
- FP nasal spray FDA approved for ages 4 and up; FF nasal spray approved for ages 2 and up
- FP inhaled FDA approved for ages 4 and up; FF inhaled approved for ages 5 and up
- FF has a higher affinity for both nasal and lung tissue compared with FP; this translates to enhanced lung residency and once-daily efficacy in asthma as shown by studies with inhaled FF
- Once-daily dosing of inhaled FF vs. twice-daily FP
Available FF & FP single-entity preparations
Fluticasone furoate (Nasal spray)
- For seasonal and perennial allergic rhinitis in patients 2 years of age and older
- Once-daily dosing
- Avamys® (GSK)
Fluticasone furoate (Oral inhalation)
- For maintenance treatment of asthma in patients aged 5 years and older
- Once-daily dosing
- Arnuity Ellipta® (GSK)
Fluticasone propionate (Nasal spray)
- For seasonal and perennial allergic rhinitis in patients 4 years of age and older
- Once-daily dosing
- Flixonase® (GSK); Flusort® (Glenmark)
Fluticasone propionate (Oral inhalation)
- For maintenance treatment of asthma in patients aged 4 years and older
- Twice-daily dosing
- Flovent® (GSK)
Fluticasone propionate (Topical)
- For treatment of corticosteroid-responsive dermatoses
- Once or twice daily dosing
- Cutivate® (GSK)
Source: Wiley’s The Clinical Respiratory Journal. Available from: www.ncbi.nlm.nih.gov