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Single‐Dose Pharmacokinetics, Pharmacodynamics, Tolerability, and Safety of the Soluble Guanylate Cyclase Stimulator BAY 63‐2521: An Ascending‐Dose Study in Healthy Male Volunteers
Author(s) -
Frey Reiner,
Mück Wolfgang,
Unger Sigrun,
ArtmeierBrandt Ulrike,
Weimann Gerrit,
Wensing Georg
Publication year - 2008
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 - 10.1177/0091270008319793
Subject(s) - tolerability , pharmacokinetics , pharmacodynamics , medicine , placebo , pharmacology , blood pressure , pulmonary hypertension , adverse effect , alternative medicine , pathology
The aim of the study was to assess the safety, tolerability, pharmacokinetics, and pharmacodynamics of BAY 63–2521, a new drug in development for pulmonary hypertension. Fifty‐eight healthy male volunteers received a single oral dose of BAY 63–2521 (0.25–5 mg) or placebo. No serious adverse events were reported; there were no life‐threatening events. Heart rate over 1 minute, an indicator of the effect of a vasodilating agent on the cardiovascular system in healthy subjects, was increased dose dependently versus placebo at BAY 63–2521 doses of 1 to 5 mg ( P < .01). Mean arterial and diastolic pressures were decreased versus placebo at doses of 1 mg ( P < .05) and 5 mg ( P < .01). Systolic pressure was not significantly affected. BAY 63–2521 was readily absorbed and exhibited dose‐proportional pharmacokinetics. The pharmacodynamic and pharmacokinetic properties of BAY 63–2521 suggest that it can offer a unique mode of action in the treatment of pulmonary hypertension.