Combination of SN-38 with gefitinib or imatinib overcomes SN-38-resistant small-cell lung cancer cells

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Combination of SN-38 with gefitinib or imatinib overcomes SN-38-resistant small-cell lung cancer cells.

Irinotecan is one of the effective anticancer agents for small-cell lung cancer (SCLC) and 7-ethyl-10-hydroxy-campthothecin (SN-38) is an active metabolite of irinotecan. Gefitinib and imatinib are tyrosine kinase inhibitors which have clinical activities in several malignancies and they are also potent inhibitors of breast cancer resistance protein (BCRP) transporter, which confers the resista...

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SN-38 overcomes chemoresistance of colorectal cancer cells induced by hypoxia, through HIF1alpha.

BACKGROUND Cancer cells can acquire resistance to therapy under hypoxic condition. We aimed to investigate the mechanisms regulating chemoresistance induced by hypoxia. MATERIALS AND METHODS Human colorectal cancer cells, HT-29 and SW480, were cultured under hypoxic conditions and the sensitivity to 5-fluorouracil (FU), oxaliplatin, and SN-38 (active metabolite of irinotecan) was tested. The ...

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Investigation into the Efficacy of Val-SN-38, a Valine-Ester Prodrug of the Anti-Cancer Agent SN-38

We recently reported that Val-SN-38, a novel valine ester prodrug of SN-38, had greatly improved the intracellular accumulation of SN-38 in MCF-7 cell line, probably through enhanced uptake via amino acid transporters. In the present study, the efficacy of Val-SN-38 was further investigated both in vitro and in vivo. It was found that the in vitro cytotoxic effect of Val-SN-38 was similar to th...

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Preclinical Study on Enhancing Sacituzumab Govitecan (immu-132) Activity in Sn-38-resistant Cancer Cells Published

Morris Plains, NJ, August 18, 2016 --Immunomedics, Inc. (Nasdaq: IMMU) today announced that adding an inhibitor of ATP-binding cassette (ABC) transporters to sacituzumab govitecan, the Company’s lead antibody-drug conjugate (ADC) for solid cancer therapy, increased the median survival of mice bearing a SN-38-resistant human gastric cancer cell line. Results from this preclinical study were publ...

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Synthesis and biodistribution of [C]SN-38

SN-38 (7-ethyl-10-hydroxy camptothecin) is a topoisomerase I inhibitor that is the active chemotherapeutic agent of irinotecan, indicated for colon cancer. Because the rate of response to irinotecan treatment is low, it is of interest to have a prognostic indicator to identify and more selectively treat those who are likely to respond to treatment. We have therefore prepared SN-38 labeled with ...

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ژورنال

عنوان ژورنال: Oncology Reports

سال: 2007

ISSN: 1021-335X,1791-2431

DOI: 10.3892/or.17.5.983