Literature DB >> 30889096

Safety and feasibility of estrogen receptor-β targeted phytoSERM formulation for menopausal symptoms: phase 1b/2a randomized clinical trial.

Lon S Schneider1, Gerson Hernandez2, Liqin Zhao3, Adrian A Franke4, Yu-Ling Chen1, Sonia Pawluczyk1, Wendy J Mack1, Roberta D Brinton2.   

Abstract

OBJECTIVE: PhytoSERM is a formulation of genistein, daidzein, and S-equol that has an 83-fold selective affinity for estrogen receptor-β (ERβ); and may enhance neuron function and estrogenic mechanisms in the brain without having peripheral estrogenic activity.
METHODS: We conducted an overarching, two-stage, dose-ranging, double-blinded, randomized, placebo-controlled trial of 12 weeks duration comparing 50 and 100 mg/d of phytoSERM with placebo for noncognitively impaired, perimenopausal women aged 45 to 60, with intact uteri and ovaries, with at least one cognitive complaint, and one vasomotor-related symptom. Primary objectives were to assess safety and tolerability of a 50 and 100 mg daily dose; and, secondly, to evaluate potential indicators of efficacy on cognition and vasomotor symptoms over 4 and 12 weeks, and using an embedded, 4-week, 2-period, placebo-controlled crossover trial for a subset of participants.
RESULTS: Seventy-one women were randomized to treatment; 70 were evaluated at 4 weeks; 12 were entered into the crossover study; 5 did not complete 12 weeks. Reasons for discontinuation were withdrawal of consent (n = 1) and lost to follow-up (n = 4). Adverse events occurred in 16.7% (n = 4) placebo, 39.1% (n = 9) 50 mg/d, and 29.2% (n = 7) 100 mg/d treated participants; 85% were mild and none was severe. Vaginal bleeding occurred in 0, placebo; 1, 50 mg; and 3, 100 mg/d participants.
CONCLUSIONS: The phytoSERM formulation was well tolerated at 50 and 100 mg daily doses. Based on safety outcomes, vaginal bleeding at the 100 mg dose, and vasomotor symptoms and cognitive outcomes at 12 weeks, a daily dose of 50 mg was considered preferable for a phase 2 efficacy trial.

Entities:  

Year:  2019        PMID: 30889096      PMCID: PMC6663614          DOI: 10.1097/GME.0000000000001325

Source DB:  PubMed          Journal:  Menopause        ISSN: 1072-3714            Impact factor:   2.953


  50 in total

1.  Dietary phytoestrogen intakes and cognitive function during the menopausal transition: results from the Study of Women's Health Across the Nation Phytoestrogen Study.

Authors:  Gail A Greendale; Mei-Hua Huang; Katherine Leung; Sybil L Crawford; Ellen B Gold; Richard Wight; Elaine Waetjen; Arun S Karlamangla
Journal:  Menopause       Date:  2012-08       Impact factor: 2.953

2.  Bioavailability of pure isoflavones in healthy humans and analysis of commercial soy isoflavone supplements.

Authors:  K D Setchell; N M Brown; P Desai; L Zimmer-Nechemias; B E Wolfe; W T Brashear; A S Kirschner; A Cassidy; J E Heubi
Journal:  J Nutr       Date:  2001-04       Impact factor: 4.798

3.  The pharmacokinetics of S-(-)equol administered as SE5-OH tablets to healthy postmenopausal women.

Authors:  Kenneth D R Setchell; Xueheng Zhao; Susan E Shoaf; Karen Ragland
Journal:  J Nutr       Date:  2009-09-23       Impact factor: 4.798

4.  Potentiation of brain mitochondrial function by S-equol and R/S-equol estrogen receptor β-selective phytoSERM treatments.

Authors:  Jia Yao; Liqin Zhao; Zisu Mao; Shuhua Chen; Karren Carmen Wong; Jimmy To; Roberta Diaz Brinton
Journal:  Brain Res       Date:  2013-02-18       Impact factor: 3.252

5.  The pharmacokinetic behavior of the soy isoflavone metabolite S-(-)equol and its diastereoisomer R-(+)equol in healthy adults determined by using stable-isotope-labeled tracers.

Authors:  Kenneth Dr Setchell; Xueheng Zhao; Pinky Jha; James E Heubi; Nadine M Brown
Journal:  Am J Clin Nutr       Date:  2009-08-26       Impact factor: 7.045

6.  Effect of L-methionine on hot flashes in postmenopausal women: a randomized controlled trial.

Authors:  Thomas Guttuso; Michael P McDermott; Phillip Ng; Karl Kieburtz
Journal:  Menopause       Date:  2009 Sep-Oct       Impact factor: 2.953

7.  Comparing the pharmacokinetics of daidzein and genistein with the use of 13C-labeled tracers in premenopausal women.

Authors:  Kenneth D R Setchell; Marian S Faughnan; Tony Avades; Linda Zimmer-Nechemias; Nadine M Brown; Brian E Wolfe; Wayne T Brashear; Panjak Desai; Mark F Oldfield; Nigel P Botting; Aedin Cassidy
Journal:  Am J Clin Nutr       Date:  2003-02       Impact factor: 7.045

8.  Soya isoflavone supplementation enhances spatial working memory in men.

Authors:  Alicia A Thorp; Natalie Sinn; Jonathan D Buckley; Alison M Coates; Peter R C Howe
Journal:  Br J Nutr       Date:  2009-06-01       Impact factor: 3.718

9.  Desvenlafaxine for the treatment of vasomotor symptoms associated with menopause: a double-blind, randomized, placebo-controlled trial of efficacy and safety.

Authors:  David F Archer; Caroline M Dupont; Ginger D Constantine; James H Pickar; Sophie Olivier
Journal:  Am J Obstet Gynecol       Date:  2009-01-24       Impact factor: 8.661

10.  Brain structure and cognition 3 years after the end of an early menopausal hormone therapy trial.

Authors:  Kejal Kantarci; Nirubol Tosakulwong; Timothy G Lesnick; Samantha M Zuk; Val J Lowe; Julie A Fields; Jeffrey L Gunter; Matthew L Senjem; Megan L Settell; Carey E Gleason; Lynne T Shuster; Kent R Bailey; N Maritza Dowling; Sanjay Asthana; Clifford R Jack; Walter A Rocca; Virginia M Miller
Journal:  Neurology       Date:  2018-03-21       Impact factor: 9.910

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  8 in total

1.  Retrospective analysis of phytoSERM for management of menopause-associated vasomotor symptoms and cognitive decline: a pilot study on pharmacogenomic effects of mitochondrial haplogroup and APOE genotype on therapeutic efficacy.

Authors:  Yiwei Wang; Gerson Hernandez; Wendy J Mack; Lon S Schneider; Fei Yin; Roberta D Brinton
Journal:  Menopause       Date:  2020-01       Impact factor: 2.953

Review 2.  Sex differences in cognition following variations in endocrine status.

Authors:  Rachel Bowman; Maya Frankfurt; Victoria Luine
Journal:  Learn Mem       Date:  2022-09-02       Impact factor: 2.699

3.  Involvement of α7nAChR in the Protective Effects of Genistein Against β-Amyloid-Induced Oxidative Stress in Neurons via a PI3K/Akt/Nrf2 Pathway-Related Mechanism.

Authors:  Jianbin Guo; Guoqing Yang; Yuqing He; Huiming Xu; Hong Fan; Jing An; Lingling Zhang; Rui Zhang; Guihua Cao; Dingjun Hao; Hao Yang
Journal:  Cell Mol Neurobiol       Date:  2020-11-19       Impact factor: 5.046

Review 4.  Therapeutic Potential of Isoflavones with an Emphasis on Daidzein.

Authors:  Mohammed M Alshehri; Javad Sharifi-Rad; Jesús Herrera-Bravo; Evelyn L Jara; Luis A Salazar; Dorota Kregiel; Yadav Uprety; Muhammad Akram; Mehwish Iqbal; Miquel Martorell; Margalida Torrens-Mas; Daniel Gabriel Pons; Sevgi Durna Daştan; Natália Cruz-Martins; Fethi Ahmet Ozdemir; Manoj Kumar; William C Cho
Journal:  Oxid Med Cell Longev       Date:  2021-09-09       Impact factor: 6.543

5.  The Effect of Polyphenols on Working and Episodic Memory in Non-pathological and Pathological Aging: A Systematic Review and Meta-Analysis.

Authors:  Karin de Vries; Evelyn Medawar; Aniko Korosi; A Veronica Witte
Journal:  Front Nutr       Date:  2022-01-26

Review 6.  Potential Protective Mechanisms of S-equol, a Metabolite of Soy Isoflavone by the Gut Microbiome, on Cognitive Decline and Dementia.

Authors:  Akira Sekikawa; Whitney Wharton; Brittany Butts; Cole V Veliky; Joshua Garfein; Jiatong Li; Shatabdi Goon; Annamaria Fort; Mengyi Li; Timothy M Hughes
Journal:  Int J Mol Sci       Date:  2022-10-07       Impact factor: 6.208

Review 7.  Molecular Mechanisms of Action of Genistein in Cancer: Recent Advances.

Authors:  Hardeep Singh Tuli; Muobarak Jaber Tuorkey; Falak Thakral; Katrin Sak; Manoj Kumar; Anil Kumar Sharma; Uttam Sharma; Aklank Jain; Vaishali Aggarwal; Anupam Bishayee
Journal:  Front Pharmacol       Date:  2019-12-06       Impact factor: 5.810

Review 8.  Natural Anti-Inflammatory Compounds as Drug Candidates for Inflammatory Bowel Disease.

Authors:  Linshan Duan; Shuyu Cheng; Long Li; Yanling Liu; Dan Wang; Guoyan Liu
Journal:  Front Pharmacol       Date:  2021-07-14       Impact factor: 5.810

  8 in total

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