Mepitiostane - Revision history

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	~~'''Mepitiostane''' is an [[ethylestrenol]] ether and a synthetic, orally active [[androgen]] and [[~~anabolic steroid]] (~~AAS~~) ~~that is used in the treatment of~~ [~~[breast cancer]]. It is marketed under the brand name Thioderon. Mepitiostane is~~ a ~~prodrug of [[ethylestrenol]~~], ~~meaning it is metabolically converted into ethylestrenol within the body~~. ~~This conversion is necessary for its activity, as ethylestrenol is the active form of the drug~~.		{{Short description\|Synthetic anabolic-androgenic steroid}}
			{{Drugbox
			\| verifiedfields = changed
			\| verifiedrevid = 477318123
			\| IUPAC_name = (2S,3aS,3bR,9aR,9bS,11aS)-2,3a,6,9,9-pentamethyl-2,3,3a,3b,4,5,6,7,8,9,9a,9b,10,11,11a-tetradecahydro-1H-cyclopenta[a]phenanthrene-2,7-diol
			\| image = Mepitiostane.svg
			\| image2 = Mepitiostane.svg
			\| width = 200
			\| alt = Mepitiostane
			}}

	~~==Medical Uses==~~		'''Mepitiostane''' is a synthetic [[anabolic-androgenic steroid]] (AAS) and a derivative of [[dihydrotestosterone]] (DHT). It is known for its use in the treatment of [[breast cancer]] in women. Mepitiostane is the 17α-methylated derivative of [[epitiostanol]], which is also an AAS used for similar purposes.
	Mepitiostane is ~~primarily used~~ in the treatment of [[breast cancer]] in women. ~~Its effectiveness in this application~~ is ~~attributed to~~ its ~~ability~~ to ~~reduce~~ [[~~estrogen~~]] ~~levels in the body~~, which ~~can help~~ to ~~slow~~ the ~~growth of estrogen~~-~~sensitive cancer cells~~.
			==Chemical Structure and Properties==
			[[File:Mepitiostane.svg\|thumb\|right\|Chemical structure of Mepitiostane]]
			Mepitiostane is chemically characterized by the presence of a 17α-methyl group, which distinguishes it from its parent compound, epitiostanol. This modification enhances its oral bioavailability, making it more effective when administered orally compared to non-17α-alkylated steroids.

			The compound is a [[17α-alkylated anabolic steroid]], which means it has been modified to resist breakdown by the liver, allowing it to be effective when taken orally. However, this modification also increases the potential for [[hepatotoxicity]], a common concern with 17α-alkylated steroids.

	==Pharmacology==		==Pharmacology==
	~~===Mechanism of Action===~~		Mepitiostane functions primarily as an [[androgen receptor]] agonist. It binds to androgen receptors in target tissues, promoting anabolic effects such as increased protein synthesis and muscle growth. Its androgenic effects are relatively mild compared to its anabolic effects, which makes it suitable for use in women, particularly in the treatment of breast cancer.
	As an androgen ~~and anabolic steroid, mepitiostane's mechanism of action involves its conversion~~ to ~~ethylestrenol~~, ~~which then exerts~~ anabolic and androgenic effects~~. These~~ effects ~~are mediated through the activation of the [[androgen receptor]] (AR)~~, ~~leading to various physiological and pharmacological outcomes. In~~ the ~~context~~ of breast cancer~~, the reduction in estrogen levels is a key therapeutic effect~~.

	==~~=Pharmacokinetics=~~==		==Medical Uses==
	Mepitiostane ~~is administered orally. Upon ingestion, it is converted into ethylestrenol,~~ its ~~active metabolite. The pharmacokinetics~~ of ~~mepitiostane~~, ~~including its absorption~~, ~~distribution, metabolism, and excretion, are closely tied to those~~ of ~~ethylestrenol~~.		Mepitiostane has been used in the treatment of [[breast cancer]] due to its ability to antagonize the effects of estrogen, a hormone that can promote the growth of certain types of breast cancer cells. By binding to androgen receptors, mepitiostane can inhibit the proliferation of these cancer cells.

