Nintedanib

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

  H315：Verursacht Hautreizungen.

  H319：Verursacht schwere Augenreizung.

  H335：Kann die Atemwege reizen.

• Sicherheit

  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+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.

  P330：Mund ausspülen.

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

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

  P362：Kontaminierte Kleidung ausziehen und vor erneutem Tragen waschen.

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

  P405：Unter Verschluss aufbewahren.

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

Nintedanib Chemische Eigenschaften,Einsatz,Produktion Methoden

• Verwenden

  It is an indolinone derivative potently blocking VEGF-, PDGF-, and FGF-receptor kinases; an indolinone as triple angiokinase inhibitors. An antitumor agent.

• Verwenden

  BIBF1120 (Vargatef) is a potent inhibitor of VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

• Definition

  ChEBI: A member of the class of oxindoles that is a kinase inhibitor used (in the form of its ethylsulfonate salt) for the treatment of idiopathic pulmonary fibrosis and cancer.

• Biologische Aktivität

  nintedanib (bibf 1120) is an indolinone-derived oral active, triple angiokinase inhibitor of vascular endothelial growth factor receptor (vegfr)1-3, fibroblast growth factor receptor (fgfr)1-3 and platelet-derived growth factor receptor (pdgfr)α/β1. it has shown potent antiangiogenic activity at nanomolar (ic50, 20-100 nmol/l) by blocking these receptor-mediated signaling pathways1,2. nintedanib (bibf 1120) is in clinical development for the treatment of idiopathic pulmonary fibrosis as these receptors have been shown to be potentially involved in the pathogenesis of pulmonary fibrosis3,4. as a novel angiogenesis inhibitor, it is also being widely evaluated in different cancer models and has displayed significant anti-tumor activities by inhibiting tumor blood vessel formation5-7.to further evaluate its antitumor effects on multiple tumors, nintedanib is currently entering several

• Clinical Use

  Tyrosine kinase inhibitor:
  Treatment of locally advanced, metastatic or locally recurrent non-small cell lung cancer (NSCLC) of adenocarcinoma tumour histology in combination with docetaxel
  Treatment of Idiopathic Pulmonary Fibrosis (IPF)

• Nebenwirkungen

  The most common side effects of Nintedanib in clinical studies were gastrointestinal-related side effects, including nausea (31%), vomiting (23%), diarrhoea (76%), abdominal pain (10%) and decreased appetite (10%). Other side effects were hepatic impairment commonly seen as elevated liver enzymes, weight loss (7 per cent), nasopharyngitis (7 per cent), cough (14 per cent), upper respiratory tract infections (14 per cent), headache (12 per cent), fatigue (14 per cent), skin ulcers (16 per cent) and urinary tract infections (12 per cent).
  Reported post-marketing adverse events include gastrointestinal perforation, proteinuria and pancreatitis. In several clinical trials, nidanib has also been found to be associated with an increased risk of bleeding, possibly secondary to VEGFR inhibition. Although serious bleeding and arterial thromboembolic events (e.g., myocardial infarction (MI) and stroke) are rare, bleeding events with serious and fatal consequences have been reported in post-marketing surveillance. Therefore, the use of nidazanib has been associated with an increased risk of bleeding, possibly secondary to VEGFR inhibition. Therefore, patients treated with nidazanib and receiving full anticoagulation therapy need to be closely monitored for adverse bleeding events.

• target

  VEGFR1/2/3

• Arzneimittelwechselwirkung

  Potentially hazardous interactions with other drugs
  Antibacterials: concentration reduced by rifampicin - avoid.
  Antifungals: concentration increased by ketoconazole.
  Antipsychotics: increased risk of agranulocytosis with clozapine - avoid.

• Stoffwechsel

  Nintedanib is metabolised in the liver, initially by hydrolytic cleavage by esterases and then by glucuronidation by uridine diphosphate glucuronosyltransferase enzymes. Only a minor portion is metabolised by cytochrome P450 isoenzymes, mainly CYP3A4. More than 90% of a dose is eliminated by faecal/biliary excretion.

• Lager

  Store at -20°C

• Einzelnachweise

  [1]hilberg, f. et al. bibf 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. cancer research 68, 4774-4782, doi:10.1158/0008-5472.can-07-6307 (2008).

Nintedanib Upstream-Materialien And Downstream Produkte

Nintedanib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global(386)Suppliers

656247-17-5, Nintedanib Verwandte Suche: