Home : DrugWatch : Evista : Wikipedia : Selective estrogen receptor modulator

Wikipedia - Selective estrogen receptor modulator

These bottles and pills are of the drugs tamoxifen and raloxifene that are being used in a breast cancer prevention trial (STAR).

Selective Estrogen Receptor Modulators (SERMs) are a class of compounds that act on the estrogen receptor.[1] A characteristic that distinguishes these substances from pure receptor agonists and antagonists is that their action is different in various tissues, thereby granting the possibility to selectively inhibit or stimulate estrogen-like action in various tissues. Phytoserms are scientifically accepted SERMs from a botanical source.

Contents

[edit] Members and uses

SERMs are used dependent on their pattern of action in various tissues:

Name Uses Effects/location
clomifene used in anovulation antagonist at hypothalamus
femarelle managing menopause symptoms, osteoporosis agonist at brain and bone
ormeloxifene contraception agonist at bone; antagonist at uterus and breast
raloxifene osteoporosis, breast cancer agonist at bone; antagonist at uterus and breast
tamoxifen breast cancer antagonist at breast; agonist at uterus
toremifene breast cancer

Other members include afimoxifene, arzoxifene, bazedoxifene, and lasofoxifene.

Some SERMs may be good replacements for hormone replacement therapy (HRT), which had been commonly used to treat menopause symptoms until the publication of wide scale studies showing that HRT slightly increases the risk of breast cancer [2] and thrombosis.[3] Some of the above agents still have significant side-effects which contraindicate widespread use.

SERMs are also commonly used during PCT or Post Cycle Therapy after the use of anabolic steroids, or during a steroid cycle in case of the sudden onset of estrogenic symptoms. Bodybuilders who take hormonal supplements can experience gynecomastia and similar symptoms because the body metabolizes some steroids into estrogen. This increase in estrogen can occur during or after a steroid cycle, so responsible body builders will usually cycle a SERM after a steroid cycle to ensure that their body is not flooded with excess estrogen. They also often keep a SERM on hand in case of emergency.

[edit] Mechanism of action

Estrogenic compounds span a spectrum of activity ranging from:

  • full agonists (agonistic in all tissues) such as the natural endogenous hormone estrogen
  • mixed agonists/antagonistics (agonistic in some tissues while antagonist in others) such as tamoxifen (a SERM)
  • pure antagonists (antagonistic in all tissues) such as fulvestrant (ICI-182780).

The mechanism of mixed agonism/antagonism may differ depending on the chemical structure of the SERM, but for at least for some SERMs, it appears to be related to (1) the ratio of co-activator to co-repressor proteins in different cell types and (2) the conformation of the estrogen receptor induced by drug binding which in turn determines how strongly the drug/receptor complex recruits co-activators (resulting in an agonist response) relative to co-repressors (resulting in antagonism). For example, the prototypical SERM tamoxifen acts as an antagonist in breast and conversely an agonist in uterus. The concentration of steroid receptor co-activator 1 (SRC-1; NCOA1) is higher in uterus than in breast, therefore SERMs such as tamoxifen are more agonistic in uterus than in breast. In contrast, raloxifene behaves as an antagonist in both tissues. It appears that raloxifene more strongly recruits co-repressor proteins and consequently is still an antagonist in the uterus despite the higher concentration of co-activators relative to co-repressors.[4][5]

[edit] Actions

The actions of SERMs on various tissues:

[edit] References

  1. ^ Riggs BL, Hartmann LC (2003). "Selective estrogen-receptor modulators -- mechanisms of action and application to clinical practice". N Engl J Med 348 (7): 618–29. doi:10.1056/NEJMc030651. PMID 12584371. 
  2. ^ Reeves GK, Beral V, Green J, Gathani T, Bull D (November 2006). "Hormonal therapy for menopause and breast-cancer risk by histological type: a cohort study and meta-analysis". Lancet Oncol. 7 (11): 910–8. doi:10.1016/S1470-2045(06)70911-1. PMID 17081916. 
  3. ^ Rossouw JE, Anderson GL, Prentice RL, LaCroix AZ, Kooperberg C, Stefanick ML, Jackson RD, Beresford SA, Howard BV, Johnson KC, Kotchen JM, Ockene J; Writing Group for the Women's Health Initiative Investigators (July 2002). "Risks and benefits of estrogen plus progestin in healthy postmenopausal women: principal results From the Women's Health Initiative randomized controlled trial". JAMA 288 (3): 321–33. doi:10.1001/jama.288.3.321. PMID 12117397. http://jama.ama-assn.org/cgi/pmidlookup?view=long&pmid=12117397. 
  4. ^ Shang Y, Brown M (2002). "Molecular determinants for the tissue specificity of SERMs". Science 295 (5564): 2465–8. doi:10.1126/science.1068537. PMID 11923541. 
  5. ^ Smith CL, O'Malley BW (2004). "Coregulator function: a key to understanding tissue specificity of selective receptor modulators". Endocr Rev 25 (1): 45–71. doi:10.1210/er.2003-0023. PMID 14769827. 

