Selective Estrogen Receptor Modulators: An Update on Recent Clinical Findings

Shelly, W.B.; Draper, Michael W.; Krishnan, Venkatesh; Wong, Mayme; Jaffe, Robert B.

doi:10.1097/ogx.0b013e31816400d7

Cited by 160 publications

(23 citation statements)

References 174 publications

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“…These Ormeloxifene is an optimally designed SERM, which behaves like an estrogen antagonist in uterus with mild agonistic action on vagina, bone and serum lipids. [4][5][6] Ormeloxifene has been evaluated for the management of menorrhagia but not against progesterone. This study was an attempt to find out the effectiveness of ormeloxifene against medroxyprogesterone acetate (MPA).…”

Section: Introductionmentioning

confidence: 99%

Ormeloxifene versus Medroxyprogesterone Acetate (MPA) in the Treatment of Dysfunctional Uterine Bleeding: A Double-Blind Randomized Controlled Trial

Shravage¹,

Mekhala²,

Bellad³

et al. 2011

Journal of South Asian Federation of Obstetrics and Gynaecology

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Objective To find the effectiveness of ormeloxifene vs medroxyprogesterone acetate (MPA) to reduce blood loss in dysfunctional uterine bleeding (DUB). Materials and methods: Design—A double blind randomized controlled trial. Data source—The women attending gynecology OPD in teaching hospital attached to Jawaharlal Nehru Medical College, Belgaum, India for menorrhagia, meeting the selection criteria were enrolled into the study. Randomization—Computer-generated randomization, with block size of two, was done into two groups. Intervention—One group (group A) received capsule ormeloxifene 60 mg to be taken two days a week at an interval of 3 days, and a placebo form of medroxyprogesterone acetate for 21 days starting from day 2 to 5 of the menstrual cycle for three consecutive cycles. Other group (group B) received medroxyprogesterone acetate (MPA) 10 mg for 21 days starting from day 2 to 5 of the menstrual cycle, and a placebo form of ormeloxifene for 2 days a week with an interval of 3 days for three consecutive cycles. The drug and its placebo were in similar capsular form. All the participants were ensured to use the similar type of sanitary napkins, and transvaginal ultrasonography was done to note the endometrial thickness (ET) before and after the drug therapy. Blinding—The department of clinical pharmacy prepared the drug packets and kept the randomization code till the data was analyzed, thus ensuring the double blinding. Outcome Participants were interviewed during subsequent cycle. Pictorial blood assessment chart (PBAC) score was used to calculate blood loss during menses at the first and subsequent three months. Data analysis The mean PBAC scores and endometrial thickness were compared in two groups. Results The mean pretreatment PBAC scores in group A and group B were 262.26 and 238.71 ml respectively. The mean PBAC scores at the end of the study period were 73 and 108 in group A and B respectively, reporting an overall reduction in mean blood loss by 85.7 and 54.76% (p = 0.0205) in group A and B respectively. Thus, there was a significant reduction in blood loss in the group receiving ormeloxifene. The reduction in the mean endometrial thickness was more in ormeloxifene group. However, this was not statistically significant (p = 0.0942). Conclusion Ormeloxifene is more effective as compared to MPA in reducing the blood loss in the treatment of DUB.

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Section: Introductionmentioning

confidence: 99%

Ormeloxifene versus Medroxyprogesterone Acetate (MPA) in the Treatment of Dysfunctional Uterine Bleeding: A Double-Blind Randomized Controlled Trial

Shravage¹,

Mekhala²,

Bellad³

et al. 2011

Journal of South Asian Federation of Obstetrics and Gynaecology

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“…It acts as estrogen antagonist in uterine endometrium, leading to endometrial atrophy hence decreases menstrual blood loss. 27 This may explain for the oligomenorrhea in the form of delayed or scanty menses and in certain cases amenorrhea as the side effect of this therapy which is mostly dose dependent and reversible once the drug is stopped. This has been evidenced by a great number of studies.…”

