Bioavailability and Pharmacokinetics of Genistein: Mechanistic Studies on its ADME

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 16, 12 Issues, 2016

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex

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Bioavailability and Pharmacokinetics of Genistein: Mechanistic Studies on its ADME

Anti-Cancer Agents in Medicinal Chemistry, 12(10): 1264-1280.

Author(s): Zhen Yang, Kaustubh Kulkarni, Wei Zhu and Ming Hu.

Affiliation: Department of Pharmacological and Pharmaceutical Science, College of Pharmacy, University of Houston, Houston, Texas 77030.


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.


Genistein, Flavonoids, Isoflavone, Bioavailability, Pharmacokinetics, ADME, Metabolism, Transporter, BCRP, estrogen-dependent breast, preneoplastic cells.

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Article Details

Volume: 12
Issue Number: 10
First Page: 1264
Last Page: 1280
Page Count: 17
DOI: 10.2174/187152012803833107
Price: $58

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