Hemay005 is a novel phosphodiesterase type 4(PDE4) inhibitor being developed for the treatment of psoriasis. This study is the first administration of Hemay005 in humans to establish the initial safety, tolerability, and pharmacokinetic profile following single doses of Hemay005. A total of approximately 44 subjects will be randomized into 6 cohorts(10mg, 20mg, 40mg, 80mg, 120mg, 180mg), approximately 8 healthy subjects will be enrolled (6 active and 2 placebo) at each dose cohort by sentinel method(1 active and 1 placebo,5 active and 1 placebo), with the exception of 10mg (4 active) cohort. This study includes an 28-day Screening Period, a 1-day Treatment Period, and an End of Study Visit occurring approximately 11days (±3 days) after study drug administration.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
DOUBLE
Enrollment
68
Subjects will be randomized into 6 cohorts(10mg, 20mg, 40mg, 80mg, 120mg, 180mg) orally single dose
Subjects will be randomized into 5 cohorts(20mg, 40mg, 80mg, 120mg, 180mg) orally single dose
Peking Union Medical College Hospital
Beijin, China
Number of adverse events and serious adverse events
Time frame: Day 1 up to Day 11±3
Cmax
Maximum observed plasma concentration
Time frame: pre-dose, 0.5, 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48 hours post-dose
Tmax
Time of maximum concentration
Time frame: pre-dose, 0.5, 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48 hours post-dose
AUCt
Area under the plasma concentration-time curve from time zero extrapolated to infinity
Time frame: pre-dose, 0.5, 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48 hours post-dose
AUC∞
Area under the plasma concentration-time curve from time zero to the last quantifiable concentration
Time frame: pre-dose, 0.5, 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48 hours post-dose
t1/2
Terminal elimination half-life
Time frame: pre-dose, 0.5, 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48 hours post-dose
CL/F
Apparent total plasma clearance
Time frame: pre-dose, 0.5, 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48 hours post-dose
Vz/F
Apparent total volume of distribution
Time frame: pre-dose, 0.5, 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48 hours post-dose
Cumulative urinary excretion
Time frame: pre-dose, 0-4 hours,4-8 hours,8-12 hours,12-24 hours,24-36 hours,36-48 hours post-dose
Accumulative urine excretion rate
Time frame: pre-dose, 0-4 hours,4-8 hours,8-12 hours,12-24 hours,24-36 hours,36-48 hours post-dose
Renal clearance
Time frame: pre-dose, 0-4 hours,4-8 hours,8-12 hours,12-24 hours,24-36 hours,36-48 hours post-dose
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