Tsukagoshi S
Cancer Chemotherapy Center, Japanese Foundation Cancer Research.
Gan To Kagaku Ryoho. 1993 Sep;20(12):1877-83.
Cytarabine ocfosfate (commercial name: Starasid) is a prodrug having stearyl group attached to phosphoric acid at 5' position of arabinose moiety of cytosine arabinoside (Ara-C). This drug is given orally. The mode of action is in the inhibition of DNA synthesis after conversion to Ara-CTP as in Ara-C. The drug is metabolized in the liver, producing the intermediate metabolite, C-C3PCA which is converted to Ara-C gradually. This property results in the maintenance of relatively long time the blood Ara-C levels. This was proved to be active clinically against acute leukemia and MDS.
阿糖胞苷十八烷磷酸酯(商品名:Starasid)是一种前体药物,在阿糖胞苷(Ara-C)阿拉伯糖部分的5'位磷酸上连接有硬脂基。该药物通过口服给药。其作用方式是在转化为Ara-CTP后抑制DNA合成,与Ara-C的作用方式相同。该药物在肝脏中代谢,产生中间代谢产物C-C3PCA,后者逐渐转化为Ara-C。这一特性使得血液中的Ara-C水平能够在较长时间内维持。临床证明,该药物对急性白血病和骨髓增生异常综合征有效。