Irinotecan是一种拓扑异构酶 I (topoisomerase I) 抑制剂，可用于结肠癌和直肠癌的研究。
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Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor by preventing the DNA strand's religation through its binding to the topoisomerase I-DNA complex[1].
体内研究
Administered as Irinotecan (CPT-11, 5 mg/kg) through daily intratumoral injections for five days across two successive weeks in rats, and via continuous intraperitoneal infusion using an osmotic minipump in mice, it notably impedes tumor growth, whereas a dosage of 10 mg/kg exhibits no significant tumor growth inhibition by intraperitoneal injection[1].
Furthermore, Irinotecan (CPT-11, 100-300 mg/kg, i.p.) markedly diminishes tumor growth in HT-29 xenografts within athymic female mice by the 21st day. Combination treatments of Irinotecan (125 mg/kg) with TSP-1 (10 mg/kg per day) and Irinotecan (150 mg/kg) with TSP-1 (20 mg/kg per day) achieve tumor growth inhibition rates of 84% and 89%, respectively, surpassing the efficacy of Irinotecan alone at dosages of 250 and 300 mg/kg[3].
体外研究
As a potent topoisomerase I inhibitor, Irinotecan curtails the proliferation of LoVo and HT-29 cells, presenting IC50 values of 15.8 ± 5.1 and 5.17 ± 1.4 μM, respectively, and similarly induces cleavable complexes in both cell types[2].
Irinotecan also hampers the growth of human umbilical vein endothelial cells (HUVEC), showcasing an IC50 of 1.3 μM[3].
Irinotecan/伊立替康 细胞实验
Cell Line
Concentration
Treated Time
Description
References
RKO cells
2.5 µM
96 hours
Induce cellular senescence and evaluate changes in cell proliferation, migration, and invasion abilities
Mol Cancer. 2024 Apr 4;23(1):70
HCT116 cells
1.5 µM
96 hours
Induce cellular senescence and evaluate changes in cell proliferation, migration, and invasion abilities
Test the sensitivity of PDX tumor tissue slices to irinotecan, results were consistent with patients' clinical responses.
Clin Cancer Res. 2016 Dec 15;22(24):6021-6030.
HT29 cells
3.125 to 100 µM
24 h
Irinotecan (CPT-11) as the positive control significantly inhibited the proliferation of HT29 cells, with a GI50 of 5.19 µM.
Biomolecules. 2019 Aug 27;9(9):418.
HT29-dx cells
1 µM
24 h
The anti-tumor effect of irinotecan on chemotherapy-resistant HT29-dx cells was studied. The results showed that irinotecan could reduce the IC50 value of drug-resistant cells and restore its anti-tumor effect
Mol Cancer. 2013 Nov 13;12:137.
HT-29 human colorectal cancer cells
20 µM
1.5 h
To investigate the effects of irinotecan alone or in combination with 5-FU on the growth, metabolic activity, and proliferation of HT-29 cells. The results showed that irinotecan alone or in combination with 5-FU significantly inhibited the growth, metabolic activity, and proliferation of HT-29 cells.
Int J Mol Sci. 2023 Jun 20;24(12):10385.
TFK-1 cells
20 µg/ml
72 h
Irinotecan treatment significantly reduced cell viability, increased cytotoxicity, and induced the expression of inflammation-related genes in TFK-1 cells.
Sci Rep. 2019 Mar 13;9(1):4338.
EGI-1 cells
20 µg/ml
72 h
Irinotecan treatment significantly reduced cell viability, increased cytotoxicity, and induced the expression of inflammation-related genes in EGI-1 cells.
To study the role of eIF3a in irinotecan sensitivity in vivo, it was found that eIF3a downregulation increased resistance to irinotecan.
Cell Prolif. 2022 Apr;55(4):e13208
Mice
FLC PDX models
Intraperitoneal injection
5 mg/kg
Irinotecan: 5 days a week for 2 weeks; DT2216: Once or twice a week for 3 weeks
To evaluate the synergistic effect of Irinotecan and DT2216 in FLC PDX models, results showed that Irinotecan and DT2216 have remarkable synergy in vivo at clinically achievable doses not associated with significant thrombocytopenia
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