Repeated Oral Once Daily Intake of Increasing Doses of the Novel Synthetic Genistein Product Bonistein™ in Healthy Volunteers

Abstract

Bonistein™ is a new product consisting of > 99.5 % synthetic genistein, an isoflavone with phyto-oestrogenic properties, which might be a safe and efficacious alternative for the prevention of post-menopausal bone loss to the traditional hormone replacement therapy. A randomised, open-labelled and sequential-group phase I study was performed to assess safety, tolerability and pharmacokinetic characteristics of oral administrations of Bonistein™. Thirty healthy volunteers received in three subsequent groups 30, 60 or 120 mg once daily for 14 days. For the pharmacokinetic profiles of Bonistein™, blood samples were taken on study Days 1 (after first dose) and 14 (steady state). Repeated intake of Bonistein™ was well tolerated. A total of 33 adverse events were reported, mainly of mild intensity. No relevant changes in clinical laboratory or vital signs were observed. The pharmacokinetic characteristics of Bonistein™ revealed comparable results for extent and rate of absorption on Days 1 and 14. Both AUC and C_max values of Bonistein™ increased in proportion with the dose.

Key words

Bonistein - genistein - safety - multiple dosing - pharmacokinetics - steady state

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