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Single‐Dose Pharmacokinetics of Atrasentan, an Endothelin‐A Receptor Antagonist
Author(s) -
Samara Emil,
Dutta Sandeep,
Cao Guoliang,
Granneman G. R.,
Dordal Margaret S.,
MD R. J. Padley
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 - 10.1177/00912700122010258
Subject(s) - pharmacokinetics , medicine , pharmacology , volume of distribution , placebo , distribution (mathematics) , mathematics , mathematical analysis , alternative medicine , pathology
The pharmacokinetics of 1, 10, 23.25, and 139.5 mg doses of atrasentan was assessed in a placebo‐controlled, double‐blind, single oral dose study in 24 healthy male subjects. Atrasentan was well tolerated. Atrasentan pharmacokinetics was linear in the 1 to 23.25 mg dose range, with some dose dependency in the highest dose group. Harmonic mean terminal half‐life was similar across all dose groups (20–25 h). Apparent oral clearance was low (12 L/h) for the highest dose group compared with the other three dose groups (21–27 L/h). The apparent volume of distribution was large (∼6 L/kg), consistent with extensive tissue distribution.