イダルビシン·塩酸塩 化学特性,用途語,生産方法
外観
赤黄色～黄赤色, 結晶性粉末～粉末
溶解性
メタノールにやや溶けにくく、水及びエタノール(95)に溶けにくく、アセトニトリル又はジエチルエーテルにほとんど溶けない。
用途
アントラサイクリン系抗生物
質です。DNA 合成阻害作用を示します。
効能
抗悪性腫瘍薬, トポイソメラーゼII阻害薬
商品名
イダマイシン (ファイザー)
説明
Idarubicin hydrochloride is a derivative of daunorubicin indicated for acute nonlymphocytic
leukemia, acute lymphocytic leukemia, and acute myeloid leukemia.
Compared with daunorubicin, idarubicin hydrochloride is less cardiotoxic, has milder
side effects, is orally active and more potent in experimental leukemias. Idarubicin
hydrochloride is also reportedly active in daunorubicin-resistant patients, breast cancer,Hodgkin's and non-Hodgkin's lymphoma.
化学的特性
Orange Solid
使用
Idarubicin hydrochloride (Idamycin) is used to traet acute myeloid leukemia in adults.
一般的な説明
Idarubicin is available in 5-, 10-, and 20-mL vials for IV administrationin the treatment of acute myeloid leukemia andacute nonlymphocytic leukemia. The compound lacks the4-methoxy group and terminal side-chain alcohol of doxorubicinmaking it the most lipophilic of the four major anthracyclines(doxorubicin, daunorubicin, epirubicin, idarubicin),and it is considered less cardiotoxic than doxorubicin. Theremoval of the 4-methoxy group also increases inhibition oftopoisomerase II. The drug has a fast distributive phase anda high volume of distribution reflecting binding to tissue.Concentrations in blood and bone marrow cells are 100 timeshigher than those found in plasma, reflecting its use in treatingleukemias. Metabolism of the agent primarily occurs byconversion to idarubicinol via reduction of the side chain ketoneto the alcohol, which retains activity as an antineoplastic.Elimination occurs primarily in the bile. Adverse effectsare similar to those found for doxorubicin; however, there isa lower incidence of cardiotoxicity.
作用機序
Increased rates of remission have been noted with the use of idarubicin compared to other anthracyclines antineoplastic agents. Unlike its congeners, idarubicin shows significant oral bioavailability and is lipophilic enough to penetrate the blood-brain barrier. Currently, however, it is given only by the IV route and is not used in the treatment of brain cancer.
臨床応用
Its primary indication is in acute myeloid leukemia, and it is
administered in combination with other antileukemic drug.
副作用
Common adverse reactions to Idarubicin hydrochloride may include nausea and vomiting, mucositis, and some patients may experience serious adverse reactions including transient elevation of hepatic aminotransferases and total bilirubin, alopecia, transient rash, urticaria at the site of injection, and skin toxicity
[1].
安全性プロファイル
A poison by ingestion,
subcutaneous, intravenous, and
intraperitoneal routes. When heated to
decomposition it emits toxic vapors of NOx,
HCl, and Cl-.
代謝
Idarubicin is reduced by aldoketoreductases to idarubicinol, which is as active as the parent drug. Because there is no aromatic methoxy group, there is no O-dealkylation to the C4-phenol. The major metabolite is free, unconjugated idarubicinol. The half-lives of both idarubicin and idarubicinol are 22 and 45 hours, respectively. Idarubicin is administered IV at a dose of 10 to 12 mg/m2 /day for 3 to 4 days, and the idarubicinol metabolite can still be found in therapeutic concentrations in the blood 8 days after administration. Like other anthracyclines, excretion primarily is fecal, with a lesser dependence on renal elimination.
イダルビシン·塩酸塩 上流と下流の製品情報
原材料
5,12-Naphthacenedione, 9-acetyl-7,8,9,10-tetrahydro-6,9,11-trihydroxy-7-[[2,3,6-trideoxy-3-[(2,2,2-trifluoroacetyl)amino]-α-L-lyxo-hexopyranosyl]oxy]-, (7S,9S)-
イダルビシン
準備製品