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Single‐ and multiple‐dose pharmacokinetics of tofacitinib in healthy Chinese volunteers
Author(s) -
Krishnaswami Sriram,
Wang Tao,
Yuan Yi,
Alvey Christine W.,
Checchio Tina,
Peterson Mark,
Shi Haihong,
Riese Richard
Publication year - 2015
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.202
Subject(s) - tofacitinib , pharmacokinetics , medicine , pharmacology , rheumatoid arthritis
Tofacitinib is an oral Janus kinase inhibitor. The objective of this phase 1, open‐label study was to characterize the single‐ and multiple‐dose pharmacokinetics (PK) of tofacitinib in 12 healthy, adult Chinese volunteers. Eligible subjects received oral tofacitinib 10 mg once daily on days 1 and 6 and twice daily on days 2–5. Blood samples were collected on day 1 predose and over 24 hours postdose (day 2 predose), predose on days 3–6, and over 12 hours postdose on day 6. PK parameters were calculated using noncompartmental analysis. Mean concentration–time profiles for days 1 and 6 were similar, with median time to peak concentration of 0.5 hours on both days. Plasma concentrations declined rapidly following attainment of peak concentrations, with a mean terminal half‐life of 3.3 hours on day 1 (single dose) and 2.5 hours on day 6 (multiple dose). No accumulation in plasma occurred with twice‐daily administration: accumulation ratio of 1.04. The rapid absorption, elimination, and systemic exposures (peak and area under the concentration–time curve) observed in healthy Chinese volunteers in this study are similar to those previously reported in white subjects.