Why the study?
Does the new aldosterone antagonist OH OPC(ME)-K have comparable renal antimineralocorticoid activity to spironolactone in healthy men?
Does the new aldosterone antagonist OH OPC(ME)-K have comparable renal antimineralocorticoid activity to spironolactone in healthy men?
A simple single-dose protocol can provide a useful estimate of the relative potency of new aldosterone antagonists compared to spironolactone at an early stage of development.
OH OPC(ME)-K shows ~0.6 relative potency to spironolactone; supports single-dose bioassays for early potency estimation of novel aldosterone antagonists.
The renal antimineralocorticoid activity of single oral doses of a new aldosterone antagonist OH OPC(ME)-K was compared to that of spironolactone in two studies in healthy men. OH OPC(ME)-K reversed the urinary electrolyte response to fludrocortisone in the period up to 16 hr after treatment, but it was less potent than spironolactone on a weight basis. The best estimate of the relative potency of OH OPC(ME)-K: spironolactone (derived from a simple protocol using equal single doses of the two drugs) was 0.60:1 (95% confidence limits 0.24:1 to 1.42:1), in good agreement with the estimate from a more complex three-dose parallel-line bioassay (0.61:1, 95% confidence limits 0.48:1 to 0.79:1). The results of simple single-dose studies can be used, with certain assumptions, to provide a useful estimate of the relative potency of new aldosterone antagonists at an early stage of development.
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McInnes et al. (1981) studied this question.
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