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By Ronald T. Borchardt, Roger M. Freidinger, Tomi K. Sawyer, Philip L. Smith

This quantity offers case histories illustrating the kinds of interdisciplinary interactions essential to layout drug applicants with optimum pharmacological, pharmaceutical, biopharmaceutical, and metabolic/pharmacokinetic homes. Key positive aspects comprise an incisive dialogue of HIV protease inhibitors and 287 illustrations.

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J. Pharm. 73:231–237. Steinberg, M. , Wiest, S. , and Palkowitz, A. , 1993, Nonpeptide angiotensin II receptor antagonists, Cardiovasc. Drug Rev. 11:312–358. , and Sever, P. , 1993, Non–angiotensin effects of angiotensin-converting enzyme inhibitors, Clin. Sci. 85:661–670. , Jones, D. , and Leckie, B. , 1983, Novel transition-state analogue inhibitors of renin, in: Peptides, Structure and Function. Proceedings of the Eighth American Peptide Symposium (V. J. Hruby and D. H. ), pp. , Rockford, IL.

D. rat model were definitive and discouraging. Whereas portal drug levels for A-65317 were higher than those observed with 4 and 5b, essentially no drug reached the systemic circulation, indicating almost complete hepatic extraction. , 1990, 1992a). Despite the lack of oral activity, the discovery and characterization of enalkiren and A-65317 was a significant milestone for the project, one that required 3-1/3 years of research and the synthesis and biological evaluation of 1400 inhibitors to achieve.

2. INHIBITOR SOLUBILITY Following these disappointing results, we focused our attention on physicochemical properties that could be quickly and easily measured and that might potentially correlate with either intestinal absorption or biliary excretion. Our primary analysis was aqueous solubility, although octanol–water partition coefficient data were also obtained for selected inhibitors. , 1989). d. rat model and that it was more efficient to proceed directly to the in vivo system. , 1989) were in fact quite insoluble (Table II), leading us to speculate that this was the underlying factor behind the lack of intestinal absorption.

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