Swords R, Giles F
Department of Haematology, University College Hospital Galway, Galway, Ireland.
Hematology. 2007 Jun;12(3):219-27. doi: 10.1080/10245330701406881.
Troxacitabine (Troxatyl; BCH-4556; (-)-2'-deoxy-3'-oxacytadine) is the first synthetic l-nucleoside enantiomer to demonstrate broad spectrum cytotoxic activity. It was obtained by exchanging the sulphur endocyclic atom with oxygen in the structure of lamivudine, following the discovery that this agent had cytotoxic, as well as anti-viral activity. The unique "unnatural" stereochemistry of troxacitabine has produced impressive cytotoxic potency against a wide range of malignancies in the laboratory which led to its selection for clinical development. The initial trials with troxacitabine have established its efficacy in both solid and haematological malignancies, including those resistant to ara-C (cytarabine). This review will consider troxacitabine in terms of its pharmacology, mode of action, pharmacokinetics, tolerability and clinical efficacy.
曲沙他滨（Troxatyl；BCH - 4556；(-)-2'-脱氧-3'-氧杂胞苷）是首个展现出广谱细胞毒性活性的合成左旋核苷对映体。在发现拉米夫定结构中的硫内ocyclic原子被氧取代后，该化合物具有细胞毒性以及抗病毒活性，从而获得了曲沙他滨。曲沙他滨独特的“非天然”立体化学在实验室中对多种恶性肿瘤产生了令人印象深刻的细胞毒性效力，这使其被选用于临床开发。曲沙他滨的初步试验已证实其在实体瘤和血液系统恶性肿瘤中均有效，包括对阿糖胞苷（Ara - C）耐药的肿瘤。本综述将从曲沙他滨的药理学、作用方式、药代动力学、耐受性和临床疗效等方面进行探讨。
