testolactone

Testolactone
Systematic (IUPAC) name
	(4aS,4bR,10aR,10bS,12aS)-10a,12a-Dimethyl-3,4,4a,5,6,10a,10b,11,12,12a-decahydro-2H-naphtho[2,1-f]chromene-2,8(4bH)-dione
Clinical data
AHFS/Drugs.com	Consumer Drug Information
Pregnancy; category	US: C (Risk not ruled out); ;
Routes of; administration	Oral
Pharmacokinetic data
Protein binding	~85%
Metabolism	Hepatic
Excretion	Renal
Identifiers
CAS Number	968-93-4
ATC code	None
PubChem	CID: 13769
IUPHAR/BPS	7303
DrugBank	DB00894
ChemSpider	13172
UNII	6J9BLA949Q
KEGG	D00153
ChEBI	CHEBI:9460
ChEMBL	CHEMBL1571
Chemical data
Formula	C19H24O3
Molecular mass	300.39 g/mol
	SMILES CC12CCC3C(C1CCC(=O)O2)CCC4=CC(=O)C=CC34C ;
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Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/01/04 15:01:02」(JST)

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Testolactone (brand name Teslac) is an antineoplastic agent that is a derivative of progesterone and is used to treat advanced stage breast cancer.^[1]

It is nonselective.^[2]

Pharmacology

Testolactone is a synthetic antineoplastic agent that is structurally distinct from the androgen steroid nucleus in possessing a six-membered lactone ring in place of the usual five-membered carbocyclic D-ring. Despite some similarity to testosterone, testolactone has no in vivo androgenic effect. No other hormonal effects have been reported in clinical studies in patients receiving testolactone.^[3]

Mechanism of action

The principal action of testolactone is reported to be inhibition of steroid aromatase activity and the reduction in estrone synthesis that follows. Androstenedione, a 19-carbon steroid hormone produced in the adrenal glands and the gonads, is where estrone synthesis originates and is the source of estrogen in postmenopausal women. In vitro studies report that the aromatase inhibition may be noncompetitive and irreversible, and could possibly account for the persistence of this drug's effect on estrogen synthesis after drug withdrawal.^[3]

Uses

This drug is mainly used for treating various types of breast cancer in women who have been through menopause or whose ovaries no longer function.^[4] It works by blocking the production of estrogen, which helps prevent the growth of breast cancers that are activated by estrogen. It may also prevent tumor cells from being activated by other hormones.^[4] It also has been used to postpone precocious puberty because of its ability to block estrogen production.^[5]

Side effects

The most common side effects include:

Abnormal skin sensations
Aches of the legs and arms
General body discomfort
Hair loss
Loss of appetite
Nausea
Redness of the tongue
Vomiting

References

^ Testolactone at DrugBank.ca
^ Dunkel L (July 2006). "Use of aromatase inhibitors to increase final height". Mol. Cell. Endocrinol. 254-255: 207–16. doi:10.1016/j.mce.2006.04.031. PMID 16766117.
^ ^a ^b DrugBank: DB00894 (Testolactone)
^ ^a ^b Testolactone facts and comparisons at Drugs.com
^ Carel, J.-C.; Lahlou, N; Roger, M; Chaussain, JL (2004). "Precocious puberty and statural growth". Human Reproduction Update 10 (2): 135–47. doi:10.1093/humupd/dmh012. PMID 15073143.

UpToDate Contents

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1. 思春期早発症の治療 treatment of precocious puberty
2. デスモイド腫瘍：全身療法 desmoid tumors systemic therapy
3. 幼児および小児における 21-ヒドロキシラーゼ欠損症による典型的な先天性副腎皮質過形成の治療 treatment of classic congenital adrenal hyperplasia due to 21 hydroxylase deficiency in infants and children
4. アスリートにおけるアンドロゲンおよびその他のホルモンの使用 use of androgens and other hormones by athletes
5. 女性化乳房のマネージメント management of gynecomastia

English Journal

NGF induces adult stem Leydig cells to proliferate and differentiate during Leydig cell regeneration.

Zhang L1, Wang H, Yang Y, Liu H, Zhang Q, Xiang Q, Ge R, Su Z, Huang Y.
Biochemical and biophysical research communications.Biochem Biophys Res Commun.2013 Jun 28;436(2):300-5. doi: 10.1016/j.bbrc.2013.05.098. Epub 2013 Jun 4.
Nerve growth factor (NGF) has been reported to be involved in male reproductive physiology. However, few reports have described the activity of NGF during Leydig cell development. The objective of the present study was to examine the role of NGF during stem-Leydig-cell (SLC) regeneration. We investi
PMID 23743199

Aromatase inhibitors for male infertility.

Schlegel PN.
Fertility and sterility.Fertil Steril.2012 Dec;98(6):1359-62. doi: 10.1016/j.fertnstert.2012.10.023. Epub 2012 Oct 25.
Some men with severely defective sperm production commonly have excess aromatase activity, reflected by low serum testosterone and relatively elevated estradiol levels. Aromatase inhibitors can increase endogenous testosterone production and serum testosterone levels. Treatment of infertile males wi
PMID 23103016

Increased medial temporal lobe and striatal grey-matter volume in a rare disorder of androgen excess: a voxel-based morphometry (VBM) study.

Mueller SC1, Merke DP, Leschek EW, Fromm S, VanRyzin C, Ernst M.
The international journal of neuropsychopharmacology / official scientific journal of the Collegium Internationale Neuropsychopharmacologicum (CINP).Int J Neuropsychopharmacol.2011 May;14(4):445-57. doi: 10.1017/S1461145710001136. Epub 2010 Sep 22.
Major questions remain about how sex hormones influence human brain development and cognition. Studies in humans and animals suggest a strong impact of androgen on the structure and function of the medial temporal lobe (MTL) and striatum. Using voxel-based morphometry (DARTEL), we compared MTL and s
PMID 20860880

Japanese Journal

Familial Male-limited Precocious Pubertyに対するスピロノラクトン : テストラクトン併用療法の短期効果

森谷直樹
ホルモンと臨牀 44(9), 23-27, 1996-09-01
NAID 10007093237

高 (estradiol/testosterone) 比の乏精子症に対するtestolactone (aromatase inhibitor) の治療効果

伊藤直樹,熊本悦明,丸田浩,塚本泰司,高木良雄,三熊直人,南部明民,立木仁
日本泌尿器科學會雜誌 82(2), 204-209, 1991-02-20
… 男子不妊症9例にaromatase inhibitorであるtestolactone (Teslac[○!R]) 1.0g/日3ヵ月投与を行ったところ4例で精子数の改善 (治療前精子数に比し10x10^6/ml以上の増加) を認めた. … 血中sexhormone binding globulin (SHBG) を測定したところ, testolactone投与後でSHBGは低下しており血中遊離testosteroneの上昇はこれによるものと考えられた. …
NAID 110003093531

Testolactone, sulindac, warfarin, and vitamin K1 for unresectable desmoid tumors

WADDEL W. R.
Am J Surg 161, 416-421, 1991
NAID 30009813865

Related Pictures

[1] Testolactone at DrugBank.ca

[pmid16766117-2] Dunkel L (July 2006). "Use of aromatase inhibitors to increase final height". Mol. Cell. Endocrinol. 254-255: 207–16. doi:10.1016/j.mce.2006.04.031. PMID 16766117.

[drugbank-3] DrugBank: DB00894 (Testolactone)

[comparison-4] Testolactone facts and comparisons at Drugs.com

[5] Carel, J.-C.; Lahlou, N; Roger, M; Chaussain, JL (2004). "Precocious puberty and statural growth". Human Reproduction Update 10 (2): 135–47. doi:10.1093/humupd/dmh012. PMID 15073143.

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