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10.1111/bcp.12380 http://scihub22266oqcxt.onion/10.1111/bcp.12380 C4243901!4243901!24628035     free     free     free Warning: file_get_contents(https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=24628035&cmd=llinks): Failed to open stream: HTTP request failed! 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Tolerability, pharmacokinetics and pharmacodynamics of TA-8995, a selective cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects |pdf=|usr=}}{{24628035}} gab.com Text Tolerability, pharmacokinetics and pharmacodynamics of TA-8995, a selective cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects JO: Br J Clin Pharmacol http://www.kidney.de/pget.php?&tw=1&pmid=24628035 #FOAvip 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. Twit Text FOAVip Tolerability, pharmacokinetics and pharmacodynamics of TA-8995, a selective cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects ????Br J Clin Pharmacol http://www.kidney.de/pget.php?&tw=1&pmid=24628035 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=24628035 #FOAvip English Wikipedia <ref>{{Cite pmid|24628035}}</ref> 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 JJP Br J Clin Pharmacol 2014[Sep]; 78 (3): 498-508 PMID24628035show 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. äTolerability, pharmacokinetics and pharmacodynamics of TA-8995, a sele(epmc).pdf DeepDyve Pubget Overpricing