Teniposid Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Chemische Eigenschaften
White Solid
Verwenden
Teniposide is a podophyllotoxin derivative that causes dose-dependent single- and double-stranded breaks in DNA by inhibiting topoisomerase II. Its cytostatic effects are related to its ability to stabilize the DNA-topoisomerase II complex during DNA replication, inducing DNA damage and cellular apoptosis. Teniposide has been widely used in the treatment of various cancers including, small cell lung cancer, malignant lymphoma, breast cancer, oral squamous cell carcinoma, and acute lymphoblastic leukemia.
Definition
ChEBI: A furonaphthodioxole that is a synthetic derivative of podophyllotoxin with anti-tumour activity; causes single- and double-stranded breaks in DNA and DNA-protein cross-links and prevents repair by topoisomerase II binding.
Indications
Teniposide (VM-26, Vumon) is closely related to etoposide
in structure, mechanisms of action and resistance,
and adverse effects. It is more lipophilic and approximately
threefold more potent than etoposide. Its major
uses have been in pediatric cancers, particularly in acute
lymphoblastic leukemias.
Allgemeine Beschreibung
Teniposide is available in 50-mg ampules with Cremophor ELfor IV administration in the treatment of acute lymphoblasticleukemia (ALL). The agent is more potent as an inhibitor oftopoisomerase II. The pharmacokinetics of teniposide issimilar to that of etoposide; however, the more lipophilic teniposideis more highly protein bound (99%) and less isexcreted unchanged in the urine (10%–20%). There is alsogreater overall metabolism of teniposide; however, CYP3A4-mediated conversion to the active catechol is slower comparedwith etoposide. Elimination occurs primarily in the urine witha terminal elimination half-life of 5 hours.
Clinical Use
Teniposide is used in combination with other agents for the treatment of refractory childhood acute lymphoblastic leukemia.
Sicherheitsprofil
Poison by
intraperitoneal and subcutaneous routes. An
experimental teratogen. Human systemic
effects by ingestion and intravenous route:
anorexia, nausea or vomiting, leukopenia,
agranulocytosis and aplastic anemia of the
blood, bone marrow changes, and hair
changes. Experimental reproductive effects.
Human mutation data reported. When
heated to decomposition it emits very toxic fumes of SOx.
Teniposid Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
