Alestramustine: Difference between revisions

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{{Short description|A chemotherapeutic agent}}
{{Short description|A chemotherapeutic agent used in cancer treatment}}
{{Drugbox
{{Drugbox
| verifiedfields = changed
| verifiedfields = changed
| verifiedrevid = 477002123
| verifiedrevid = 477002123
| IUPAC_name = (2''R'')-2-[(2''S'')-3-(4-aminophenyl)-2-hydroxypropoxy]-2-oxoethyl 17-((2''R'')-3-hydroxy-2-(hydroxymethyl)-2-methylpropyl)-3-oxo-13-methyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-yl carbonate
| image = Alestramustine.svg
| image = Alestramustine.svg
| image2 =
}}
}}


'''Alestramustine''' is a [[chemotherapy|chemotherapeutic]] agent that combines the properties of an [[alkylating agent]] and an [[estrogen]]. It is used in the treatment of [[prostate cancer]].
'''Alestramustine''' is a [[chemotherapeutic agent]] that combines the properties of an [[alkylating agent]] and an [[estrogen]]. It is primarily used in the treatment of [[prostate cancer]].


==Mechanism of action==
==Mechanism of Action==
Alestramustine is a [[prodrug]] that is metabolized into two active components: [[estradiol]] and [[nor-nitrogen mustard]]. The estradiol component allows the drug to target [[hormone-sensitive cancer|hormone-sensitive]] tissues, such as the prostate, while the nor-nitrogen mustard acts as an alkylating agent, interfering with [[DNA replication]] and [[cell division]].
Alestramustine is a [[prodrug]] that is metabolized into two active components: [[estradiol]] and [[normustine]]. The estradiol component acts as an estrogen, which can help in reducing the levels of [[testosterone]], a hormone that can promote the growth of prostate cancer cells. The normustine component is an alkylating agent that works by damaging the DNA of cancer cells, thereby inhibiting their ability to divide and grow.


==Pharmacokinetics==
==Pharmacokinetics==
Upon administration, alestramustine is rapidly absorbed and converted into its active metabolites. The drug's distribution is influenced by its lipophilic nature, allowing it to penetrate [[cell membranes]] effectively. The metabolism of alestramustine primarily occurs in the [[liver]], and its metabolites are excreted via the [[urinary system]].
Upon administration, alestramustine is absorbed and metabolized in the body. The estradiol component is responsible for the hormonal effects, while the normustine component provides the cytotoxic effects. The drug is designed to target cancer cells more effectively by utilizing the affinity of estradiol for estrogen receptors, which are often overexpressed in certain types of cancer cells.


==Clinical use==
==Clinical Use==
Alestramustine is primarily used in the treatment of [[advanced prostate cancer]]. It is particularly beneficial in cases where the cancer has become resistant to conventional [[hormone therapy]]. The drug's dual mechanism of action allows it to target cancer cells more effectively than traditional therapies.
Alestramustine is used in the treatment of [[hormone-sensitive prostate cancer]]. It is particularly useful in cases where other forms of hormone therapy have failed. The combination of hormonal and cytotoxic effects makes it a valuable option in the management of advanced prostate cancer.


==Side effects==
==Side Effects==
Common side effects of alestramustine include [[nausea]], [[vomiting]], and [[fatigue]]. Due to its estrogenic component, patients may also experience [[gynecomastia]] and [[fluid retention]]. Long-term use can lead to [[cardiovascular complications]] and [[thromboembolic events]].
The use of alestramustine can lead to several side effects, which are typical of both estrogenic and alkylating agents. Common side effects include:
* [[Gynecomastia]]
* [[Nausea]]
* [[Vomiting]]
* [[Fatigue]]
* [[Hot flashes]]
 
More serious side effects can include:
* [[Thromboembolic events]]
* [[Cardiovascular complications]]
* [[Bone marrow suppression]]
 
==Administration==
Alestramustine is typically administered orally. The dosage and treatment regimen depend on the specific needs of the patient and the stage of the cancer.


==Related pages==
==Related pages==
* [[Prostate cancer]]
* [[Prostate cancer]]
* [[Chemotherapy]]
* [[Chemotherapy]]
* [[Hormone therapy (oncology)]]
* [[Alkylating agent]]
* [[Alkylating agent]]
* [[Hormone therapy]]
==Gallery==
<gallery>
File:Alestramustine.svg|Chemical structure of Alestramustine
</gallery>


[[Category:Chemotherapeutic agents]]
[[Category:Chemotherapeutic agents]]
[[Category:Prodrugs]]
[[Category:Prodrugs]]
[[Category:Estrogens]]
[[Category:Estrogens]]
<gallery>
File:Alestramustine.svg|Alestramustine
</gallery>

Latest revision as of 00:40, 20 February 2025

A chemotherapeutic agent used in cancer treatment


Alestramustine
File:Alestramustine.svg
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Alestramustine is a chemotherapeutic agent that combines the properties of an alkylating agent and an estrogen. It is primarily used in the treatment of prostate cancer.

Mechanism of Action[edit]

Alestramustine is a prodrug that is metabolized into two active components: estradiol and normustine. The estradiol component acts as an estrogen, which can help in reducing the levels of testosterone, a hormone that can promote the growth of prostate cancer cells. The normustine component is an alkylating agent that works by damaging the DNA of cancer cells, thereby inhibiting their ability to divide and grow.

Pharmacokinetics[edit]

Upon administration, alestramustine is absorbed and metabolized in the body. The estradiol component is responsible for the hormonal effects, while the normustine component provides the cytotoxic effects. The drug is designed to target cancer cells more effectively by utilizing the affinity of estradiol for estrogen receptors, which are often overexpressed in certain types of cancer cells.

Clinical Use[edit]

Alestramustine is used in the treatment of hormone-sensitive prostate cancer. It is particularly useful in cases where other forms of hormone therapy have failed. The combination of hormonal and cytotoxic effects makes it a valuable option in the management of advanced prostate cancer.

Side Effects[edit]

The use of alestramustine can lead to several side effects, which are typical of both estrogenic and alkylating agents. Common side effects include:

More serious side effects can include:

Administration[edit]

Alestramustine is typically administered orally. The dosage and treatment regimen depend on the specific needs of the patient and the stage of the cancer.

Related pages[edit]