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Pharmacokinetics of Single and Repeat Doses of Fluticasone Furoate/Umeclidinium/Vilanterol in Healthy Chinese Adults
Author(s) -
Li Yan,
Li Huafang,
Sheng Yucheng,
Du Xin,
Yao Yuhui,
Luo Xian,
Ma Peiming
Publication year - 2018
Publication title -
clinical pharmacology in drug development
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.711
H-Index - 22
eISSN - 2160-7648
pISSN - 2160-763X
DOI - 10.1002/cpdd.626
Subject(s) - fluticasone propionate , medicine , pharmacokinetics , dry powder inhaler , cmax , pharmacology , dosing , area under the curve , zoology , inhaler , corticosteroid , asthma , biology
Abstract The pharmacokinetics (PK) and safety of single‐inhaler fluticasone furoate/umeclidinium/vilanterol (FF/UMEC/VI) after single and repeat dosing in healthy Chinese adults were assessed. In this open‐label study (NCT02837380), subjects received once‐daily FF/UMEC/VI 100/62.5/25 µg on day 1 and repeat doses on days 2–7. PK parameters (days 1 and 7) included maximum observed concentration (C max ) and area under the plasma concentration‐time curve (AUC) from time zero (predose) to last time of quantifiable concentration (AUC 0–t ). Terminal phase half‐life (t ½ ) on day 1 was estimated. The primary objective was to assess systemic exposure of FF 100 µg, UMEC 62.5 µg, and VI 25 µg following single‐inhaler triple therapy on days 1 and 7. On day 1, geometric mean t ½ of UMEC and VI was 0.36 and 0.52 hours, respectively; t ½ of FF was not representative because of nonquantifiable concentration data. On days 1 and 7, geometric mean C max of FF was 10.46 and 27.32 pg/mL, respectively; C max of UMEC was 144.14 and 241.35 pg/mL, respectively; and C max of VI was 120.42 and 196.78 pg/mL, respectively. AUC 0–t of FF was 1.77 and 276.96 pg·h/mL, respectively; AUC 0–t of UMEC was 28.44 and 117.19 pg·h/mL, respectively; and AUC 0–t of VI, 42.46 and 101.12 pg·h/mL, respectively. The PK of FF/UMEC/VI was as expected for the individual‐component PK previously reported in healthy Chinese adults. No new safety signals were observed.