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Irinotecan

伊立替康

Mechanism of action:

Irinotecan 是一種喜樹鹼類（camptothecin）衍生物。Irinotecan 進入體內後，由羧酸酯酶（carboxylesterase）代謝為 SN-38。SN-38 能抑制 DNA 拓撲異構酶 I（topoisomerase I）的活性。正常情況下，拓撲異構酶 I 會在 DNA 複製過程中暫時切斷單股 DNA 以釋放張力，之後再進行重接。SN-38 會穩定 DNA-拓撲異構酶 I 切割的複合體，阻止被切斷的 DNA 單股重新接合，誘發細胞的 DNA 損傷與凋亡。

​Reference(s):

1. Ramesh M et al. (2010). Irinotecan and its active metabolite, SN-38: review of bioanalytical methods and recent update from clinical pharmacology perspectives. Biomed Chromatogr. 


2. Chabot GG et al. (1997). Clinical pharmacokinetics of irinotecan. Clin Pharmacokinet. 


3. Rothenberg ML et al. (2001). Irinotecan (CPT-11): recent developments and future directions—colorectal cancer and beyond. Oncologist.

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