Goserelin

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Achtung

• Gefahrenhinweise

  H317：Kann allergische Hautreaktionen verursachen.

  H332：Gesundheitsschädlich bei Einatmen.

  H334：Kann bei Einatmen Allergie, asthmaartige Symptome oder Atembeschwerden verursachen.

• Sicherheit

  P261：Einatmen von Staub vermeiden.

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

  P272：Kontaminierte Arbeitskleidung nicht außerhalb des Arbeitsplatzes tragen.

  P280：Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.

  P285：Bei unzureichender Belüftung Atemschutz tragen.

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

  P304+P341：BEI EINATMEN: Bei Atembeschwerden an die frische Luft bringen und in einer Position ruhigstellen, die das Atmen erleichtert

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

  P321：Besondere Behandlung

  P333+P313：Bei Hautreizung oder -ausschlag: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen.

  P342+P311：Bei Symptomen der Atemwege: GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen.

  P363：Kontaminierte Kleidung vor erneutem Tragen waschen.

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

Goserelin Chemische Eigenschaften,Einsatz,Produktion Methoden

• S-Sätze Betriebsanweisung:

  S22:Staub nicht einatmen.
  S24/25:Berührung mit den Augen und der Haut vermeiden.

• Beschreibung

  Goserelin is an analog of luteinizing hormone-releasing hormone (LHRH) useful in the treatment of malignancies responsive to hormonal manipulation. Administered parenterally in a biodegradable depot, goserelin is reportedly as effective as orchidectomy and oophorectomy in patients with advanced prostate carcinoma and pre-menopausal breast cancer.

• Chemische Eigenschaften

  White or almost white powder.

• Originator

  ICI (United Kingdom)

• Verwenden

  Labelled Goserelin (G767500). Synthetic peptide agonist analog of LH-RH. Antineoplastic (hormonal).

• Verwenden

  Goserelin USP (Zoladex) is used to treat Prostatic carcinoma.

• Verwenden

  Labeled Goserelin, intended for use as an internal standard for the quantification of Goserelin by GC- or LC-mass spectrometry.

• Definition

  ChEBI: Goserelin is an organic molecular entity.

• Manufacturing Process

  (a) Solid Phase Preparation of Nonapeptide
  The solid phase synthesis was carried out in automatic mode on an Applied Biosystems 430A Peptide Synthesizer using Boc-Pro-OBzl-polystyrene resin 1% cross-linked with divinylbenzene (Peninsula Laboratories), 1.25 g, 0.38 meq/g though nominally 0.7 meq/g). The following protected amino acids were converted to benzotriazolyl esters by reaction with HOBt (1- hydroxybenzotriasole) and DIPC (di-isopropylcarbodiimide) in DMF immediately before use. The protected amino acids were coupled in the following sequence: Boc-Arg(HCl)-OH; Boc-Leu-OH; Fmoc-D-Ser(But)-OH; Fmoc-Tyr(BrZ)-OH; Fmoc-Ser-OH; Fmoc-Trp-OH; Fmoc-His(Fmoc)-OH; PyrOH. The sequence of operations for the first two stages (using Boc-protectedamino acids) was: removal of Boc with 45% triflouroacetic acid in dichloromethane;10% DIEA (diethyl amine)/DMF wash; coupling (2 equivalents of protected amino acid HOBt ester); removal of Boc as above. The sequence of operations for the last six stages (using Fmoc-protectedamino acids) was: removal of Fmoc with 20% piperidine/DMF; 0.5 molar HOBt/DMF wash; coupling (1 equivalent of protected amino acid HOBt ester). All coupling reactions except that using Boc-Arg(HCl)-OH were of 1 hour duration; the Boc-Arg(HCl)-OH one was of 2 hours duration. There was thus obtained the nonapeptide-resin (1.7 g; 0.29 mmole peptide per g) with the Tyr still protected by BrZ.
  (b) Cleavage of Peptide From Resin
  The peptide resin prepared above was treated with a 20-fold excess of anhydrous hydrazine in DMF (20 ml) at laboratory temperature for 24 hours, and the mixture was filtered and evaporated to dryness. This procedure also removed the BrZ protecting group from the Tyr moeity. The residue was purified by gel filtration on a column (LH 20 Sephadex) using a 20:1 v/v mixture of water and acetic acid as eluant. There was thus obtained Pyr-HisTrp-Ser-Tyr-D-Ser(But)-Leu-Arg(H+)-Pro-NH-NH2. The structure of which was confirmed by amino acid analysis and mass spectroscopy.
  (c) Preparation of Goserelin
  A solution of potassium cyanate (11 mg) in water (1.36 ml) was added portionwise during 1 hour to a solution of the above hydrazide (118 mg) in a 20:1 v/v mixture of water and acetic acid (10 ml). The mixture was freezedried and the residue was purified by reverse-phase column chromatography (Dynamax 60 ANG, C18, 1 inch diameter) using a gradient of 10% to 40% by volume of acetonitrile in water containing 0.1% trifluoroacetic acid. There was thus obtained goserelin (100 mg, 25% yield overall), the structure of which was confirmed by mass spectroscopy.

• Trademarks

  Zoladex (Zeneca).

• Therapeutic Function

  Antineoplastic, Antitumor

• Clinical Use

  Synthetic decapeptide analogue of LHRH:
  
  Treatment of advanced prostate cancer, breast cancer, endometriosis and endometrial thinning and uterine fibroids

• Nebenwirkungen

  Hot flashes (flushing), dizziness, headache, increased sweating, decreased sexual interest/ability, trouble sleeping, nausea, change in breast size, vaginal dryness, or hair loss may occur. Pain, bruising, bleeding, redness, or swelling at the injection site may also occur.
  This medication may rarely make your blood sugar rise, which can cause or worsen diabetes.
  Serious side effects including: symptoms of a heart attack (such as chest/jaw/left arm pain, shortness of breath, unusual sweating), signs of a stroke (such as weakness on one side of the body, trouble speaking, sudden vision changes, confusion), fast/irregular heartbeat, severe dizziness, fainting.
  In men using this medication for prostate cancer, a rare but very serious urinary blockage problem or spinal cord problem (compression) can occur, especially during the first month of treatment.

• Arzneimittelwechselwirkung

  Goserelin may be given on its own or is often combined with another hormone therapy such as tamoxifen or drugs known as aromatase inhibitors (anastrozole, exemestane and letrozole).
  The risk or severity of QTc prolongation can be increased when Goserelin is combined with Clozapine. The risk or severity of methemoglobinemia can be increased when Goserelin is combined with Cocaine.

• Stoffwechsel

  Metabolised by tissue peptidases and is excreted in urine and bile as unchanged drug and metabolites.

Goserelin Upstream-Materialien And Downstream Produkte

Goserelin Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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