	==~~Adverse~~ Effects==		==Side Effects==
	~~Like~~ other ~~androgens and~~ anabolic steroids, mepitiostane can cause a range of ~~adverse~~ effects. These may include virilization in women, ~~hepatotoxicity~~, ~~alterations in lipid profiles~~, and ~~changes in libido~~. ~~The severity and occurrence of these side effects can vary based on the dosage and duration~~ of ~~treatment~~.		As with other anabolic steroids, mepitiostane can cause a range of side effects. These may include [[virilization]] in women, such as deepening of the voice, increased body hair, and other masculinizing effects. Due to its 17α-alkylation, there is also a risk of liver damage with prolonged use.

	==~~Contraindications~~==		==Related Compounds==
	Mepitiostane is ~~contraindicated in patients with known hypersensitivity~~ to ~~the drug or~~ its ~~components~~. ~~It is also contraindicated in individuals with prostate cancer, as androgens can accelerate the growth~~ of ~~prostate cancer cells. Pregnant~~ and ~~breastfeeding women should avoid using~~ mepitiostane ~~due to potential risks to the fetus or infant~~.		Mepitiostane is closely related to [[epitiostanol]], which is its non-17α-alkylated counterpart. Both compounds share similar mechanisms of action and therapeutic uses, but mepitiostane's oral bioavailability makes it more convenient for certain treatment regimens.

	==~~See Also~~==		==Related Pages==
	* [[Anabolic steroid]]		* [[Anabolic steroid]]
			* [[Dihydrotestosterone]]
	* [[Breast cancer]]		* [[Breast cancer]]
	* [[Androgen receptor]]		* [[Androgen receptor]]

	~~==References==~~		[[Category:Androgens and anabolic steroids]]
	~~<references/>~~		[[Category:Breast cancer treatments]]
			[[Category:17α-Alkylated anabolic steroids]]
	[[Category:~~Anabolic~~ steroids]]
	[[Category:~~Prodrugs~~]]
	[[Category:~~Breast cancer treatment~~]]

	~~{{Pharmacology-stub}}~~
	~~{{Medicine-stub}}~~
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	~~File:Mepitiostane.svg\|Mepitiostane~~
	~~</gallery>~~
	~~<gallery>~~
	~~File:Mepitiostane.svg\|Mepitiostane~~
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New page

'''Mepitiostane''' is an [[ethylestrenol]] ether and a synthetic, orally active [[androgen]] and [[anabolic steroid]] (AAS) that is used in the treatment of [[breast cancer]]. It is marketed under the brand name Thioderon. Mepitiostane is a prodrug of [[ethylestrenol]], meaning it is metabolically converted into ethylestrenol within the body. This conversion is necessary for its activity, as ethylestrenol is the active form of the drug.

==Medical Uses==
Mepitiostane is primarily used in the treatment of [[breast cancer]] in women. Its effectiveness in this application is attributed to its ability to reduce [[estrogen]] levels in the body, which can help to slow the growth of estrogen-sensitive cancer cells.

==Pharmacology==
===Mechanism of Action===
As an androgen and anabolic steroid, mepitiostane's mechanism of action involves its conversion to ethylestrenol, which then exerts anabolic and androgenic effects. These effects are mediated through the activation of the [[androgen receptor]] (AR), leading to various physiological and pharmacological outcomes. In the context of breast cancer, the reduction in estrogen levels is a key therapeutic effect.

===Pharmacokinetics===
Mepitiostane is administered orally. Upon ingestion, it is converted into ethylestrenol, its active metabolite. The pharmacokinetics of mepitiostane, including its absorption, distribution, metabolism, and excretion, are closely tied to those of ethylestrenol.

==Adverse Effects==
Like other androgens and anabolic steroids, mepitiostane can cause a range of adverse effects. These may include virilization in women, hepatotoxicity, alterations in lipid profiles, and changes in libido. The severity and occurrence of these side effects can vary based on the dosage and duration of treatment.

==Contraindications==
Mepitiostane is contraindicated in patients with known hypersensitivity to the drug or its components. It is also contraindicated in individuals with prostate cancer, as androgens can accelerate the growth of prostate cancer cells. Pregnant and breastfeeding women should avoid using mepitiostane due to potential risks to the fetus or infant.

==See Also==
* [[Anabolic steroid]]
* [[Breast cancer]]
* [[Androgen receptor]]

==References==
<references/>

[[Category:Anabolic steroids]]
[[Category:Prodrugs]]
[[Category:Breast cancer treatment]]

{{Pharmacology-stub}}
{{Medicine-stub}}