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外観
黄赤色～赤褐色, 結晶性粉末～粉末
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溶解性
水及びメタノールにやや溶けやすく、エタノール(95)に溶けにくく、アセトニトリルにほとんど溶けない。
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用途
アントラサイクリン系抗生物
質です。がん細胞の DNA と結合し、DNA ポ
リメラーゼ、RNA ポリメラーゼ反応を阻害す
ることにより核酸の生合成を阻害し、細胞分
裂抑制作用を示します。
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用途
アントラサイクリン系抗生物
質です。ドキソルビシン塩酸塩の 4' 位 OH 基
が反転した立体異性体です。DNA ポリメラー
ゼ、RNA ポリメラーゼ反応を阻害することに
より核酸の生合成を阻害し、細胞分裂を抑制
します。
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効能
抗悪性腫瘍薬, トポイソメラーゼII阻害薬
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商品名
ファルモルビシン (ファイザー); ファルモルビシン (ファイザー)
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説明
Epirubicin hydrochloride is an antitumor antibiotic which is epimeric with
doxorubicin a t the 4’-position of the amino sugar moiety. It has shown utility in
the treatment of mammary, gastric, colorectal, pulmonary and ovarian carcinomas,
as well as malignant lymphoma and melanoma and soft tissue sarcoma. It is
reported to be less sardiotoxic than doxorubicin.
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化学的特性
Orange-Red Crystalline Solid
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使用
Used as an antineoplastic
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生物学の機能
This stereoisomer of doxorubicin has the 4′-hydroxy group of the daunosamine sugar oriented in the β-position . Epirubicin will be slowly reduced to the active C13 alcohol (epirubicinol), giving it a 30- to 38-hour half life, which is similar to that of doxorubicin. Unlike doxorubicinol, however, which was equally active with doxorubicin, epirubicinol has only one-tenth the activity of its parent drug and is not believed to contribute significantly to the therapeutic action of this agent.
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生物活性
Antibiotic antitumor agent. Inhibits the synthesis and function of DNA (IC 50 = 62.7 μ M in rat glioblastoma cell lines) and inhibits the relaxing property of topoisomerase II.
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臨床応用
Epirubicin is indicated for use in breast cancer, and the starting dose is 100 to 120 mg/m2 (compared to a starting dose of 60–75 mg/m2 for doxorubicin).
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副作用
The side effects and precautions are as outlined previously for doxorubicin, although there is a lower risk of serious myocardial toxicity or myelotoxicity.
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代謝
Cleavage of the epimerized sugar will occur before excretion, generating an aglycone that is indistinguishable from that generated by doxorubicin. Although excretion is primarily biliary, dosage reduction in severe renal impairment, as well as in hepatic dysfunction, is warranted.
