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Gemcitabine

吉西他濱
Mechanism of action:
Gemcitabine 是一種去氧胞苷核苷(deoxycytidine nucleoside)類似物。Gemcitabine 進入細胞後,先由去氧胞苷激酶(deoxycytidine kinase)磷酸化為 gemcitabine monophosphate(dFdCMP),再轉化為 dFdCDP 與 dFdCTP。dFdCDP 可抑制核苷酸還原酶(ribonucleotide reductase),降低去氧核苷酸(dNTP)的生成;dFdCTP 會與 dCTP 競爭,被摻入正在合成的 DNA 中,最後 DNA 複製受阻與損傷累積,啟動細胞週期停滯與凋亡路徑。
Reference(s):
1. Noble S et al. (1997). Gemcitabine. A review of its pharmacology and clinical potential in non-small cell lung cancer and pancreatic cancer. Drugs.
2. Toschi L et al. (2005). Role of gemcitabine in cancer therapy. Future Oncol.
3. Ciccolini J et al. (2016). Pharmacokinetics and pharmacogenetics of gemcitabine as a mainstay in adult and pediatric oncology: an EORTC-PAMM perspective. Cancer Chemother Pharmacol.
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