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Pharmacokinetics of CS‐866, a New Angiotensin II Receptor Blocker, in Healthy Subjects
Author(s) -
Schwocho Lee R.,
Masonson Harvey N.
Publication year - 2001
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 - 10.1177/00912700122010393
Subject(s) - pharmacokinetics , bioavailability , oral administration , pharmacology , chemistry , urine , antagonist , medicine , receptor , biology , biochemistry
CS‐866, a novel angiotensin IIreceptor blocker, is rapidly and completely metabolized to RNH‐6270, its active metabolite. The pharmacokinetics of RNH‐6270 following oral CS‐866 or intravenous RNH‐6270 administration was determined in 104 healthy male volunteers. The pharmacokinetics of RNH‐6270 was linear over dose ranges of 1 to 32 mg (intravenous RNH‐6270 administration) and 10 to 160 mg (oral CS‐866 administration). The time to maximum plasma concentration of RNH‐6270 after oral CS‐866 administration ranged from 1.4 to 2.8 hours, and the terminal elimination half‐life ranged from 12 to 18 hours. Absolute bioavailability of RNH‐6270 after oral administration of CS‐866 was 26%. Administration of CS‐866 once daily for 10 days did not result in drug accumulation. When administered intravenously, RNH‐6270 has a volume of distribution of 15 to 25 L. Approximately 35% to 50% of RNH‐6270 is excreted unchanged in the urine. CS‐866 was safe and well tolerated at doses of up to 160 mg/day.