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1

Ando, Koji, Yuho Ebata, Eiji Oki, Tomoharu Yoshizumi, and Ajit Bharti. "Development of new therapeutic strategies to enhance the effectiveness of irinotecan in colorectal cancer treatment." Journal of Clinical Oncology 43, no. 4_suppl (2025): 217. https://doi.org/10.1200/jco.2025.43.4_suppl.217.

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217 Background: Chemotherapy plays an important role in the treatment of colorectal cancer. Irinotecan, a topoisomerase I inhibitor, is used in therapies such as FOLFIRI and FOLFOXIRI. However, many patients become resistant to irinotecan, and the detailed mechanisms of resistance are not fully understood. The aim is to develop new therapeutic strategies by elucidating the mechanisms of irinotecan resistance. Methods: We used in vitro approach to demonstrate the mechanism of topoI degradation. Immunohistochemistry staining was used to explore the biomarker for irinotecan, Finally, in vivo appr
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2

Aoki, Masahiko, Hirokazu Shoji, Hiroshi Imazeki, et al. "The hyperprogressive disease during nivolumab treatment or irinotecan treatment in patients with advanced gastric cancer." Journal of Clinical Oncology 37, no. 4_suppl (2019): 124. http://dx.doi.org/10.1200/jco.2019.37.4_suppl.124.

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124 Background: Nivolumab has demonstrated a survival benefit as a single agent in patients with advanced gastric cancer (AGC) refractory to, or intolerant of, two or more previous regimens in phase III study (ATTRACTION-2). However, an acceleration of tumor growth during immunotherapy, (hyperprogressive disease: HPD), was reported in advanced cancers treated with immunotherapy. The frequency and outcome of HPD in AGC comparing between immunotherapy and cytotoxic agents are little known. The aim of this study was to clarify the prevalence and background of HPD in patients treated with nivoluma
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Falcone, Alfredo, Antonello Di Paolo, Gianluca Masi, et al. "Sequence Effect of Irinotecan and Fluorouracil Treatment on Pharmacokinetics and Toxicity in Chemotherapy-Naive Metastatic Colorectal Cancer Patients." Journal of Clinical Oncology 19, no. 15 (2001): 3456–62. http://dx.doi.org/10.1200/jco.2001.19.15.3456.

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PURPOSE: To investigate the sequence effect of irinotecan and a 48-hour infusion of fluorouracil (5-FU) modulated by leucovorin (LV) on the plasma pharmacokinetics of irinotecan and its metabolites, the toxicity profile of this combination, and irinotecan’s maximum-tolerated dose (MTD). PATIENTS AND METHODS: Thirty-three metastatic colorectal cancer patients were randomized to receive a 60-minute infusion of irinotecan before or after a 48-hour infusion of 5-FU modulated by LV. The reverse sequence was used after 21 days for the second cycle. 5-FU 3,500 mg/m2 was preceded by l-LV 250 mg/m2. Ir
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4

Ahire, Eknath D., and Sanjay J. Kshirsagar. "Irinotecan's molecular mechanisms against cancer: a primary system biology and chemoinformatics approach for novel formulation development." Current Issues in Pharmacy and Medical Sciences 38, no. 1 (2025): 31–37. https://doi.org/10.12923/cipms-2025-0005.

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Cancer is the third most common type of cancer generally. It affects 6.1% of the entire world’s population and kills 9.2% of all people of both sexes. Even though people with colon cancer have a number of chemotherapies and surgeries to choose from, the disease often returns after the first treatment. AutoDockVina by PyRx 0.8v was used to do molecular docking. The admetSAR2.0 web server was employed for ADMET analysis. The MolSoft and ADVERPred tools were applied to predict the drug's potential for abuse and its potential for side effects. The anti-tumor effects of irinotecan may be aimed at t
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5

Vanhoefer, Udo, Andreas Harstrick, Wolf Achterrath, Shousong Cao, Siegfried Seeber, and Youcef M. Rustum. "Irinotecan in the Treatment of Colorectal Cancer: Clinical Overview." Journal of Clinical Oncology 19, no. 5 (2001): 1501–18. http://dx.doi.org/10.1200/jco.2001.19.5.1501.

