Table 1.

INCS Physicochemical, Pharmacokinetic and Pharmacological Characteristics

INCSa	RRAb	Log Pc	Therapeutic Dosed, µg/day	Dose Volume, µL/day	Bioavailabilitye, %	CL, L/h	Plasma AUCf for 20% Cortisol Suppression, pg/mL*h	Dose for 20% Cortisol Suppression, µg/day	TIg
FF	298912	4.1712	11062,63	20063	0.5062	6512	848	11,095	101
FP	177512	3.8912	20064	400 [mg]64	0.5134	6912	1332	18,020	90
MF	210012	4.7312	20065	400 [mg]65	0.4632,38	5412	1126	13,215	66
CICh	120012	3.0012	20066	28066	7.473,i	22812	2158	6650	33
TAA	23312	1.8512	22067	120	4638	3712	8935	713	3.2
FLU	19012	1.3612	464/40068	800 [mg]68	5068	5812	10,953	1271	2.7
BUD	93512	2.3212	25669	20070	3138	8412	2206	562	2.2
BDPh	134512	3.2712	33671	800 [mg]71	4435,38	12012	2179	594	1.8
DEX	10072	1.68	400		75	17	6750	154	0.4

Notes: ^aAll in ANS formulation except CIC, which uses a MDI; ^bRelative to DEX where DEX affinity = 100; ^cValues (lipophilicity) are defined as the log10 of the octanol/water partition coefficient; ^dTherapeutic doses for AR for adults and children (≥12) unless further specified (for BDP >12; FLU ≥14); ^eF, absolute bioavailability via nasal route (nose and gut absorption) determined in healthy subjects; ^fPlasma AUC (F dose/CL) is the estimated daily dose that would result in 20% cortisol suppression;¹² gDose for 20% cortisol suppression/therapeutic dose; ^hValues are for the active metabolites BMP and des-CIC; ⁱValue calculated based on Weiswasser et al J Allergy Clin Immunol. 2008,⁷³ using the clearance and relative to value for oral inhalation.

Abbreviations: ANS, aqueous nasal spray; AR, allergic rhinitis; AUC, area under the curve; BDP, beclomethasone dipropionate; BMP, beclomethasone 17-monopropionate; BUD, budesonide; CIC, ciclesonide; CL, plasma clearance; Des-CIC, desisobutyryl ciclesonide; DEX, dexamethasone; FF, fluticasone furoate; FLU, flunisolide; FP, fluticasone propionate; INCS, intranasal corticosteroid; MDI, metered-dose inhaler; MF, mometasone furoate; RRA, relative receptor affinity; TAA, triamcinolone acetonide; TI, therapeutic index.