Wirkstoffe H

H3B-8800

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

 
HQP1351 - GZD824 Dimesylate(HQP1351)

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

Ascentage Pharma Releases Updated Data of its Novel BCR-ABL Inhibitor, HQP1351, in an Oral Presentation Nominated for "Best of ASH"

Link to ASH 2019 Presentation

More info on ClinicalTrials.gov

Hydroxyurea/Hydroxycarbamid - LITALIR®

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 zur Fachinformation des Compendium®:
Medikamenteniformation: Für den Arzt  Patienteninformation
Information des Médicaments:  Info prof. Info patient
Informazione sul medicamento: info per il paziente
 
More Information in English: