ERAAs for menopause treatment: Welcome the ‘designer estrogens’

Hirsch, Heather; Shih, Elim; Thacker, Holly L.

doi:10.3949/ccjm.84a.15140

Cited by 6 publications

(7 citation statements)

References 50 publications

(40 reference statements)

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“…30 MPA would be a better choice because fulvestrant causes menopausal symptoms and is much less tolerable in premenopausal women. 40 In addition, MPA is much less expensive and can be stored at room temperature. One potential concern is that MPA induces cervical epithelium atrophy ( Figure 1B).…”

Section: Discussionmentioning

confidence: 99%

Medroxyprogesterone Acetate Prevention of Cervical Cancer through Progesterone Receptor in a Human Papillomavirus Transgenic Mouse Model

Baik

Mehta

Chung

2019

The American Journal of Pathology

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Cervical dysplastic lesions called cervical intraepithelial neoplasias (CINs) need be treated to prevent cervical cancer. Currently available surgical procedures are effective, but the development of noninvasive treatment is warranted. In human papillomavirus transgenic mice engineered to express human papillomavirus type 16 E6 and E7, short-term treatment with 17b-estradiol induces CINs that progress to cervical cancer if the treatment is continued. In the present study, this mouse model was used to determine whether medroxyprogesterone acetate (MPA), a progestin drug, is chemopreventive. Human papillomavirus transgenic mice bearing CIN lesions were treated with MPA plus 17b-estradiol. Unlike control mice treated with 17b-estradiol alone, cervical cancer was absent in the MPA-treated mice. This observation suggests that MPA prevented CIN from progressing to invasive cancer. MPA was associated with inhibited cell proliferation and the promotion of apoptosis in CIN lesions. Confirming the role of the progesterone receptor, the preventive effect of MPA was absent in human papillomavirus transgenic mice in which the expression of progesterone receptor was genetically ablated. These results suggest that MPA is efficient in treating progesterone receptorepositive CIN lesions. These findings provide the basis for a biomarker-driven clinical trial of the secondary prevention of cervical cancer.

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Section: Discussionmentioning

confidence: 99%

Medroxyprogesterone Acetate Prevention of Cervical Cancer through Progesterone Receptor in a Human Papillomavirus Transgenic Mouse Model

Baik

Mehta

Chung

2019

The American Journal of Pathology

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“…47 In SMART-3 both doses of conjugated equine estrogen -BZA were more effective than placebo at increasing superficial vaginal cells and decreased parabasal cells at 12 weeks (P < .01). 49 Safety and side effect profiles were similar to placebo. Unlike common estrogen/progestogen therapy, conjugated equine estrogen -BZA is not associated with increased breast tenderness.…”

Section: Estrogen Receptor Agonist-antagonistsmentioning

confidence: 85%

Postmenopausal Hormone Therapy—Local and Systemic: A Pharmacologic Perspective

Smith

Sahni

Thacker

2020

The Journal of Clinical Pharma

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Every woman, if she lives long enough, will transition into menopause, and as the US population ages, women will be spending more time in a postmenopausal state than before. For postmenopausal women, the decision to initiate menopausal hormone therapy should be individualized. A thorough evaluation of the patient's cardiovascular, venous thromboembolic, cancer, and fracture risk should be considered along with the woman's quality of life. Hormone therapy exerts its therapeutic effects on vasomotor symptoms, the skeleton, and the genitourinary system independent of age since menopause and these benefits are lost once hormone therapy is stopped. Here we review the pharmacologic properties dose, formulation, mode of administration, timing of initiation, and duration of hormonal therapies in regard to optimizing benefit and minimizing risk to the patient. This discussion will focus on the effects of common hormonal therapies including estrogen (local and systemic), progesterone, estrogen receptor agonist/antagonist, and local dehydroepiandrosterone and include a brief review of compounded bioidentical hormone therapy.

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“…SERMs/ERAAs have been used in the prevention and treatment of postmenopausal bone fractures related to osteoporosis or to breast cancer 10) . SERMs/ ERAAs include antagonist (tamoxifen) and agonists (raloxifene, ospemifene, arzoxifene, lasofoxifene, toremifene, and conjugated estrogen/bazedoxifene) 10) . tissue specificity, localization of subcellular activity, and target molecules 6) .…”

Section: Underlying Mechanisms Of Gender Difference In Ascvd: Estrogementioning

confidence: 99%

SIRT1 and Gender Differences in Atherosclerotic Cardiovascular Disease

Shimabukuro

2020

JAT

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ERAAs for menopause treatment: Welcome the ‘designer estrogens’

Cited by 6 publications

References 50 publications

Medroxyprogesterone Acetate Prevention of Cervical Cancer through Progesterone Receptor in a Human Papillomavirus Transgenic Mouse Model

Medroxyprogesterone Acetate Prevention of Cervical Cancer through Progesterone Receptor in a Human Papillomavirus Transgenic Mouse Model

Postmenopausal Hormone Therapy—Local and Systemic: A Pharmacologic Perspective

SIRT1 and Gender Differences in Atherosclerotic Cardiovascular Disease

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