テニポシド 化学特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結晶
用途
DNAトポイソメラーゼIIの阻害剤、抗悪性腫瘍剤
効能
抗悪性腫瘍薬, トポイソメラーゼII阻害薬
化学的特性
White Solid
使用
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.
定義
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.
適応症
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.
一般的な説明
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.
臨床応用
Teniposide is used in combination with other agents for the treatment of refractory childhood acute lymphoblastic leukemia.
安全性プロファイル
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.
テニポシド 上流と下流の製品情報
原材料
準備製品