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The 2 nd Polyphenol Meeting

The 2 nd Polyphenol Meeting. Recent Progress of Equol Science Tokyo, Japan July 25, 2008. S-equol is Present in Man as a Metabolic Transformation of Daidzein. OH. O. Intestinal Bacteria Dietary Carbohydrate. HO. O. HO. O. Daidzein (a soy isoflavone). S-equol.

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The 2 nd Polyphenol Meeting

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  1. The 2nd Polyphenol Meeting Recent Progress of Equol Science Tokyo, Japan July 25, 2008

  2. S-equol is Present in Man as a Metabolic Transformation of Daidzein OH O • Intestinal • Bacteria • Dietary • Carbohydrate HO O HO O Daidzein (a soy isoflavone) S-equol

  3. Equol Producers have Health Benefits • Less osteoporosis with greater bone density • Menopausal symptoms less severe • Prostate and breast cancer risk reduced • Lower risk of cardiovascular diseases • Learning and memory may be enhanced • Improved glucose metabolism

  4. S-Equol is Well Absorbed in Man Setchell et al. Am J Clin Nutr 81: 1072-079, 2005 500 S-Equol: 20 mg oral dose Elimination half-life = 4.9 h 400 300 Plasma Concentration (ng/mL) 200 100 Equol Concentration in Japanese 0 0 5 10 15 20 25 Time (h)

  5. S-equol: Mechanism of Action • Binds selectively to ER-β • Antioxidant • Chemoprotective • Down regulates ER- and androgen receptor • Activates NOS and NO production

  6. S-equol is a Potent, Non-steroidal, ER β Selective Agonist OH S-equol HO O

  7. Ausio’s Strategy Develop S-equol as an oral drug for Vasomotor Symptoms and Benign Prostatic Hypertrophy

  8. Progress in Drug Development • Commercial scale synthetic process • Stable drug product • Animal pharmacology supports clinical development • IND filed with FDA • Phase 1 safety studies

  9. Safety Studies for IND • No effect on the uterus • Genotoxicity (all negative) • Safety Pharmacology (all negative) • Respiratory (rat) • Neurotoxicity (rat) • Cardiovascular (monkey)

  10. Safety Studies for IND • ADME (rat, monkey) • 28-day GLP toxicity studies • Rat • Monkey • Large safety margin for human studies

  11. Regulatory and Clinical Development • Pre IND Meeting with FDA • IND submission • Phase 1 studies • Single rising dose (August) • Multi rising dose (October) • Phase 2 studies • Vasomotor Symptoms • Benign Prostatic Hypertrophy

  12. Summary • Since S-equol has been in man for 4,000 years, we believe it to be safe • Equol producers have many health benefits • Ausio is in a strong position to develop S-equol as a drug • Strong patent position • High purity product • IND submitted • Clinical data will confirm safety and efficacy

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