Wirkstoffe H
According to the NCI website the splicing inhibitor H3B-8800 is an orally bioavailable inhibitor of the splicing factor 3B subunit 1 (SF3B1), with potential antineoplastic activity. Upon administration, H3B-8800 binds to and blocks the activity of SF3B1, a core spliceosome protein that is mutated in various cancer cells. This modulates RNA splicing by preventing aberrant mRNA splicing by the spliceosome, blocks RNA mis-splicing, enhances proper RNA splicing and prevents the expression of certain tumor-associated genes. This leads to an induction of apoptosis and prevents tumor cell proliferation. In many cancer cells, core spliceosome proteins, including SF3B1, U2 small nuclear ribonucleoprotein auxiliary factor 1 (U2AF1), serine/arginine-rich splicing factor 2 (SRSF2) and U2 small nuclear ribonucleoprotein auxiliary factor subunit-related protein 2 (ZRSR2), are mutated and aberrantly activated leading to a dysregulation of mRNA splicing. Check for active clinical trials using this agent.
More Information in English:
Link to National Cancer Institute
According to the NCI website the BCR-ABL/KIT/AKT/ERK inhibitor HQP1351 is an orally bioavailable inhibitor of a variety of kinases, including the Bcr-Abl tyrosine kinase, the mast/stem cell growth factor receptor Kit (c-Kit), the serine/threonine protein kinase Akt (protein kinase B), and the extracellular signal-regulated kinase (ERK) with antineoplastic activity. Upon administration, HQP1351 targets, binds to and inhibits the kinase activities of Bcr-Abl, AKT, c-Kit and ERK. This inhibits their mediated signaling pathways and inhibits proliferation of tumor cells in which these kinases are overexpressed and/or mutated. Bcr-Abl, c-Kit, AKT and ERK play key roles in the proliferation, differentiation and survival of tumor cells. Check for active clinical trials using this agent.
More Information in English:
Link to National Cancer Institute
Der Antimetabolit Hydroxyurea/Hydroxycarbamid - Litalir® ist ein monohydroxyl-substituierter Harnstoff (Hydroxycarbamat). Hydroxyurea hemmt selektiv die Ribonucleosid-Diphosphat-Reduktase, ein Enzym, das für die Umwandlung von Ribonukleosid Diphosphat zu Desoxyribonukleosid Diphosphat erforderlich ist, wodurch die Zellen am Verlassen der G1/S-Phase des Zellzyklus gehindert werden. Dieses Mittel weist auch radiosensibilisierende Aktivitäten auf, indem es Zellen in der strahlungsempfindlichen G1 Phase verharren lässt und die DNA-Reparatur stört.
Indikationen/Anwendungsmöglichkeiten gemäss Compendium®:
- Chronisch-myeloische Leukämie und andere myeloproliferative Syndrome wie essentielle Thrombozythämie, Myelofibrose und Polycythaemia vera mit starker Thrombozytose.
Link to National Cancer Institute
Link zu Wiki
Link zu PharmaWiki
More Information for patients:
Link to MedlinePlus, a service of the U.S. National Library of Medicine, National Institutes of Health
Info for Patients presented by Scott Hamilton from Chemocare.com