scholarly journals The NK3 Receptor Antagonist ESN364 Suppresses Sex Hormones in Men and Women

2016 ◽  
Vol 101 (2) ◽  
pp. 417-426 ◽  
Author(s):  
Graeme L. Fraser ◽  
Steven Ramael ◽  
Hamid R. Hoveyda ◽  
Lien Gheyle ◽  
Jean Combalbert
Keyword(s):  
Menstrual Cycle ◽  
Oral Administration ◽  
Women’S Health ◽  
Women's Health ◽  
Sex Hormones ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Men And Women ◽  
Endometrial Thickening ◽  
Nk3 Receptor ◽  
Health Disorders

Context: Women's health disorders are commonly treated by agents that suppress the hypothalamic-pituitary-gonadal axis. NK3 receptor antagonism modulates this axis with distinct pharmacology compared to existing therapies. Objective: The study aim was to evaluate safety, pharmacokinetics, and pharmacodynamics on gonadotropins and sex hormones after single- and multiple-dose administration of an NK3R antagonist to healthy men and women. Design and Setting: This was a first-in-human, double-blind, placebo-controlled, combined single and multiple ascending dose trial. Participants: Forty-one men and 24 regularly cycling women participated in the study. Intervention(s): In part 1 of the study, men received single oral doses of 3–180 mg or placebo. In part 2, men received placebo or 20, 60, or 180 mg each day for 10 days. In part 3, women received placebo or 20, 60, or 180 mg each day for 21 days, where dosing was initiated on day 3 ± 2 after menses. Main Outcome Measure(s): Safety, tolerability, pharmacokinetics, and pharmacodynamics on circulating levels of LH, FSH, testosterone, estradiol, and progesterone, in addition to physiological biomarkers of endometrial thickening, follicle growth, and the duration of the menstrual cycle were evaluated. Results: ESN364 was well-tolerated and rapidly bioavailable with linear pharmacokinetics and no drug accumulation with repeated, daily oral administration. Drug treatment dose-dependently decreased basal LH, but not FSH, and consequently decreased estradiol and progesterone (in women) as well as testosterone (in men). The hormonal changes in women corresponded to delayed ovulation, decreased endometrial thickening, impeded follicular maturation, and prolongation of the menstrual cycle. Drug effects were rapidly reversible. Conclusions: Oral administration of the NK3R antagonist, ESN364, suppressed the hypothalamic-pituitary-gonadal axis in healthy volunteers by selective modulation of gonadotropin secretion, leading to a restrained decrease in ovarian hormone levels in women. These results suggest that ESN364 may offer therapeutic benefit in the treatment of women's health disorders with a mitigated risk of menopausal-like adverse events.

scholarly journals One drug does not fit all: impact of sex and gender on pharmacological response

2017 ◽  
Vol 39 (1) ◽  
pp. 14-17
Author(s):  
Flavia Franconi ◽  
Ilaria Campesi
Keyword(s):  
Women’S Health ◽  
Women's Health ◽  
Demographic Characteristics ◽  
Sex And Gender ◽  
Men And Women ◽  
Pharmacological Response ◽  
Health And Illness ◽  
And Gender ◽  
Study Participants ◽  
Gender Specific

It is important to remember that gender health and illness should not to be conflated with women's health and illness. Turshen1 reports that numerous studies with ‘gender’ in the title use the word gender as a synonym for ‘women’ and as a result, men's gender-specific needs are missed. In addition, in reporting demographic characteristics of the study participants, some clinical trialists use the term ‘gender’ and some ‘sex’ to indicate men and women and this may create confusion. It can be difficult to separate the two concepts, because there are continuous and constant interactions and relationships between sex and gender3. In other words, sex and gender work together. However, little attention is paid to the fact that gender is a sex modifier. It is relevant to have in mind that both sex and gender affect health and illness4.

scholarly journals Serum Sex Hormones and the Risk of Fracture Across the Menopausal Transition: Study of Women’s Health Across the Nation

2019 ◽  
Vol 104 (6) ◽  
pp. 2412-2418 ◽  
Author(s):  
Jane A Cauley ◽  
Kristine Ruppert ◽  
Yinjuan Lian ◽  
Joel S Finkelstein ◽  
Carrie A Karvonen-Gutierrez ◽  
...  
Keyword(s):  
Women’S Health ◽  
Women's Health ◽  
Sex Hormones ◽  
Menopausal Transition ◽  
Risk Of Fracture ◽  
Transition Study

scholarly journals Correlation Differences between Sex and Stress Hormones in Men And Women

2021 ◽  
Vol 6 (1) ◽  
pp. 327-331
Author(s):  
L. D. Popova ◽  
I. M. Vasylyeva ◽  
O. A. Nakonechna
Keyword(s):  
Menstrual Cycle ◽  
Blood Serum ◽  
Sex Hormones ◽  
Negative Correlation ◽  
Luteal Phase ◽  
Stress Hormones ◽  
Follicular Phase ◽  
Sympathoadrenal System ◽  
Men And Women ◽  
Positive Correlations

The excessive aggression is an actual problem of modern society but the mechanisms of aggressiveness development have not been sufficiently investigated. Women aggression is considered to differ from men one and results obtained on males cannot be extrapolated on females. Sex hormones have a crucial role in the generation of sexually dimorphic aggression circuits during development and their maintenance during adulthood. Hypothalamic pituitary adrenal axis and sympathoadrenal system are major neuroendocrine systems that respond to stress. Stress hormones are involved into behavioral reactions of organism. Gonadal, hypothalamic pituitary adrenal axes, and sympathoadrenal system are tightly interrelated and every of them can influence another one. The purpose of the study was to estimate correlation differences between sex and stress hormones in men and women. Material and methods. Forty healthy young people aged 18 to 22 years with a body mass index of 19-24 (21 women and 19 men) were enrolled in the study. Hormone levels in blood serum were determined by Testosterone, Estradiol, Cortisol ELISA kits (Italy), Epinephrine/Norepinephrine (EPI) ELISA kit (China). Results and discussion. In all phases of the menstrual cycle, the level of cortisol in women was lower than in men, but in the luteal phase these differences were not statistically significant. In all phases of the menstrual cycle, the blood serum norepinephrine content in women was lower than in men, but in the follicular phase these differences were not statistically significant. The level of epinephrine in women during ovulation and luteal phase did not differ from the level of epinephrine in men, but in follicular phase it was significantly lower. Calculations of correlations between individual hormones revealed a significant difference between them in men and women. Positive correlations between testosterone and estradiol and between cortisol and epinephrine; a strong negative correlation between epinephrine and testosterone/norepinephrine ratio were found in men. Positive correlation between testosterone and cortisol and negative correlation between estradiol and cortisol/testosterone ratio were revealed in women. Conclusion. In women, strong correlations were found between cortisol and sex hormones; in men, strong interrelationship was revealed between cortisol and epinephrine. Both in men and in women (in all phases of the menstrual cycle), high positive correlations between testosterone/norepinephrine and cortisol/norepinephrine ratios were observed

scholarly journals Development of an Assessment Tool of Menstrual-Cycle-Related Signs and Symptoms Based on Thai Traditional Medicine Principles for Evaluation of Women’s Health

2021 ◽  
Vol 2021 ◽  
pp. 1-16
Author(s):  
Kodchanipha Sutthibut ◽  
Arunporn Itharat ◽  
Phechnoy Singchungchai ◽  
Preecha Wanichsetakul ◽  
Weerachai Pipatrattanaseree ◽  
...  
Keyword(s):  
Factor Analysis ◽  
Menstrual Cycle ◽  
Traditional Medicine ◽  
Women’S Health ◽  
Women's Health ◽  
Content Validity ◽  
Associated Factors ◽  
Delphi Technique ◽  
Assessment Tool ◽  
Signs And Symptoms

Background. Utilization of Thai traditional medicine (TTM) was considered in menstrual-cycle-related signs and symptoms (MCSs) to evaluate women’s health. TTM clinicians diagnosed the MCSs by signs, symptoms, and associated factors of patients including a physical examination to find patterns of imbalance elements and the origin of the disorder to optimize treatment. Thus, the purpose of this study was to develop a new assessment tool, the menstrual-cycle-related signs and symptoms questionnaire (MCSQ) based on TTM principles for evaluation of women’s menstrual health. Methods. The items and components of the MCSQ were adjusted by TTM expert consensus using the Delphi technique. The content validity of the MCSQ was quantified by the content validity index (CVI). MCSQ were examined by construct validity and internal consistency reliability using exploratory factor analysis (EFA) and Cronbach’s α coefficient, respectively. Results: All 19 experts (100%) responded to the questionnaires in the three rounds of the Delphi technique. The MCSQ showed high content validity of individual items (I-CVI = 0.83–1.00) and high overall content validity of the questionnaire (S-CVI/AVE = 0.98). Overall, 429 of 432 participants completed the questionnaire (99.31%). After factor analysis, the final MCSQ was divided into two sections, which consisted of 49 items. The first had 23 items focusing on the MCSs. And, the second had 14 items of personal and medical data including 12 items of associated factors. Cronbach’s α coefficient of the final MCSQ was 0.87, and that of each component was between 0.32 and 0.82. Conclusions. This study reports a new MCS questionnaire tool, which was developed from TTM knowledge to evaluate women’s health. This questionnaire showed an acceptable level of validity and reliability. Thus, it is also expected to be useful in clinical practice and ongoing research on evaluation of women’s health.

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