[edit] See also

[edit] External links

v • d • e
Estrogens and progestogens (G03C-D)
Progestogens/
progestins
(progesterone)
Agonist
Other/
ungrouped
Antiprogestogen/
SPRM
Estrogens
Agonist
#WHO-EM. ‡Withdrawn from market. CLINICAL TRIALS: †Phase III. §Never to phase III
v • d • e
Receptor antagonists: hormone antagonists
Hypothalamic/pituitary axes
Eicosanoid
Other
Retrieved from "http://en.wikipedia.org/wiki/Selective_estrogen_receptor_modulator"

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Selective estrogen receptor modulator".

Need An Evista Attorney?

First Name Last Name Email Address State
Has Your Health Been Negatively Affected?

Please Describe the Injury

Your Friend's Email Address

Your Email Address

Type a Message (optional)


Looking for an Evista attorney in District of Columbia? Get in touch with one of our Evista attorneys in District of Columbia now.

 

Close (x)

Looking for an Attorney?


Please type your question:

Close (x)

logo Find Legal Help for Your Evista Case - Submit Your Information Below

Do you need legal assistance with your Evista case?
LegalView may be able to help.


Submit your information below for a free, no-cost evaluation.

We'll submit your information to one of our partner firms.
LegalView's partners represent clients throughout the United States, for a very wide range of legal issues. Submit your information now, to see if one of LegalView's partners can help!

* Indicates Required Fields

First name *
Last name *
Email Address *
Phone Number *
()  -

State *
Legal Issue * DrugWatch: Evista Change
Was There an Injury?
Please Describe The Injury

DISCLAIMER and STATEMENT OF NON-CONFIDENTIALITY

By submitting this form, you agree that completing the above is not intended to create an attorney-client relationship.

Disclosure

Legal WebTV Network LLC, LegalView.com, and LegalWebMedia.com are group advertising sponsored by the attorneys identified here. It is not a lawyer referral service. If you submit information on this website [more...]

Legal WebTV Network LLC, LegalView.com, and LegalWebMedia.com are group advertising sponsored by the attorneys identified here. It is not a lawyer referral service. If you submit information on this website, LegalWebMedia.com will submit your information to the law firms that pay for this group advertising and to respond to your requests for information concerning legal services in their assigned local areas. If there is no sponsoring firm in your state, your inquiry will be submitted to one of the sponsoring law firms on a predetermined, rotating basis. If the sponsoring law firm accepts your case, it will associate with licensed attorneys practicing in your state, if required; the sponsoring law firm may also contact other law firms to see if they may be able to assist.

The information provided by the LegalView.com and LegalWebMedia.com websites is for advertising and informational purposes and should not be considered as legal advice from the sponsoring attorneys. The websites contain general information and may not reflect current legal developments, verdicts, or settlements. LegalView.com contains information created by others or supplied through open forums; the sponsoring law firms are not responsible for the accuracy of this information. Any person viewing or receiving information from these websites should not act or refrain from acting on the basis of any such information without first seeking appropriate legal advice from an attorney in your area. Legal WebTV Network, LLC expressly disclaims any liability with respect to actions taken or not taken by the recipient based on any or all of the information or contents contained in these websites.

Any information sent to Legal WebTV Network LLC through this website is done using standard Web encryption techology. LegalView.com will exercise all reasonable care, within technological limits, to protect the confidentiality of any information submitted via Internet e-mail or through this website. By accessing this website, you may be seeking an attorney to represent you or legal advice. However, none of the sponsoring attorneys represent you yet.

The choice of a lawyer is an important decision and should not be based solely upon advertisements.

Any transmission of information, whether via Internet e-mail or through the website, is solely for evaluation purposes by the sponsoring law firms and their associates. The transmission of any information to any attorney sponsoring advertising on LegalView.com or LegalWebMedia.com does not create an attorney-client relationship between the sender and any recipient. An attorney-client relationship can only be created by a written, signed-fee agreement entered into with an attorney. The sponsoring attorneys will treat your information as a confidential communication for the purpose of obtaining legal services or legal advice.

For more information about the sponsoring law firms, please click here.
This form is secure and encrypted. More information about secure forms and your privacy here.