クラドリビン 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
効能
抗悪性腫瘍薬, 代謝拮抗薬
商品名
ロイスタチン (ヤンセンファーマ)
説明
Cladribine, an adenosine deaminase inhibitor, was introduced in the United States as a
single intravenous treatment for hairy cell leukemia. The incorporation of a chlorine atom at
the 2-position of deoxyadenosine renders cladribine more resistant to enzymatic attack by
adenosine deaminase, resulting in a more prolonged cytotoxic effect. Cladribine efficiently
crosses lymphocyte and monocyte cell membranes and is metabolized in cells to the
biologically active triphosphate, which inhibits DNA synthesis. While most antineoplastic
drugs are active primarily against dividing cells, cladribine destroys both resting and
proliferating cells. Its potential uses in the treatment of autoimmune hemolytic anemia,
multiple sclerosis, chronic lymphocytic leukemia and various lymphomas have also been
evaluated.
化学的特性
White Crystalline Solid
使用
It is a substituted purine nucleoside with antileukemic activity
定義
ChEBI: 2'-Deoxyadenosine in which the hydrogen at position 2 on the purine ring has been substituted by chlorine. It inhibits the synthesis and repair of DNA, particularly in lymphocytes and monocytes, and is used as an antimetabolite antineoplastic drug for the
treatment of lymphoid malignancies including hairy-cell leukaemia and chronic lymphocytic leukaemia.
適応症
Cladribine (Leustatin) is a synthetic purine nucleoside
that is converted to an active cytotoxic metabolite by
the enzyme deoxycytidine kinase. Like the other purine
antimetabolites, it is relatively selective for both normal
and malignant lymphoid cells and kills resting as well as
dividing cells by mechanisms that are not completely
understood.
The drug is highly active against hairy cell leukemia,
producing complete remissions in more than 60% of patients
treated with a single 7-day course. Activity has
also been noted in other low-grade lymphoid malignancies.
The major side effect is myelosuppression.
一般的な説明
The drug is available in a 10-mg or 10-mL single-use vialfor IV use. Cladribine is used for chronic lymphocyticleukemia, hairy cell leukemia, and non-Hodgkin’s lymphoma.The mechanism of action of this purine deoxyadenosineanalog involves incorporation into DNA resultingin inhibition of DNA chain extension and inhibitionof DNA synthesis and function. This incorporation intoDNA occurs via the triphosphate metabolite active species.The 2-chloro group on the adenine ring produces resistanceto breakdown by adenosine deaminase. Resistance to the anticancereffects can occur because of decreased expressionof the activating enzyme or overexpression of the catabolicenzymes. Oral bioavailability is variable and averages about50%. The drug crosses the blood-brain barrier; however,CSF concentrations reach only 25% of those in plasma. Thedrug is selectively activated inside the cell, and intracellularconcentrations of phosphorylated metabolites exceed thosein plasma. Toxicities include myelosuppression, neutropenia,immunosuppression, fever, nausea, and vomiting.
クラドリビン 上流と下流の製品情報
原材料
準備製品