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. 2019 Oct;47(10):1122–1135. doi: 10.1124/dmd.119.086744

TABLE 3.

Properties of representative inhaled, lung targeted compounds

Lung retention mechanism(s) for each compound are denoted by checkmarks.

Compound Target cLogP cpKa Lung Retention Mechanism(s)
Dissolution-Limited Tissue Affinity Low Permeability Slow Off-Rate
Basic Lipophilic
Fluticasone propionatea Glucocorticoid receptor 3.3 <3
Fluticasone furoateb Glucocorticoid receptor 3.7 <3
Salmeterol Xinafoatec β2-adrenergic receptor 4.1 9.4 d
Salbutamole β2-adrenergic receptor 0.6 9.4
Tiotropium bromidef Muscarinic receptors (M3, M1) −2.3 <3
Compound 3.05g Epithelial sodium channel −2.0 8.5
GSK2269557/Nemiralisibh PI3Kδ 4.8 8.7, 4.1
d

Apparent slow off-rate likely due to partitioning into lipid membrane bilayers.

e

Anderson et al. (1994), Dickson et al. (2016), and references therein.

g

Kley et al. (2016).