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レトロゾール

レトロゾール 化学構造式
112809-51-5
CAS番号.
112809-51-5
化学名:
レトロゾール
别名:
4,4'-[(1H-1,2,4-トリアゾール-1-イル)メチレン]ジベンゾニトリル;フェマラ;レトロゾール;フェマーラ;4,4'-[(1H-1,2,4-トリアゾール-1-イル)メチレン]ビスベンゾニトリル;4,4'-(1H-1,2,4-トリアゾール-1-イルメチレン)ビスベンゾニトリル;1-ビス(4-シアノフェニル)メチル-1,2,4-トリアゾール;4,4'-(1,2,4-トリアゾール-1-イルメチレン)ジベンゾニトリル;レトロゾール (JAN)
英語化学名:
Letrozole
英語别名:
Letroz;FEMARA;etrozoL;Lelrozol;Lerozole;LETROZOL;LETRAZOLE;CGS-20267;LETROZOLE;letrozolex
CBNumber:
CB9286355
化学式:
C17H11N5
分子量:
285.3
MOL File:
112809-51-5.mol

レトロゾール 物理性質

融点 :
181-183°C
沸点 :
563.5±60.0 °C(Predicted)
比重(密度) :
1.21±0.1 g/cm3(Predicted)
貯蔵温度 :
2-8°C
溶解性:
DMSO: >50mg/mL
酸解離定数(Pka):
1.52±0.11(Predicted)
外見 :
White powder
色:
white to off-white
Merck :
14,5450
InChIKey:
HPJKCIUCZWXJDR-UHFFFAOYSA-N
CAS データベース:
112809-51-5(CAS DataBase Reference)

安全性情報

主な危険性  Xi
Rフレーズ  36/37/38
Sフレーズ  26-36
WGK Germany  3
RTECS 番号 DI4957000
HSコード  2933997500
有毒物質データの 112809-51-5(Hazardous Substances Data)
毒劇物取締法 劇物

レトロゾール 価格 もっと(11)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01LKTL1878 レトロゾール
Letrozole
112809-51-5 25mg ¥19300 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01LKTL1878 レトロゾール
Letrozole
112809-51-5 50mg ¥30400 2021-03-23 購入
東京化成工業 L0248 レトロゾール >98.0%(HPLC)(T)
Letrozole >98.0%(HPLC)(T)
112809-51-5 1g ¥13500 2021-03-23 購入
Sigma-Aldrich Japan L6545 レトロゾール ≥98% (HPLC)
Letrozole ≥98% (HPLC)
112809-51-5 10mg ¥21200 2021-03-23 購入
Sigma-Aldrich Japan Y0000685 European Pharmacopoeia (EP) Reference Standard
Letrozole European Pharmacopoeia (EP) Reference Standard
112809-51-5 ¥35200 2021-03-23 購入

レトロゾール 化学特性,用途語,生産方法

用途

レトロゾール(英: letrozole)は乳癌の治療で用いられるアロマターゼ阻害薬の一種であり、アロマターゼから作られるエストロゲンの産生を抑えることによってホルモン依存性の腫瘍を抑える効果が期待される。

効能

抗悪性腫瘍薬, エストロゲン生合成阻害薬

商品名

フェマーラ (ノバルティスファーマ)

説明

Letrozole (trade name: Femara) is an orally active nonsteroidal aromatase inhibitor. As a competitive inhibitor of the aromatase, Letrozole inhibits the conversion of androgens to estrogen (estrogen stimulates breast tissues and breast cancer reoccurrence) and gonadal steroidogenesis. It can be used for the treatment of breast cancer that is hormonally-responsive or has an unknown receptor status in postmenopausal women. Besides this, Letrozole also has some off-label use such as ovarian stimulation, pretreatment of termination of pregnancy, treatment of gynecomastia, treatment of endometriosis, and promoting spermatogenesis for male patients of nonobstructive azoospermia.

化学的特性

white to light yellow crystal

Originator

Novartis (Switzerland)

使用

A nonsteroidal aromatase inhibitor structurally related to Fadrozole. Antineoplastic

Manufacturing Process

From 4-bromomethylbenzonitrile and 1H-[1,2,4]triazole was obtained 4- [1,2,4]triazol-1-ylmethylbenzonitrile. Treatment of that with strong base (tertBuOK) results in formation of the anion by removal of the relatively acidic benzyl proton. This anion was condensed with p-fluorobenzinitrile to give benzhydryl tetrazole (Letrozole)

brand name

Femara (Novar tis).