Section: Discussionmentioning

confidence: 99%

A prospective study on the role of centchroman in regression of fibroadenoma

et al. 2021

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Background: Fibroadenoma commonly present as painless breast lump in young girls. Nearly 10-15% regress spontaneously over the period of 6-60 months, rest are managed surgically. Centchroman (Saheli), a novel non-steroidal, selective anti-estrogen has been used for the treatment of mastalgia and its effectiveness in the treatment of fibroadenoma is being tested in the ongoing trials. Methods: A total of 60 patients between 15-35 years of age with painless lump breast of size 2 to 5 centimeters confirmed as fibroadenoma by fine needle aspiration cytology (FNAC) were included in the study. Detailed patient's characteristics, clinical history, physical examination (for size in 2 dimensions), ultrasound findings (for size in 3 dimensions) were assessed. All participants included in the study were given tablet Centchroman (Saheli) 30 mg thrice weekly orally for 3 months. Size of Fibroadenoma was reassessed clinically for size in two dimensions and ultrasonologically for size in three dimensions at 4 weeks and 3 months of starting of therapy.Results: Out of 60 patients, 18 patients (30%) had complete response, 40 patients (66.66%) showed a decrease in the size of fibroadenoma and only 2 patients (3.33%) had no response to this therapy. None showed an increase in size.Conclusions: It may prove to be the most effective modality for the treatment of small sized fibroadenoma breast especially in unmarried girls with minimal side effects. Ultrasonology may be relied upon for follow up measurements since it is more accurate in measuring the dimensions.

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“…Tamoxifen is a triphenylethylene belonging to the class of drugs known as selective estrogen receptor modulators (SERMs). SERMs bind to and either activate or repress the estrogen receptor (ER), a nuclear hormone receptor (NHR) transcription factor (Shelly et al, 2008). Tamoxifen is commonly used to treat ER-positive breast cancers, as well as other estrogen-dependent ailments such as ovarian or endometrial carcinoma (Jordan, 2003;Shagufta and Ahmad, 2018).…”

Section: Systematic Identification Of C B a Effec He H D G E Ementioning

confidence: 99%

Bacterial diet modulates tamoxifen-induced death via host fatty acid metabolism

Diot

García-González

Vieira

et al. 2021

Preprint

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SUMMARYTamoxifen is a selective estrogen receptor (ER) modulator that is used to treat ER-positive breast cancer, but that at high doses kills both ER-positive and ER-negative breast cancer cells. We recapitulate this off-target effect in Caenorhabditis elegans, which does not have an ER ortholog. We find that different bacteria dramatically modulate tamoxifen toxicity in C. elegans, with a three-order of magnitude difference between animals fed Escherichia coli, Comamonas aquatica, and Bacillus subtilis. Remarkably, host fatty acid (FA) biosynthesis mitigates tamoxifen toxicity, and different bacteria provide the animal with different FAs, resulting in distinct FA profiles. Surprisingly these bacteria modulate tamoxifen toxicity by different death mechanisms, some of which are modulated by FA supplementation and others by antioxidants. Together, this work reveals a complex interplay between microbiota, FA metabolism and tamoxifen toxicity that may provide a blueprint for similar studies in more complex mammals.

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Selective Estrogen Receptor Modulators: An Update on Recent Clinical Findings

Cited by 160 publications

References 174 publications

Ormeloxifene versus Medroxyprogesterone Acetate (MPA) in the Treatment of Dysfunctional Uterine Bleeding: A Double-Blind Randomized Controlled Trial

Ormeloxifene versus Medroxyprogesterone Acetate (MPA) in the Treatment of Dysfunctional Uterine Bleeding: A Double-Blind Randomized Controlled Trial

A prospective study on the role of centchroman in regression of fibroadenoma

Bacterial diet modulates tamoxifen-induced death via host fatty acid metabolism

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