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The Effects of a New Thromboxane Synthetase Inhibitor, CGS‐13080, in Man
Author(s) -
MACNAB MALCOLM W.,
FOLTZ E. L.,
GRAVES BETTY S.,
RINEHART ROY K.,
TRIPP SPENCER L.,
FELICIANO NANCY R.,
SEN SUPRADIP
Publication year - 1984
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1984.tb02768.x
Subject(s) - pharmacology , thromboxane a synthase , thromboxane a2 , medicine , platelet
CGS‐13080 is a new potent selective inhibitor of thromboxane synthetase. This study reports the results of a safety and efficacy study of single oral doses in normal healthy volunteers. The compound was well tolerated by all subjects without evidence of any adverse reactions. Serum thromboxane B 2 levels (the stable metabolic product of thromboxane A 2 ) were significantly reduced after administration of the compound, with the maximal effect of a 99 per cent reduction occurring at 0.5 and 1 hour after administration. There was a concomitant increase in PGE 2 and 6‐keto‐PGF 1α (the stable metabolic product of PGI 2 ), suggesting a shunting of cyclic endoperoxide metabolism. The apparent half‐life of the compound is about 1 hour, but return to 50 percent of the original thromboxane B 2 levels was achieved between 4 and 6 hours. Platelet aggregation to collagen and bleeding times failed to demonstrate significant changes after drug administration. Bleeding times showed a slight increase 2 hours after administration of the compound.