Wirkstoffe N

nab-paclitaxel - Abraxane®

Abraxane®; According to the NCI website nab-paclitaxel (paclitaxel albumin-stabilized nanoparticle formulation) is a cremophor EL-free, albumin-stabilized nanoparticle formulation of the natural taxane paclitaxel with antineoplastic activity. Paclitaxel binds to and stabilizes microtubules, preventing their depolymerization and so inhibiting cellular motility, mitosis, and replication. This formulation solubilizes paclitaxel without the use of the solvent Cremophor, thereby permitting the administration of larger doses of paclitaxel while avoiding the toxic effects associated with Cremophor.

INDICATIONS According to PDR.net

  • Non-Small Cell Lung Cancer - Locally Advanced or Metastatic
  • Metastatic Pancreatic Adenocarcinoma
  • Metastatic Breast Cancer After failure of combination chemotherapy or relapse w/in 6 months of adjuvant chemotherapy 

Indikationen/Anwendungsmöglichkeiten gemäss Arzneimittelkompendium:

  • Abraxane ist indiziert für die Behandlung des metastasierenden Mammakarzinoms nach Versagen einer Chemotherapie oder Rezidiv innert 6 Monaten nach adjuvanter Chemotherapie. In der Vortherapie sollte ein Anthrazyklin enthalten gewesen sein, es sei denn, es bestand eine klinische Kontraindikation.
  • Abraxane, in Kombination mit Gemcitabin, ist indiziert für die Erstlinienbehandlung von Patienten mit lokal fortgeschrittenem nicht resezierbarem oder metastasiertem Adenokarzinom des Pankreas.
Link zur Fachinformation des Arzneimittel-Kompendiums der Schweiz:
Medikamenteniformation: Für den Arzt
Information des Médicaments: Info prof.
 

Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to MedlinePlus, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to National Cancer Institute
Link zu Wiki
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

Taxane

Necitumumab

According to the NCI website necitumumab is a fully human IgG1 monoclonal antibody directed against the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Necitumumab binds to and blocks the ligand binding site of EGFR, thereby preventing the activation and subsequent dimerization of the receptor. This may lead to an inhibition of EGFR-dependent downstream pathways and so inhibition of EGFR-dependent tumor cell proliferation and metastasis. EGFR, a member of the epidermal growth factor family of extracellular protein ligands, may be overexpressed on the cell surfaces of various tumor cell types.

Link to Drug Information Portal

Link to National Cancer Institute

Link zu Wiki

Monoclonal Antibodies

Nelarabine

Atriance®; According to the NCI nelarabine is an arabinonucleoside antimetabolite with antineoplastic activity. Nelarabine is demethoxylated by adenosine deaminase to become biologically active 9-beta-D-arabinosylguanine (ara-G); ara-G incorporates into DNA, thereby inhibiting DNA synthesis and inducing an S phase-dependent apoptosis of tumor cells.

Indikationen/Anwendungsmöglichkeiten gemäss Arzneimittel-Kompendium der Schweiz®:

Behandlung von Patienten mit akuter lymphoblastischer T-Zell-Leukämie und lymphoblastischem T-Zell-Lymphom, die auf Behandlungen mit mindestens zwei Chemotherapieregimes nicht angesprochen haben oder nach der chemotherapeutischen Behandlung ein Rezidiv oder eine Progression entwickelten.

Link to Drug Information Portal
Link to MedlinePlus
Link to National Cancer Institute
Link zu Wiki
Link zu PharmaWiki
Link to Physicians Desk Reference (PDR)
Link to European Medicines Agency (EMEA)
Link zur Fachinformation des Arzneimittel-Kompendium der Schweiz
Info for Patients presented by Scott Hamilton from Chemocare.com

Chemotherapy

Neratinib

Acording to the NCI website Neratinib is an orally available, 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity. Neratinib binds to the HER-2 receptor irreversibly, thereby reducing autophosphorylation in cells, apparently by targeting a cysteine residue in the ATP-binding pocket of the receptor. Treatment of cells with this agent results in inhibition of downstream signal transduction events and cell cycle regulatory pathways; arrest at the G1-S (Gap 1/DNA synthesis)-phase transition of the cell division cycle; and ultimately decreased cellular proliferation. Neratinib also inhibits the epidermal growth factor receptor (EGFR) kinase and the proliferation of EGFR-dependent cells.

