Formestane

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Achtung

• Gefahrenhinweise

  H360：Kann die Fruchtbarkeit beeinträchtigen oder das Kind im Mutterleib schädigen.

• Sicherheit

  P201：Vor Gebrauch besondere Anweisungen einholen.

  P308+P313：BEI Exposition oder falls betroffen: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen.

Formestane Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R60:Kann die Fortpflanzungsfähigkeit beeinträchtigen.

• S-Sätze Betriebsanweisung:

  S53:Exposition vermeiden - vor Gebrauch besondere Anweisungen einholen.
  S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
  S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).

• Beschreibung

  Formestane is a potent aromatase inhibitor launched in the UK as a second-line endocrine treatment for breast cancer. As a synthetic derivative of androstanedione, the natural substrate for the biosynthesis of estrogen by the enzyme aromatase, formastane selectively inhibits aromatase and binds to its steroid receptor site to cause a rapid and sustained fall in circulating estrogen level and, therefore, inhibits tumor growth. In patients with existing bulky primary tumors, formestane effectively reduces the size of the tumors. Formastane has apparent tolerability advantages and less side effects than other agents such as aminoglutethimide.

• Beschreibung

  4-hydroxy Androstenedione (4-HAD) is a steroidal inhibitor of aromatase (also known as cytochrome P450 19A1; K_i = 27 nM). As aromatase catalyzes the conversion of androgens to estrogens, aromatase inhibitors, including 4-HAD, are used against hormone-sensitive breast cancer in menopausal women. They are also abused in combination with anabolic steroids in racehorses and athletes. This product is intended for forensic and research applications.

• Chemische Eigenschaften

  Needles

• Originator

  Ciba-Geigy (Switzerland)

• History

  Formestane is a second-generation steroidal aromatase inhibitor, and the first one to reach clinical use during the early 1990s[1].

• Verwenden

  An antitumor drug. An aromatase inhibitor.

• Verwenden

  antineoplastic, aromatase inhibitor

• Definition

  ChEBI: A 17-oxo steroid that is androst-4-ene-3,17-dione in which the hydrogen at position 4 is replaced by a hydroxy group. Formestane was the first selective, type I steroidal aromatase inhibitor, suppressing oestrogen production from anabolic steroids or proho mones. It was formerly used in the treatment of oestrogen-receptor positive breast cancer in post-meopausal women. As it has poor oral bioavailability, it had to be administered by (fortnightly) intramuscular injection. It fell out of use with the subseque t development of cheaper, orally active aromatase inhibitors. Formestane is listed by the World Anti-Doping Agency as a substance prohibited from use by athletes.

• Trademarks

  Lentaron

• Mechanism of action

  Aromatase inhibitors such as formestane and letrozole reduce plasma estradiol levels by inhibiting the conversion of testosterone to estrogen. This compound was first described as a competitive inhibitor, but subsequent evidence proved that its binding to aromatase was irreversible. Hence, it is a suicide inhibitor. In the dog, but not rodents, this results in Leydig cell hypertrophy and hyperplasia. This is thought to be due to the differential sensitivity of the pituitary feedback mechanism to estrogens and androgens in the different species[1-2].

• Einzelnachweise

  [1] Avenda?o C, et al. Anticancer Drugs That Inhibit Hormone Action. Medicinal Chemistry of Anticancer Drugs, 2008; 53-91.0
  [2] Berczi I, et al. Biologically Controlled Mutations are Right for Evolution. Insights to Neuroimmune Biology, 2016; 217-241.

Formestane Upstream-Materialien And Downstream Produkte

Formestane Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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