Abiraterone

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

  H315：Verursacht Hautreizungen.

  H319：Verursacht schwere Augenreizung.

  H332：Gesundheitsschädlich bei Einatmen.

  H335：Kann die Atemwege reizen.

• Sicherheit

  P233：Behälter dicht verschlossen halten.

  P260：Dampf/Aerosol/Nebel nicht einatmen.

  P261：Einatmen von Staub vermeiden.

  P264：Nach Gebrauch gründlich waschen.

  P264：Nach Gebrauch gründlich waschen.

  P270：Bei Gebrauch nicht essen, trinken oder rauchen.

  P271：Nur im Freien oder in gut belüfteten Räumen verwenden.

  P280：Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.

  P301+P312：BEI VERSCHLUCKEN: Bei Unwohlsein GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen.

  P302+P352：BEI BERÜHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckmäßig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen.

  P304：BEI EINATMEN

  P304+P340：BEI EINATMEN: Die Person an die frische Luft bringen und für ungehinderte Atmung sorgen.

  P305+P351+P338：BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen.

  P312：Bei Unwohlsein GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen.

  P321：Besondere Behandlung

  P330：Mund ausspülen.

  P332+P313：Bei Hautreizung: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen.

  P337+P313：Bei anhaltender Augenreizung: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen.

  P340：Die betroffene Person an die frische Luft bringen und in einer Position ruhigstellen, die das Atmen erleichtert.

  P362：Kontaminierte Kleidung ausziehen und vor erneutem Tragen waschen.

  P403：An einem gut belüfteten Ort aufbewahren.

  P403+P233：An einem gut belüfteten Ort aufbewahren. Behälter dicht verschlossen halten.

  P405：Unter Verschluss aufbewahren.

  P501：Inhalt/Behälter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen.

Abiraterone Chemische Eigenschaften,Einsatz,Produktion Methoden

• Chemische Eigenschaften

  White Solid

• Originator

  Abiraterone,Cougar

• History

  Abiraterone (brand name: Zytiga) is an anti-cancer drug developed by Centocor Ortho Biotech Inc.  It was first approved by the FDA on 28 April 2011 for the treatment of advanced prostate cancer.  In December 2012, the FDA expanded Zytiga's approved use to include treatment of men with advanced (metastatic) castration-resistant prostate cancer prior to chemotherapy.  By February 2018, the FDA further approved Zytiga (abiraterone acetate) in combination with prednisone for the treatment of early metastatic prostate cancer.

• Verwenden

  Prasteronyl Abiraterone is a dimer impurity of Abiraterone (A108490), a steroidal cytochrome P 450 17α-hydroxylase-17,20-lyase inhibitor (CYP17), is currently undergoing phase II clinical trials as a potential drug for the treatment of androgen-dependent prostate cancer.

• Verwenden

  Abiraterone, a steroidal cytochrome P 450 17α-hydroxylase-17,20-lyase inhibitor (CYP17), is currently undergoing phase II clinical trials as a potential drug for the treatment of androgen-dependent pr ostate cancer.

• Definition

  ChEBI: A 3beta-sterol that is androsta-5,16-dien-3beta-ol substituted at position 17 by a 3-pyridyl group. Administered as the O-acetate, it is used for treatment of metastatic castrate-resistant prostate cance .

• Manufacturing Process

  Diethyl(3-pyridyl)borane (3.38 g, 23 mmol) from Aldrich Chemical Co. Ltd. was added to a stirred solution of 3β-acetoxyandrosta-5,16-dien-17-yl trifluoromethanesulphonate (6.94 g, 15 mmol) in THF (75 ml) containing bis(triphenylphosphine)palladium(II) chloride (0.105 g, 0.15 mmol). An aqueous solution of sodium carbonate (2 M, 30 ml) was then added and the mixture heated, with stirring, by an oil bath at 80°C for 1 h, and allowed to cool. The mixture was partitioned between diethyl ether and water, the ether phase was dried (Na2CO3), filtered through a short plug of silica, and concentrated. Chromatography, on elution with light petroleum-diethyl ether (2:1), afforded the 3β-acetoxy-17-(3-pyridyl)androsta-5,16-diene (4.95 g, 84%) which crystallised from hexane, m.p. 144-145°C.
  To a solution of 3β-acetoxy-17-(3-pyridyl)androsta-5,16-diene (4.90 g, 12.5 mmol) in methanol (50 ml) was added an aqueous solution of sodium hydroxide (10% w/v, 10 ml) and the mixture heated, with stirring, on an oil bath at 80°C for 5 min, then allowed to cool. The mixture was poured into water, neutralised with hydrochloric acid (1 M), rebasified with saturated sodium bicarbonate solution, and extracted with hot toluene. The toluene extracts were combined, dried (Na2CO3), and concentrated. Chromatography, on elution with toluene-diethyl ether (2:1) afforded the 17-(3- pyridyl)androsta-5,16-dien-3β-ol (3.45 g, 79%) which crystallised from toluene, m.p. 228-229°C.

• Therapeutic Function

  Antiandrogen

• Biologische Aktivität

  abiraterone (17-(3-pyridyl)androsta-5,16-dien-3β-ol) is a potent small-molecule inhibitor of cyp17 complex (17 alpha-monooxygenase) which is a member of the cytochrome p450 family consisting of 17 alpha-hydroxylase and c17,20-lyase and catalyzing the 17 alpha-hydroxylation of intermediates of steroid biosynthesis involved in testerone sysnthesis. abiraterone inhibits cyp17 complex by binding to the haem iron of cyp17a1, which forms a 60o angle above the haem plane and packs against the central i helix with 3β-oh interacting with aspargine 202 in the f helix. abiraterone is currently being investigated to treat late stage prostate cancer, in which it consistently suppresses testosterone levels, leads to significant reduction in psa level, and prolong life in patients with castration-resistant prostate cancer (crpc).natasha m. devore and emily e. scott. structures of cytochrome p450 17a1 with prostate cancer drugs abiraterone and tok-001. nature 2012; 482: 116-120farshid dayyani, gary e. gallick, christopher j. logothetis, paul g. corn. novel therapies for metastatic castrate-resistant prostate cancer. jnci j natl cancer inst (2011); 103(22): 1665-1675

• target

  CYP17

Abiraterone Upstream-Materialien And Downstream Produkte

Abiraterone Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global(473)Suppliers

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