 

Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to National Cancer Institute
Link to Wikipedia

Receptor Tyrosine Kinase signaling Pathway
Receptor tyrosine kinases (RTK)s are very important signaling pathway, which not only include growth factor receptors such as EGFR(HER)VEGFR PDGFRFGGFRIGF-1R, Mast/stem cell growth factor receptor ( c-Met) and HER2, but also other gene products which are expressed by the oncogenes such as SRC, Bcr, c-Met and Abl as well.
Read more at selleckbio about Receptor Tyrosine Kinase Signaling Pathway

Tyrosin Kinase Inhibitor

Nilotinib - Tasigna®

Nilotinib - Tasigna® ist ein oral bioverfügbares Aminopyrimidin-Derivat und ein Bcr-Abl-Tyrosinkinase-Inhibitor mit antineoplastischer Aktivität. Entwickelt zur Überwindung einer  Imatinib Resistenz bindet Nilotinib an die Kinase-Domäne des Abl Proteins des Bcr-Abl-Fusionsproteins und stabilisiert dadurch die inaktive Konformation der Domäne, was zur Hemmung der Bcr-Abl-vermittelten Proliferation von Philadelphia-Chromosom-positiven (Ph+) chronisch-myeloischen Leukämie (CML)-Zellen führt. Dieses Mittel hemmt auch den Tyrosin-Rezeptor-Kinase abhängigen Plättchenwachstumsfaktor-Rezeptor (PDGF-R) und c-kit, eine mutierte Tyrosin-Rezeptor-Kinase, die konstitutiv in den meisten gastrointestinalen Stromatumoren (GIST) aktiviert ist. Mit einem Bindungsmodus, der energetisch günstiger ist als mit Imatinib, verfügt Nilotinib über eine etwa 20-fach erhöhte Wirksamkeit bei Kinase- und Proliferationstests im Vergleich zu Imatinib.

Indikationen/Anwendungsmöglichkeiten gemäss Arzneimittel-Kompendium der Schweiz®:

  • Erstlinienbehandlung von erwachsenen Patienten mit Philadelphiachromosom-positiver chronischer myeloischer Leukämie (Ph+ CML) in der chronischen Phase.
  • Behandlung von Patienten mit Philadelphiachromosom-positiver chronischer myeloischer Leukämie (Ph+ CML) in der chronischen und in der akzelerierten Phase bei Resistenz oder hoher Toxizität unter Vorbehandlung mit Imatinib.
 
 
Link zur Fachinformation des Arzneimittel-Kompendiums der Schweiz:
Medikamenteniformation: Für den Arzt  Patienteninformation
Information des Médicaments:  Info prof. Info patient
Informazione sul medicamento: info per il paziente
 
More Information in English:
 
More Information for patients:

Bcr-Abl and the Receptor Tyrosine Kinase signaling Pathway
Receptor tyrosine kinases (RTK)s are very important signaling pathway, which not only include growth factor receptors such as EGFR(HER)VEGFRPDGFRFGGFRIGF-1R, Mast/stem cell growth factor receptor (c-Met) and HER2, but also other gene products which are expressed by the oncogenes such as SRC, Bcr, c-Met and Abl as well.
Read more at selleckbio about Receptor Tyrosine Kinase Signaling Pathway and Bcr-Abl

Introduction to Small Molecule Tyrosine Kinase Inhibitors presented by OncoLink
Nilutamide

According to the NCI website Nilutamide preferentially binds to androgen receptors and blocks androgen receptor activation by testosterone and other androgens; this agent may inhibit androgen-dependent growth of normal and neoplastic prostate cells.

Indikationen/Anwendungsmöglichkeiten gemäss Chemocare.com:
Nilutamide therapy is for men with advanced prostate cancer at stage D2, when there is evidence of metastases (cancer spread) to other areas of the body.
Anti-androgen medications are usually given in conjunction with LHRH agonists or after orchiectomy (surgical removal of the testicles).

 

Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health

Link to MedlinePlus, a service of the U.S. National Library of Medicine, National Institutes of Health

Link to National Cancer Institute

Link zu Wiki

Link to Physicians Desk Reference (PDR)

Info for Patients presented by Scott Hamilton from Chemocare.com

Antiandrogen

Nivolumab

According to the NCI website nivolumab is a fully human monoclonal antibody directed against the negative immunoregulatory human cell surface receptor PD-1 (programmed death-1 or programmed cell death-1/PCD-1) with immunopotentiation activity. Nivolumab binds to and blocks the activation of PD-1, an Ig superfamily transmembrane protein, by its ligands PD-L1 and PD-L2, resulting in the activation of T-cells and cell-mediated immune responses against tumor cells or pathogens.

Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to MedlinePlus, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to National Cancer Institute
Link zu Wiki
Link to European Medicines Agency (EMEA)