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Osteoporosis
Published in Jason Liebowitz, Philip Seo, David Hellmann, Michael Zeide, Clinical Innovation in Rheumatology, 2023
Mazen Nasrallah, Marcy B. Bolster
A novel strategy in the management of osteoporosis is the combination therapy of estrogen and a selective estrogen receptor modulator (SERM). This approach exploits the differential benefits of estrogen and SERMs on bone while minimizing the untoward effects of either agent by exploiting the nonskeletal effects of the other agent. While the beneficial effects of estrogen on bone health are undeniable, with data showing a reduction in vertebral and nonvertebral fractures, it is no longer considered a first-line therapy due to increased risk of breast cancer, cardiovascular disease, and dementia. A third-generation SERM, on the other hand, is generally protective against breast cancer9 and does not increase risk of endometrial hyperplasia,10 but its skeletal effects are modest (demonstrated efficacy against vertebral11 but not nonvertebral fractures). Furthermore, SERMs often exacerbate climacteric symptoms (vasomotor side effect). As such, the strategy of combining estrogen plus SERM was hypothesized to result in improved skeletal outcomes, while minimizing the side effects of either agent. Indeed, several phase 3 studies have validated the utility of such an approach, showing an increase in bone mineral density with good tolerability, but unfortunately did not report on fracture prevention.12, 13
Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
SERMs (Selective Estrogen Receptor Modulators) are a class of agents that act specifically on the estrogen receptor. A characteristic that distinguishes SERMS from pure receptor agonists or antagonists is that their action is different in various tissues, thereby providing the possibility of selectively inhibiting or stimulating estrogen-like action in various tissues.
Role of Aromatase Inhibitors (AIs) and Selective Estrogen Receptor Modulators (SERMs) in the Treatment of Uterine Leiomyoma
Published in John C. Petrozza, Uterine Fibroids, 2020
Currently selective estrogen receptor modulators (SERMs) are more frequently used for the treatment of osteoporosis and breast cancer, with documented proven benefits [17]. Early generation SERMs such as clomiphene citrate have been used for ovulation induction in polycystic ovarian syndrome (PCOS) related infertility. Newer SERM therapies have been developed for the treatment of postmenopausal vasomotor symptoms in patients with an intact uterus and are also indicated in the treatment of vaginal atrophy and dyspareunia associated with hypoestrogenism. Most of the estrogen representation is mediated by either estrogen receptor (ER)-α or ERβ receptors [17–19]. SERMs are chemically diverse nonsteroidal compounds that belong to one of two different chemical families: the triphenylethylenes and the benzothiophenes, with the exception of fulvestran (downregulator) that acts on the ligand binding domain (LBD) located in the ER carboxyl-terminal site, causing conformational changes which facilitate interactions as a co-activator or co-repressor proteins, and subsequently initiate or suppress the transcription of target genes [17–19]. Different types of SERMs can have both agonist and antagonist action in different target tissues; for example, tamoxifen has agonist action on bone and is an antagonist on the breast ERs and, in addition, it can also have an agonist effect on endometrial tissue.
Effects of intestinal flora on pharmacokinetics and pharmacodynamics of drugs
Published in Drug Metabolism Reviews, 2023
Amina Džidić-Krivić, Jasna Kusturica, Emina Karahmet Sher, Nejra Selak, Nejra Osmančević, Esma Karahmet Farhat, Farooq Sher
In addition, the results noticed in the study conducted by Wang at al. (Wang et al. 2019) that the administration of Escherichia coli Nissle 1917 had protective effects on intestinal injury induced by irinotecan. The key findings were that irinotecan treatment altered the diversity of gut microbiota composition. This drug increased the Proteobacteria relative abundance, compared with its abundance in control group. Therefore, Escherichia coli Nissle application improved the gut microbiota dysbiosis (Wang et al. 2019). In recent years, there were many studies (Diot et al. 2021) that have been developing a model system by using the nematode Caenorhabditis elegans to assess the response of the animals to different drugs such as tamoxifen. It belongs to the class of drugs called SERMs, selective estrogen receptor modulators that is the standard treatment for breast cancers positive for estrogen receptors together with chemotherapy and radiation therapy. The authors of this study (Diot et al. 2021) changed the diet of larval stage animals with one of the three following bacteria: C.aquatica, B. subtilis or E. coli. After the tamoxifen administration to C.elegans, it was proven that tamoxifen toxicity increased in animals fed by C.aquatica and B. subtilis that showed a delay in development.
Skin, hair and beyond: the impact of menopause
Published in Climacteric, 2022
C. C. Zouboulis, U. Blume-Peytavi, M. Kosmadaki, E. Roó, D. Vexiau-Robert, D. Kerob, S. R. Goldstein
Perimenopausal symptomatology is variable in different women. Generally, within 4–5 years of menopause, 80% of women will be devoid of symptoms or have only mild symptoms, while 20% may have symptoms for up to 10 years or longer. The most common climacteric symptoms in around 75% of women are vasomotor symptoms (VMS), including hot flashes, night sweats and sleep disturbance, that may start during perimenopause. VMS will often lead women to consult a physician. A multiethnic study in 3302 women enrolled at seven US sites found that the median total VMS duration was 7.4 years [6]. Risks for hot flashes include early or iatrogenic menopause, females with skin of color or Hispanic ethnic groups, high body mass index or sedentary lifestyle, smoking, anxiety, depression, psychosocial stress and use of selective estrogen receptor modulators (SERMs) or aromatase inhibitors [7].
Clomiphene citrate improved testosterone and sperm concentration in hypogonadal males
Published in Systems Biology in Reproductive Medicine, 2020
Ava Delu, Robert J. Kiltz, Vladimir A. Kuznetsov, J. C. Trussell
While one meta-analysis of randomized controlled trials demonstrated that SERM treatment is associated with statistically significant increases in sperm concentration, motility, and pregnancy rates (Chua et al. 2013), not all similar studies are able to confirm such a desirous outcome (Willets et al. 2013). It seems necessary to further investigate if the positive effects of CC treatment on TT level and sperm concentration associates with improved pregnancy and live birth outcomes. Future studies should include a larger cohort size, post-CC pregnancy and live birth rates, and a study designed with the opportunity to evaluate personalized/multifactorial variables. Lastly, future studies may need to consider a higher serum TT cut point (>400 ng/dL) for prompting EMT in hypogonadal men with UI.