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.jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117 Br+J+Clin+Pharmacol
2014 ; 78
(3
): 498-508
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Tolerability, pharmacokinetics and pharmacodynamics of TA-8995, a selective
cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects
#MMPMID24628035
Ford J
; Lawson M
; Fowler D
; Maruyama N
; Mito S
; Tomiyasu K
; Kinoshita S
; Suzuki C
; Kawaguchi A
; Round P
; Boyce M
; Warrington S
; Weber W
; van Deventer S
; Kastelein JJ
Br J Clin Pharmacol
2014[Sep]; 78
(3
): 498-508
PMID24628035
show ga
AIMS: Two double-blind, randomized studies were conducted to assess the
tolerability, pharmacokinetics and pharmacodynamics of oral TA-8995, a new
cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects.
METHODS: Study 1: Subjects received single doses of TA-8995 or placebo (fasted).
Doses were 5, 10, 25, 50 (fed/fasted), 100 and 150?mg (Caucasian males,
18-55?years), 25?mg (Caucasian males, > 65?years and Caucasian females,
18-55?years), 25, 50, 100 and 150?mg (Japanese males, 18-55?years). Study 2:
Caucasian males (18-55?years) received 1, 2.5, 10 or 25?mg once daily TA-8995 or
placebo for 21-28?days. Blood and urine for pharmacokinetics and/or
pharmacodynamics were collected. Tolerability was assessed by adverse events,
vital signs, electrocardiograms and laboratory safety tests. RESULTS: Peak
TA-8995 concentrations occurred approximately 4?h post-dose. Mean half-lives
ranged from 81 to 166?h, without an obvious dose relationship. Exposure increased
less than proportionally to dose. TA-8995 was not excreted in urine. Following
2.5 to 25?mg once daily dosing, TA-8995 demonstrated nearly complete inhibition
of CETP activity (92-99%), increased high density lipoprotein-cholesterol (HDL-C)
by 96 to 140% and decreased low density liporotein-cholesterol (LDL-C) by 40% to
53%. There were dose-related increases in apolipoproteins A-1 and E, HDL2-C and
HDL3-C, and decreases in apolipoprotein B and lipoprotein A. There was no
evidence of significant effects of age, gender, ethnicity or food on
pharmacokinetics or pharmacodynamics. All doses were well tolerated. CONCLUSIONS:
TA-8995 is a potent CETP inhibitor and warrants further investigation.
|*Asian People
[MESH]
|*White People
[MESH]
|Adolescent
[MESH]
|Adult
[MESH]
|Cholesterol Ester Transfer Proteins/*antagonists & inhibitors
[MESH]