SERMs
•
12 gostaram•3,015 visualizações
it reflects cancer especially, focuses on breast cancer, treatment and the current problems related with the drugs; so we can focus on the new targets to treat the disease.
Recomendados
Mais conteúdo relacionado
Mais procurados
Mais procurados (20)
Semelhante a SERMs
Semelhante a SERMs (20)
Último
Último (20)
SERMs
- 1. Presented By Neha Dhiman M.Pharm Medicinal Chemistry 1st sem CUPB
- 2. 2 INTRODUCTION ROLE MOA BENEFITS DEMERITS NEW STRATEGY FOR BREAST CANCER FLOW OF PRESENTATION
- 3. SERM 3 Selective Estrogen Receptor Modulators. SERMs are the non steroidal compounds that are capable of binding Estrogen receptor and produces several responses , ranging from pure estrogenic agonist to anti-estrogenic activity depending upon the type of tissue involved.
- 4. Estrogen receptors are present in many cells in different tissues in our body. But each receptor is different in their structure. So breast cell estrogen receptors are different from bone cell estrogen receptors and both of those estrogen receptors are different from uterine estrogen receptors. 4 ERs 3OS8
- 5. 5 ERs ER-α ER-β Mammary glands breast, uterus, ovary, Prostate, bones, heart, intestine, adipose tissue and immune system.
- 6. 6 Action
- 7. 7 Selective As their name says, SERMs are "selective" – this means that a SERM that blocks estrogen's action in some tissues or can activate estrogen's action in other cells.
- 8. Selective estrogen receptor modulators (SERMs) are now being used as a treatment for Osteoporosis Breast cancer and Postmenopausal symptoms 8 Role
- 10. They are not safe for the women who are pregnant or breastfeeding. They are especially made for the women whose ovaries no longer produce estrogen i.e. for postmenopausal women. Safety 10
- 11. 11 Mechanism of Action (MOA)
- 12. 12 Osteoporosis Estrogens have been extensively used to prevent bone loss. They are also beneficial for the relief of menopausal symptoms. In postmenopausal women estrogen level decreases. SERMs became attractive in this case.
- 13. 13 Postmenopausal women SERM reduces bone resorption, increases bone mineral density and reduces the number and size of osteoclasts. Estrogen level Decreases Osteoclast Osteoblast Decrease Apoptosis Increase Apoptosis Bone resorption Bone formation
- 14. 14 SERMs in Breast Cancer ER SERM + COMPLEX No transcription No cellular proliferation
- 15. 15 MOA The cell doesn't receive estrogen's signals to grow and multiply If estrogen not binds to a breast cell Estrogen can't attach to the cell. SERMs binds the estrogen receptors in breast cells SERMs block the effects of estrogen in the breast tissue
- 16. 16Decreased cancer risk Increased cancer risk
- 17. Some SERMs e.g. Toremifene increased HDL-C and decreased triglycerides in postmenopausal breast cancer patients. 17 Cardiovascular System Estrogen SERMs Increases HDL-C and lower triglycerides Lowers LDL-C Decreases LDL-C in postmenopausal women
- 18. 18 Specific effects of Tamoxifen • Inhibits bone resorption and reduced bone lossEstrogen agonist in the bone • Increasing risk of blood clots • Increases hot flashes and leg crampsSERM and estrogen-like effect • With increased risk of uterine cancer similar to estrogen Estrogen agonist in the uterus • Reduces breast cancer riskEstrogen antagonist in the breast • Lowers LDL cholesterol and raises HDL cholesterolEstrogen agonist in the liver
- 19. 19 Tamoxifen Raloxifene Category A triphenylethylene A benzothiophene Breast Reduce cancer risk in pre and post menopausal women Reduce cancer risk in postmenopausal women Cholesterol Reduced LDL-C Reduced LDL-C In bones Increases bone density in postmenopausal women but reduction in fracture risk is limited Increased bone mineral density by 2%-3% and reduced the incidence of new vertebral fractures by 30% and 50%. In Uterus Partial estrogen agonist Increases endometrial thickness Neither act as agonist Nor increases endometrial thickness
- 20. 20 Benefits of SERM Tamoxifen and Raloxifene are the most commonly used SERM. Tamoxifen and Raloxifene acts as estrogen agonist in bone and liver. Tamoxifen is an estrogen agonist in uterus while raloxifen is an antagonist in the uterus. Tamoxifen and Raloxifene, both acts as estrogen antagonist in the breast.
- 21. 21 Specificity depends upon the coactivator and corepressor.
- 22. Thus, the key difference between these SERMs to be used for breast cancer is their endometrial safety. A new approach to reduce the breast cancer risk is the development of aromatase inhibitors. 22 New approach for breast cancer
- 23. . 23 SERM V/S AI Most of the studies comparing SERMs to Aromatase Inhibitors (AI). An aromatase inhibitor is the best type of hormonal therapy to start with for postmenopausal women. Especially for breast cancer. When treating early-stage, hormone- receptor-positive breast cancer, aromatase inhibitors have more benefits and fewer serious side effects than tamoxifen.
- 24. 24 MOA of AI
- 25. SERMs are used for the treatment of symptoms that occurs in the post menopausal women. Tamoxifen and Raloxifene are the most commonly used SERMs but they have some mild and severe side effects. For the early stage hormone dependent positive breast cancer its better to use aromatase inhibitors to inhibit the overexpression of estrogen receptor. 25 Conclusion
- 26. 26
Notas do Editor
- Selective Estrogen Receptor Modulators Adolfo Diez-Perez (SERMS) Autonomous University of Barcelona, Department of Internal Medicine, Hospital del Mar-URFOA-IMIM, Barcelona, Spain.