Miproxifene: Difference between revisions

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{{Short description|Selective estrogen receptor modulator}}
== Miproxifene ==
{{Drugbox
| verifiedfields = changed
| verifiedrevid = 477002123
| IUPAC_name = 1-[4-[(Z)-1,2-diphenylbut-1-enyl]phenoxy]-3-(dimethylamino)propan-2-ol
| image = Miproxifene.png
| width = 200px
| CAS_number = 129912-70-1
| PubChem = 3033965
| ChemSpiderID = 2298535
| UNII = 0X9U0Q2R8K
| KEGG = D05082
| ChEMBL = 2104010
| C=25
| H=29
| N=1
| O=2
| smiles = CC/C(=C(/c1ccc(OCC(CN(C)C)O)cc1)\c2ccccc2)c3ccccc3
}}


'''Miproxifene''' is a [[selective estrogen receptor modulator]] (SERM) that has been studied for its potential use in the treatment of [[breast cancer]]. It is a derivative of [[tamoxifen]], a well-known SERM used in the treatment and prevention of breast cancer.
[[File:Chemical_structure_of_Miproxifene.png|Chemical structure of Miproxifene|thumb|right]]


==Mechanism of Action==
'''Miproxifene''' is a [[selective estrogen receptor modulator]] (SERM) that was developed for the treatment of [[breast cancer]]. It is a nonsteroidal compound that exhibits both estrogenic and antiestrogenic properties depending on the target tissue. Miproxifene is structurally related to other SERMs such as [[tamoxifen]] and [[raloxifene]].
Miproxifene functions by binding to [[estrogen receptors]] in the body, particularly those found in breast tissue. By doing so, it can block the effects of estrogen, a hormone that can promote the growth of certain types of breast cancer cells. This mechanism is similar to that of other SERMs, which can act as estrogen antagonists in some tissues while acting as agonists in others.


==Pharmacology==
== Mechanism of Action ==
Miproxifene is designed to have a more favorable profile compared to tamoxifen, with the aim of reducing side effects and improving efficacy. The drug's structure allows it to selectively modulate estrogen receptor activity, potentially offering benefits in terms of reduced risk of [[endometrial cancer]] and other estrogen-related side effects.


==Clinical Development==
Miproxifene functions by binding to [[estrogen receptors]] (ERs) in various tissues. It acts as an [[estrogen receptor antagonist]] in breast tissue, which helps to inhibit the proliferation of [[estrogen receptor-positive breast cancer]] cells. In other tissues, such as bone and the cardiovascular system, miproxifene may exhibit partial agonist activity, which can be beneficial in maintaining bone density and cardiovascular health.
Miproxifene has been the subject of various clinical trials to assess its safety and efficacy in the treatment of breast cancer. These studies have focused on its ability to reduce tumor size and prevent the progression of the disease. However, as of the latest updates, miproxifene has not been approved for clinical use and remains an investigational drug.


==Potential Benefits==
== Development and Clinical Trials ==
The potential benefits of miproxifene include its ability to act as an effective anti-estrogen agent in breast tissue while minimizing adverse effects in other tissues. This selectivity could make it a valuable option for patients who are at risk of developing breast cancer or who have already been diagnosed with the disease.


==Side Effects==
Miproxifene was developed as a potential therapeutic agent for breast cancer due to its ability to selectively modulate estrogen receptor activity. Clinical trials were conducted to evaluate its efficacy and safety profile. However, despite promising preclinical data, miproxifene did not advance to market approval due to various factors, including competition from other more established SERMs and the results of clinical trials.
As with other SERMs, miproxifene may cause side effects, although its specific profile is still under investigation. Common side effects associated with SERMs include hot flashes, vaginal discharge, and an increased risk of thromboembolic events. The development of miproxifene aims to mitigate these risks while providing effective treatment.
 
== Pharmacokinetics ==
 
The pharmacokinetic profile of miproxifene includes its absorption, distribution, metabolism, and excretion. Miproxifene is administered orally and undergoes hepatic metabolism. The metabolites of miproxifene contribute to its pharmacological activity, similar to other SERMs.
 
== Potential Applications ==
 
While primarily investigated for breast cancer treatment, miproxifene's SERM properties suggest potential applications in other conditions influenced by estrogen receptor modulation. These may include [[osteoporosis]] and [[cardiovascular disease]], where estrogen plays a protective role.
 
== Related Pages ==


==Related Pages==
* [[Tamoxifen]]
* [[Selective estrogen receptor modulator]]
* [[Selective estrogen receptor modulator]]
* [[Breast cancer]]
* [[Breast cancer]]
* [[Tamoxifen]]
* [[Raloxifene]]
* [[Estrogen receptor]]
* [[Estrogen receptor]]


[[Category:Selective estrogen receptor modulators]]
[[Category:Selective estrogen receptor modulators]]
[[Category:Experimental cancer drugs]]
[[Category:Breast cancer treatments]]

Revision as of 11:20, 23 March 2025

Miproxifene

File:Chemical structure of Miproxifene.png
Chemical structure of Miproxifene

Miproxifene is a selective estrogen receptor modulator (SERM) that was developed for the treatment of breast cancer. It is a nonsteroidal compound that exhibits both estrogenic and antiestrogenic properties depending on the target tissue. Miproxifene is structurally related to other SERMs such as tamoxifen and raloxifene.

Mechanism of Action

Miproxifene functions by binding to estrogen receptors (ERs) in various tissues. It acts as an estrogen receptor antagonist in breast tissue, which helps to inhibit the proliferation of estrogen receptor-positive breast cancer cells. In other tissues, such as bone and the cardiovascular system, miproxifene may exhibit partial agonist activity, which can be beneficial in maintaining bone density and cardiovascular health.

Development and Clinical Trials

Miproxifene was developed as a potential therapeutic agent for breast cancer due to its ability to selectively modulate estrogen receptor activity. Clinical trials were conducted to evaluate its efficacy and safety profile. However, despite promising preclinical data, miproxifene did not advance to market approval due to various factors, including competition from other more established SERMs and the results of clinical trials.

Pharmacokinetics

The pharmacokinetic profile of miproxifene includes its absorption, distribution, metabolism, and excretion. Miproxifene is administered orally and undergoes hepatic metabolism. The metabolites of miproxifene contribute to its pharmacological activity, similar to other SERMs.

Potential Applications

While primarily investigated for breast cancer treatment, miproxifene's SERM properties suggest potential applications in other conditions influenced by estrogen receptor modulation. These may include osteoporosis and cardiovascular disease, where estrogen plays a protective role.

Related Pages

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