Title:Bioavailability and Pharmacokinetics of Genistein: Mechanistic Studies on its ADME
Volume: 12
Issue: 10
Author(s): Zhen Yang, Kaustubh Kulkarni, Wei Zhu and Ming Hu
Affiliation:
Keywords:
Genistein, Flavonoids, Isoflavone, Bioavailability, Pharmacokinetics, ADME, Metabolism, Transporter, BCRP, estrogen-dependent breast, preneoplastic cells
Abstract: Genistein, one of the most active natural flavonoids, exerts various biological effects including chemoprevention,
antioxidation, antiproliferation and anticancer. More than 30 clinical trials of genistein with various disease indications have been
conducted to evaluate its clinical efficacy. Based on many animals and human pharmacokinetic studies, it is well known that the most
challenge issue for developing genistein as a chemoprevention agent is the low oral bioavailability, which may be the major reason
relating to its ambiguous therapeutic effects and large interindividual variations in clinical trials. In order to better correlate
pharmacokinetic to pharmacodynamics results in animals and clinical studies, an in-depth understanding of pharmacokinetic behavior of
genistein and its ADME properties are needed. Numerous in vitro/in vivo ADME studies had been conducted to reveal the main factors
contributing to the low oral bioavailability of genistein. Therefore, this review focuses on summarizing the most recent progress on
mechanistic studies of genistein ADME and provides a systemic view of these processes to explain genistein pharmacokinetic behaviors
in vivo. The better understanding of genistein ADME property may lead to development of proper strategy to improve genistein oral
bioavailability via mechanism-based approaches.