Therapeutic Function

Antineoplastic

一般的な説明

Letrozole, 4,4'-(1H-1,2,4-triazol-1-ylmethylene)dibenzonitrile (Femara), is used for most of thesame indications as anastrozole. It reduces concentrations ofestrogens by 75% to 95%, with maximal suppressionachieved within 2 to 3 days. Letrozole is specific for aromataseinhibition, with no additional effects on adrenal corticoidbiosynthesis. CYPs 3A4 and 2A6 are involved in themetabolism of letrozole to the major carbinol metabolite,which is inactive. The loss of the triazole ring, which is involvedin coordination of the heme iron, would explain theloss of activity. Letrozole strongly inhibits CYP2A6 invitro, with moderate inhibition of CYP2C19. The effect ofthis in vitro inhibition on the pharmacokinetics of coadministereddrugs is unknown. Tamoxifen reduces the levels ofletrozole significantly if they are used together, so combinationtreatment with these agents is not recommended.

作用機序

Inhibition of arom atase by letrazole is competitive and highly specific , with no effect on enzymes that are responsible for the production of glucocorticosteroids and mineralocorticosteroids. This agent is significantly more effective than tamoxifen in treating horm one-dependent cancer.

臨床応用

Femara was launched in France and the UK for second-line treatment of advanced breast cancer. Letrazole can be synthesized in two steps from 4- bromomethyl-benzonitrile with 1,2,4-triazole and is a third generation aromatase inhibitor. It is a highly specific inhibitor of P450arom which prevents the conversion of androstenedione to estrone. The reduction of plasma estrogen was immediate and long lasting. This is accomplished with no inhibition of other steroid biosynthesis making it the most selective aromatase inhibitor tested. Letrazole has remarkable antitumor activity, is well tolerated and has no toxic side effects. It is 10,000 times more potent than aminoglutethimide, in vivo, the first well established aromatase inhibitor.

参考文献

https://www.drugbank.ca/drugs/DB01006
https://en.wikipedia.org/wiki/Letrozole

レトロゾール 上流と下流の製品情報

原材料

準備製品


レトロゾール 生産企業

Global( 438)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
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Hangzhou FandaChem Co.,Ltd.
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112809-51-5(レトロゾール)キーワード:


  • 112809-51-5
  • LetrozoleUsp28
  • Letrozole99%
  • CGS-20267, Femara
  • LETRAZOLE
  • letrozolex
  • Lelrozol
  • 1-[BIS(4-CYANOPHENYL)METHYL]-1,2,4-TRIAZOLE
  • 4,4'-(1H-1,2,4-Triazol-1-ylmethylene)dibenzonitrile
  • 4,4'-(1H-1,2,4-Triazole-1-ylmethylene)bisbenzonitrile
  • 4,4'-[(1H-1,2,4-Triazole-1-yl)methylene]dibenzonitrile
  • Letrozole (200 mg)
  • 4-[(4-cyanophenyl)(1H-1,2,4-triazol-1-yl)Methyl]benzonitrile
  • 20MG/50MG/1KG
  • Letrozole(FeMara)
  • Lerozole
  • Letrof L Lil
  • Letroz
  • Letrozole###112809-51-5
  • Aromatase Inhibitor II, Letrozole
  • Letrozol Tablets
  • FEMARA
  • CGS-20267
  • LETROZOL
  • LETROZOLE
  • Letrozole 4,4'-(1H-1,2,4-Triazol-1-ylmethylene)bisbenzonitrile
  • 4,4'-(1H-1,2,4-TRIAZOL-1-YLMETHYLENE) BIS-BENZONITRILE
  • Letrazole(Femara)
  • To letrozole
  • Aromatase Inhibitor II, Letrozole - CAS 112809-51-5 - Calbiochem
  • Letrozole powder
  • 4,4'-[(1H-1,2,4-トリアゾール-1-イル)メチレン]ジベンゾニトリル
  • フェマラ
  • レトロゾール
  • フェマーラ
  • 4,4'-[(1H-1,2,4-トリアゾール-1-イル)メチレン]ビスベンゾニトリル
  • 4,4'-(1H-1,2,4-トリアゾール-1-イルメチレン)ビスベンゾニトリル
  • 1-ビス(4-シアノフェニル)メチル-1,2,4-トリアゾール
  • 4,4'-(1,2,4-トリアゾール-1-イルメチレン)ジベンゾニトリル
  • レトロゾール (JAN)
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