Orale Wirkstoffe G
Gefitinib - IRESSA® ist ein Anilinochinazolin mit antineoplastischer Aktivität. Gefitinib hemmt die katalytische Aktivität zahlreicher Tyrosinkinasen einschließlich des epidermalen Wachstumsfaktorrezeptors (EGFR), was zur Hemmung des Tyrosinkinase-abhängigen Tumorwachstums führen kann. Insbesondere konkurriert Gefitinib mit der Bindung von ATP an die Tyrosin-Kinase-Domäne von EGFR um damit die Rezeptor-Autophosphorylierung zu hemmen und letztlich die Hemmung der Signalübertragung. Gefitinib kann auch den Stillstand des Zellzyklus induzieren und die Angiogenese hemmen.
Indikationen/Anwendungsmöglichkeiten gemäss Arzneimittel-Kompendium der Schweiz®:
- IRESSA ist indiziert zur Behandlung von Patienten mit Adenokarzinom der Lunge und aktivierender EGFR Mutation, wenn eine platinhaltige Chemotherapie versagt hat oder nicht möglich ist.
More Information in English:
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Link to National Cancer Institute More Information for patients:
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According to the NCI website Gilteritinib is an orally bioavailable inhibitor of the receptor tyrosine kinases (RTKs) FMS-related tyrosine kinase 3 (FLT3, STK1, or FLK2), AXL (UFO or JTK11) and anaplastic lymphoma kinase (ALK or CD246), with potential antineoplastic activity. Gilteritinib binds to and inhibits both the wild-type and mutated forms of FLT3, AXL and ALK. This may result in an inhibition of FLT3, AXL, and ALK-mediated signal transduction pathways and reduction of tumor cell proliferation in cancer cell types that overexpress these RTKs. FLT3, AXL and ALK, overexpressed or mutated in a variety of cancer cell types, play a key role in tumor cell growth and survival. Check for active clinical trials using this agent.
More Information in English:
Link to MedlinePlus, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to National Cancer Institute
Link zu PharmaWiki
Link to Physicians Desk Reference (PDR)
Link to European Medicines Agency (EMEA)
Info for Patients presented by Scott Hamilton from Chemocare.com
According to the NCI website glasdegib maleate is the salt form of glasdegib, an orally bioavailable small-molecule, smoothened (SMO) receptor inhibitor, with potential antineoplastic activity. Upon oral administration, glasdegib targets, binds to and inhibits the activity of SMO. This inhibits the activity of the Hedgehog (Hh) signaling pathway and inhibits the growth of tumor cells in which this pathway is aberrantly activated. SMO, a transmembrane protein, is involved in Hh signal transduction. The Hh signaling pathway plays an important role in cellular growth, differentiation, repair, and cancer stem cell (CSC) survival. Constitutive activation of Hh pathway signaling has been observed in various types of malignancies and is associated with uncontrolled cellular proliferation in a variety of cancers. Check for active clinical trials using this agent.
More Information in English:
Link to MedlinePlus, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to National Cancer Institute
Link zu PharmaWiki
Link to Physicians Desk Reference (PDR)
Link to European Medicines Agency (EMEA)
Info for Patients presented by Scott Hamilton from Chemocare.com