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PURPOSE AND METHODS: For more than three decades, the therapeutic options for patients with advanced colorectal cancer have almost exclusively been based on fluoropyrimidines. With the recognition that topoisomerase-I (TOP-I) is an important therapeutic target in cancer therapy, irinotecan, a semisynthetic TOP-I–interactive camptothecin derivative, has been clinically established in the treatment of colorectal cancer. RESULTS: Irinotecan was investigated as second-line chemotherapy after prior treatment with fluorouracil (FU)-based regimens in two large randomized phase III trials comparing ir
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Ali, Selda, Denisa-Mihaela Nedelcu, Radu Serescu, and Roxana Silvia Bumbăcea. "Successful Desensitization to Irinotecan in a Patient with Metastatic Esophageal Squamous Cell Carcinoma and a History of Anaphylaxis in Response to Irinotecan—Case Report and Literature Review." Journal of Clinical Medicine 13, no. 24 (2024): 7824. https://doi.org/10.3390/jcm13247824.

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Background: Irinotecan is a topoisomerase I inhibitor used for the treatment of various cancers, such as gastrointestinal, pancreatic, pulmonary, ovarian, and cervical cancers. Among chemotherapy agents, it represents a rare trigger of drug hypersensitivity reactions, with few cases being reported until today. Methods: We present the case of a patient with metastatic esophageal cancer and a history of irinotecan-induced grade IV (WAO classification) anaphylaxis. An IgE-mediated reaction was confirmed in our case, as evidenced by a positive intradermal skin test result, and we carried out a suc
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Ghodeswar, Bindu, and Santosh Chhajed. "Irinotecan Resistance Mechanisms in Cancer: Challenges and Opportunities." INTERNATIONAL JOURNAL OF DRUG DELIVERY TECHNOLOGY 14, no. 02 (2024): 1099–105. http://dx.doi.org/10.25258/ijddt.14.2.74.

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Irinotecan, a topoisomerase I inhibitor, has been widely used in the treatment of various solid tumors, including colorectal, lung, and pancreatic cancers. However, its efficacy is often limited by the development of resistance mechanisms within cancer cells. Understanding these resistance mechanisms is crucial for improving treatment outcomes and developing effective therapeutic strategies. This review article provides a comprehensive overview of the mechanisms underlying irinotecan resistance in cancer. Key resistance mechanisms discussed include the overexpression of drug efflux pumps, acti
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8

Radajewska, Anna, Helena Moreira, Dorota Bęben, et al. "Combination of Irinotecan and Melatonin with the Natural Compounds Wogonin and Celastrol for Colon Cancer Treatment." International Journal of Molecular Sciences 24, no. 11 (2023): 9544. http://dx.doi.org/10.3390/ijms24119544.

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Colorectal cancers are one of the leading cancers worldwide and are known for their high potential for metastasis and resistance to therapy. The aim of this study was to investigate the effect of various combination therapies of irinotecan with melatonin, wogonin, and celastrol on drug-sensitive colon cancer cells (LOVO cell line) and doxorubicin-resistant colon cancer stem-like cells (LOVO/DX cell subline). Melatonin is a hormone synthesized in the pineal gland and is responsible for circadian rhythm. Wogonin and celastrol are natural compounds previously used in traditional Chinese medicine.
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9

Kockaya, Guvenc, Mine Polat, Albert Wertheimer, et al. "Treatment cost of metastatic colon cancer in Turkey." Farmeconomia. Health economics and therapeutic pathways 14, no. 1 (2013): 19–25. http://dx.doi.org/10.7175/fe.v14i1.472.

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OBJECTIVES: Colon cancer is the third most common in the top cancer incidence list in Europe. In Europe 212,000 patients die every year due to colon cancer. In Turkey 120,000-130,000 new cancer patients are diagnosed every year, 7.1% of whom are diagnosed to have developed colon cancer. Metastases will occur in up to 50% of the patients who are newly diagnosed. Survival appears to be further prolonged to more than 20 months with new pharmaceuticals; however, these new pharmaceuticals increase the total cost of care. The aim of this study is to estimate the cost implications of new colon cancer
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10

Aoki, Masahiko, Hirokazu Shoji, Kengo Nagashima, et al. "Hyperprogressive disease during nivolumab or irinotecan treatment in patients with advanced gastric cancer." ESMO Open 4, no. 3 (2019): e000488. http://dx.doi.org/10.1136/esmoopen-2019-000488.

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BackgroundNivolumab showed a survival benefit for advanced gastric cancer (AGC). However, an acceleration of tumour growth during immunotherapy, (hyperprogressive disease, HPD) has been reported in various cancers. This study reviewed the HPD in patients with AGC treated with nivolumab or irinotecan.MethodsThe subjects of this retrospective study were patients with AGC with measurable lesions, and their tumour growth rates (TGR) during nivolumab or irinotecan were compared with those during prior therapy. HPD was defined as an increase in TGR more than twofold.Results34 and 66 patients receive
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11

Kciuk, Mateusz, Beata Marciniak, and Renata Kontek. "Irinotecan—Still an Important Player in Cancer Chemotherapy: A Comprehensive Overview." International Journal of Molecular Sciences 21, no. 14 (2020): 4919. http://dx.doi.org/10.3390/ijms21144919.

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Irinotecan has been used in the treatment of various malignancies for many years. Still, the knowledge regarding this drug is expanding. The pharmacogenetics of the drug is the crucial component of response to irinotecan. Furthermore, new formulations of the drug are introduced in order to better deliver the drug and avoid potentially life-threatening side effects. Here, we give a comprehensive overview on irinotecan’s molecular mode of action, metabolism, pharmacogenetics, and toxicity. Moreover, this article features clinically used combinations of the drug with other anticancer agents and i
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12

Bailly, Christian. "Irinotecan: 25 years of cancer treatment." Pharmacological Research 148 (October 2019): 104398. http://dx.doi.org/10.1016/j.phrs.2019.104398.

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13

Sagawa, Tamotsu, Hironaga Satake, Koshi Fujikawa, et al. "Phase Ib study of ramucirumab and irinotecan for metastatic gastric cancer previously treated with fluoropyrimidine with/without platina and taxane." Journal of Clinical Oncology 36, no. 4_suppl (2018): 155. http://dx.doi.org/10.1200/jco.2018.36.4_suppl.155.

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155 Background: Optimal salvage line chemotherapy for previously heavily treated advanced/ metastatic gastric cancer (AGC) is unknown, but treated with irinotecan in Japan. Ramucirumab, a human IgG-1 monoclonal antibody that targets the extracellular domain of VEGF receptor 2, is the first molecularly targeted agent proven to be effective in second-line therapy for AGC in combination with chemotherapy. Furthermore, combination chemotherapy with ramucirumab and irinotecan based regimen (FOLFIRI) is recognized as one of the promising regimens for metastatic colorectal cancer. To date, however, u
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14

Shun, Yu-Ting, Hsien-Yung Lai, Yi-Ting Chuang, and Hsuen-Fu Lin. "Successful Treatment of Irinotecan-Induced Muscle Twitching: A Case Report." Clinical Medicine Insights: Case Reports 16 (January 2023): 117954762211503. http://dx.doi.org/10.1177/11795476221150354.

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Irinotecan, a topoisomerase I inhibitor, is commonly used in the treatment of advanced colorectal cancer. Its adverse effects include delay diarrhea, severe myelosuppression, and cholinergic-like symptoms. Though 2 cases of irinotecan-induced muscle twitching were reported but the successful treatment of this adverse event still not shown. We present a 24-year-old female patient with advanced colorectal cancer received bevacizumab and FOLFIRI (irinotecan + calcium leucovorin + 5-fluorouracil) treatment. Her right pectoralis major muscle presented with involuntary muscle twitching during the in
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15

Zeng, Chao, Hang Zhou, Yang Wei, Liyang Wang, Hua Xie, and Wenxiu Yao. "Chemotherapy with or without irinotecan in patients with advanced or recurrent gastric cancer: a meta-analysis of randomized controlled trials." Chinese Medical Journal 127, no. 5 (2014): 951–56. http://dx.doi.org/10.3760/cma.j.issn.0366-6999.20131490.

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Background Studies have shown that irinotecan can improve survival in patients with advanced or recurrent gastric cancer, but the overall benefit of irinotecan in the treatment of advanced or recurrent gastric cancer remains controversial. The aim of this study was to evaluate the benefits and risks of irinotecan for survival in patients with advanced or recurrent gastric cancer. Method We searched PubMed, EmBase, the Cochrane Central Register of Controlled Trials, reference lists of articles, and proceedings of major conferences for relevant clinical trials. We included randomized controlled
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16

Hulshof, Emma C., Mirjam de With, Femke M. de Man, et al. "Safety and pharmacokinetic analysis of UGT1A1 genotype-guided dosing of irinotecan." Journal of Clinical Oncology 39, no. 15_suppl (2021): 3574. http://dx.doi.org/10.1200/jco.2021.39.15_suppl.3574.

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3574 Background: Irinotecan is commonly used in the treatment of advanced colorectal and pancreatic cancer. The polymorphisms UGT1A1*28 (7 TA repeats) and UGT1A1*93 (SNP -3156G > A) are significantly associated with increased systemic exposure of irinotecan’s active metabolite SN-38 and subsequently severe irinotecan-associated adverse-events (AEs) including (febrile) neutropenia and diarrhea. Severe AEs may lead to hospitalization, loss of quality of life, treatment delay and/or treatment discontinuation. Nonetheless, prospective genetic screening is not yet routinely performed. The aim of
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Jahan, Zeenat, Fahad A. Benthani, Nicola Currey, et al. "MCC Gene Silencing Is a CpG Island Methylator Phenotype-Associated Factor That Predisposes Colon Cancer Cells to Irinotecan and Olaparib." Cancers 14, no. 12 (2022): 2859. http://dx.doi.org/10.3390/cancers14122859.

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Chemotherapy is a mainstay of colorectal cancer treatment, and often involves a combination drug regime. CpG island methylator phenotype (CIMP)-positive tumors are potentially more responsive to the topoisomerase-inhibitor irinotecan. The mechanistic basis of the increased sensitivity of CIMP cancers to irinotecan is poorly understood. Mutated in Colorectal Cancer (MCC) is emerging as a multifunctional tumor suppressor gene in colorectal and liver cancers, and has been implicated in drug responsiveness. Here, we found that CIMP tumors undergo MCC loss almost exclusively via promoter hypermethy
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18

Wang, Wenjie, Monica Rodriguez-Silva, Arlet M. Acanda de la Rocha, et al. "Tyrosyl-DNA Phosphodiesterase 1 and Topoisomerase I Activities as Predictive Indicators for Glioblastoma Susceptibility to Genotoxic Agents." Cancers 11, no. 10 (2019): 1416. http://dx.doi.org/10.3390/cancers11101416.

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Glioblastoma (GBM) patients have an estimated survival of ~15 months with treatment, and the standard of care only modestly enhances patient survival. Identifying biomarkers representing vulnerabilities may allow for the selection of efficacious chemotherapy options to address personalized variations in GBM tumors. Irinotecan targets topoisomerase I (TOP1) by forming a ternary DNA–TOP1 cleavage complex (TOP1cc), inducing apoptosis. Tyrosyl-DNA phosphodiesterase 1 (TDP1) is a crucial repair enzyme that may reduce the effectiveness of irinotecan. We treated GBM cell lines with increasing concent
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Sobrero, Alberto F., Joan Maurel, Louis Fehrenbacher, et al. "EPIC: Phase III Trial of Cetuximab Plus Irinotecan After Fluoropyrimidine and Oxaliplatin Failure in Patients With Metastatic Colorectal Cancer." Journal of Clinical Oncology 26, no. 14 (2008): 2311–19. http://dx.doi.org/10.1200/jco.2007.13.1193.

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PurposeTo determine whether adding cetuximab to irinotecan prolongs survival in patients with metastatic colorectal cancer (mCRC) previously treated with fluoropyrimidine and oxaliplatin.Patients and MethodsThis multicenter, open-label, phase III study randomly assigned 1,298 patients with epidermal growth factor receptor–expressing mCRC who had experienced first-line fluoropyrimidine and oxaliplatin treatment failure to cetuximab (400 mg/m2day 1 followed by 250 mg/m2weekly) plus irinotecan (350 mg/m2every 3 weeks) or irinotecan alone. Primary end point was overall survival (OS); secondary end
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Kim, Seong-Ryong, Hyun Jung Lee, and Dalyong Kim. "Consistent Response on Challenge and Rechallenge of Liposomal Irinotecan in a Patient with Metastatic Pancreatic Adenocarcinoma Previously Treated with Gemcitabine plus Nab-Paclitaxel: A Case Report." Case Reports in Oncology 14, no. 3 (2021): 1882–88. http://dx.doi.org/10.1159/000521315.

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Approximately 80% of pancreatic cancer is diagnosed at an advanced stage, due to lack of or vague symptoms when the cancer is still localized, leading to a high mortality rate. Known risk factors for developing pancreatic cancer are family history, obesity, type 2 diabetes, and alcohol and tobacco use. There has been a remarkable development in diagnosis modalities and molecular testing, but early detection is still infrequent. The majority of clinical trials have not shown significant efficacy in pancreatic cancer, and treatment strategy remains limited. Additional prognostic factors should b
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Hironaka, Shuichi, Shinya Ueda, Hirofumi Yasui, et al. "Randomized, Open-Label, Phase III Study Comparing Irinotecan With Paclitaxel in Patients With Advanced Gastric Cancer Without Severe Peritoneal Metastasis After Failure of Prior Combination Chemotherapy Using Fluoropyrimidine Plus Platinum: WJOG 4007 Trial." Journal of Clinical Oncology 31, no. 35 (2013): 4438–44. http://dx.doi.org/10.1200/jco.2012.48.5805.

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Purpose This phase III study compared treatment with weekly paclitaxel and biweekly irinotecan in patients with advanced gastric cancer refractory to treatment with fluoropyrimidine plus platinum. Patients and Methods Patients were randomly assigned to receive either paclitaxel (80 mg/m2 on days 1, 8, and 15, every 4 weeks) or irinotecan (150 mg/m2 on days 1 and 15, every 4 weeks). Primary end point was overall survival (OS), and secondary end points were progression-free survival (PFS), response rate, adverse events, and proportion of patients who received third-line chemotherapy. Results Of
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Giuliani, F., and G. Colucci. "Cetuximab in Colon Cancer." International Journal of Biological Markers 22, no. 1_suppl4 (2007): 62–70. http://dx.doi.org/10.1177/17246008070221s408.

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In the last decade remarkable progress has been made in the treatment of metastatic colorectal cancer due to the introduction of oxaliplatin and irinotecan in clinical practice. The addition of biological agents seems to offer a chance to further enhance the activity of conventional chemotherapy. Cetuximab, a chimeric mouse-human monoclonal antibody targeting the extracellular domain of the epidermal growth factor receptor (EGFR), has shown low but detectable activity when employed in pretreated patients either as a single agent or in combination with irinotecan. Cetuximab in combination with
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Strock, Christopher J., Jong-In Park, D. Marc Rosen, et al. "Activity of Irinotecan and the Tyrosine Kinase Inhibitor CEP-751 in Medullary Thyroid Cancer." Journal of Clinical Endocrinology & Metabolism 91, no. 1 (2006): 79–84. http://dx.doi.org/10.1210/jc.2005-1882.

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Abstract Context: Medullary thyroid cancer (MTC) is a cancer of the parafollicular C cells that commonly presents with an inherited or acquired RET gene mutation. There is currently no effective systemic treatment for MTC. Objective: The objective of this study was to investigate a systemic therapeutic approach to treat MTC. We studied the sensitivity of an MTC cell line and xenograft to irinotecan, alone and in combination with the tyrosine kinase inhibitor, CEP-751. Results: In TT cell culture and xenografts, irinotecan treatment was highly effective. This effect was augmented by treatment w
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O'Reilly, Eileen Mary, Andy Surinach, Allison Dillon, Paul Cockrum, and Kenneth H. Yu. "Impact of prior irinotecan exposure on outcomes of metastatic pancreatic cancer (mPC) patients." Journal of Clinical Oncology 38, no. 4_suppl (2020): 667. http://dx.doi.org/10.1200/jco.2020.38.4_suppl.667.

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667 Background: Published data suggests prior exposure to irinotecan infers a lower likelihood of benefit to liposomal irinotecan. This analysis seeks to expand this hypothesis by evaluating U.S. patterns of care to understand how prior irinotecan therapy impacts outcomes in mPC. Methods: Using the Flatiron Health database, data were extracted and analyzed for treated mPC patients (pts) in the 2L+ setting between Jan 1, 2014 and Jun 30,2019. Therapies of interest included: gemcitabine/ nab-paclitaxel (GnP), FOLFOX, FOLFIRI, FOLFIRINOX (FFX), and liposomal irinotecan/5-FU/LV (nal-IRI). The refe
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Mir, Tanveer Ahmad, Ahmed S. Yassin, Eric Joseph Denha, et al. "Irinotecan inducing sinus pause bradycardia in a patient with small round cell cancer." BMJ Case Reports 13, no. 5 (2020): e232053. http://dx.doi.org/10.1136/bcr-2019-232053.

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Irinotecan is a novel anticancer drug that has worked wonders in combination with other anticancer drugs. It can be used as a single chemotherapy agent in colonic cancer treatment or in combination with 5-fluorouracil. Irinotecan has been found a better salvage therapy in patients who are resistant to 5-fluorouracil. It is also used in combination with cisplatin and other drugs for cancers such as pleural mesothelioma, Ewing’s sarcoma, lung cancer and others, and has helped reduce tumour burden. Irinotecan is generally associated with gastrointestinal side effects including nausea, vomiting an
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Jang, Hyun Joo, Eun Mi Hong, Juah Jang, et al. "Synergistic Effects of Simvastatin and Irinotecan against Colon Cancer Cells with or without Irinotecan Resistance." Gastroenterology Research and Practice 2016 (2016): 1–9. http://dx.doi.org/10.1155/2016/7891374.

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Aims. We here investigated whether the combination of simvastatin and irinotecan could induce the synergistic effect on colon cancer cells with or without resistance to irinotecan.Methods. We investigated cell proliferation assay and assessed cell death detection ELISA and caspase-3 activity assay of various concentrations of simvastatin and irinotecan to evaluate the efficacy of drug combination on colon cancer cells with or without irinotecan resistance.Results. The IC50values of simvastatin alone and irinotecan alone were115.4±0.14 μM (r=0.98) and62.5±0.18 μM (r=0.98) in HT-29 cells without
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Cunningham, Julia Marie, Petra Prins, Brian Conkright, et al. "Molecular profiling of TOPO1: A way to evaluate irinotecan treatment in colorectal cancer?" Journal of Clinical Oncology 34, no. 4_suppl (2016): 546. http://dx.doi.org/10.1200/jco.2016.34.4_suppl.546.

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546 Background: Front-line chemotherapy for metastatic colorectal cancer (mCRC) consists of a fluoropyrimidine backbone plus either oxaliplatin (FOLFOX or XELOX) or irinotecan (FOLFIRI or XELIRI). Large, prospective trials enrolling chemotherapy-naïve patients (pts) show FOLFOX and FOLFIRI treatment to be equivalent with similar response rates. Methods: Irinotecan inhibits TOPO1, which is now a candidate marker for irinotecan treatment benefit. Thus, we retrospectively analyzed TOPO1 expression level in 49 pts with mCRC who were treated with irinotecan-containing regimens at the Lombardi Compr
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Lim, Sung Hee, Jae-Joon Kim, Hyeon-Su Im, et al. "Comparison of efficacy between immune checkpoint inhibitors and irinotecan-based chemotherapy as third-line treatment for patients with advanced gastric cancer: A Korean real-world multicenter study (KCSG ST22-06)." Journal of Clinical Oncology 41, no. 16_suppl (2023): e16047-e16047. http://dx.doi.org/10.1200/jco.2023.41.16_suppl.e16047.

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e16047 Background: Immune checkpoint inhibitor (ICI) or irinotecan-based chemotherapy are frequently used after paclitaxel plus ramucirumab as second-line treatment for patients with recurrent and/or metastatic gastric cancer (RMGC). This study aimed to compare the efficacy between ICI and irinotecan-based chemotherapy as third-line treatment in patients with RMGC. Methods: We retrospectively reviewed patients with RMGC, whose third-line treatment started between July 2019 and June 2021 at 17 centers in South Korea. The ICI group included patients who received nivolumab or pembrolizumab and th
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Bugat, R. "Irinotecan in the treatment of gastric cancer." Annals of Oncology 14 (June 2003): ii37—ii40. http://dx.doi.org/10.1093/annonc/mdg727.

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Wilke, H., O. Bouché, P. Rougier, and C. H. Köhne. "Irinotecan for the treatment of gastric cancer." European Journal of Cancer Supplements 2, no. 7 (2004): 48–51. http://dx.doi.org/10.1016/j.ejcsup.2004.04.015.

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Fuchs, Charles, Edith P. Mitchell, and Paulo M. Hoff. "Irinotecan in the treatment of colorectal cancer." Cancer Treatment Reviews 32, no. 7 (2006): 491–503. http://dx.doi.org/10.1016/j.ctrv.2006.07.001.

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Guo, Weijian, Xiaowei Zhang, Yusheng Wang, et al. "FOLFIRI versus irinotecan monodrug as second-line treatment in metastatic colorectal cancer patients: An open, multicenter, prospective, randomized controlled phase III clinical study." Journal of Clinical Oncology 38, no. 15_suppl (2020): 4038. http://dx.doi.org/10.1200/jco.2020.38.15_suppl.4038.

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4038 Background: The most commonly used treatment methods for metastatic colorectal cancer (mCRC)are systemic chemotherapy, molecular targeted therapy and local treatment. The main chemotherapy drugs for mCRC include Irinotecan, Oxaliplatin and 5-Fu. V308 Research shows that FOLFOX and FOLFIRI can be standard first or second-line of each other in the treatment of metastatic colorectal cancer. However if the first-line treatment regimen containing 5-FU fails, whether it is necessary to re-challenge 5-FU when Irinotecan is applied in the second line is unknown. There is no head-to-head comparati
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Yu, Qianqian, Zhihuan Li, Xiaoqi Nie, et al. "Predictive Value of UGT1A1 Polymorphisms in Irinotecan-Induced Toxicity and Therapeutic Efficacy in Colorectal Cancer Patients." Journal of Cancer Treatment and Diagnosis 4, no. 2 (2020): 39–46. http://dx.doi.org/10.29245/2578-2967/2020/2.1182.

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Irinotecan-based chemotherapy is a fundamental cytotoxic regimen for advanced colorectal cancer. The disposition of irinotecan is known to vary in a fashion partially depending on genetic variations in the drug metabolic pathways. UDP-glucuronosyltransferase (UGT)1A1 is a predominant enzyme that converts the active metabolite of irinotecan to the inactive form via a glucuronidation process. Several UGT1A1 polymorphisms are linked to SN-38 glucuronidation and irinotecan-related adverse events, while the predictive role of UGT1A1 polymorphisms regarding therapeutic outcome is controversial. In t
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Amonkar, Mayur, David Gomez-Ulloa, Smita Kothari, et al. "Real-world treatment patterns and clinical outcomes in patients receiving second-line (2L) treatment for advanced or metastatic gastric cancer (GC)." Journal of Clinical Oncology 37, no. 4_suppl (2019): 102. http://dx.doi.org/10.1200/jco.2019.37.4_suppl.102.

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102 Background: Despite increased survival demonstrated for patients with advanced / metastatic GC due to 2L chemotherapy, different standard of care options exist. This study aims to describe RW treatment patterns and clinical outcomes in patients with advanced / metastatic GC receiving 2L treatment. Methods: Retrospective chart review study conducted in Australia, Canada, Italy and UK. Patients diagnosed with metastatic / unresectable GC receiving 2L treatment between January 2013 and July 2015 were enrolled. Patient characteristics, treatment patterns and clinical outcomes were captured for
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Odeniran, Paul O., Paradise Madlala, Nompumelelo P. Mkhwanazi, and Mahmoud E. S. Soliman. "Camptothecin and Its Derivatives from Traditional Chinese Medicine in Combination with Anticancer Therapy Regimens: A Systematic Review and Meta-Analysis." Cancers 16, no. 22 (2024): 3802. http://dx.doi.org/10.3390/cancers16223802.

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Background/Objectives: Camptothecin (CPT) and its derivatives, irinotecan and topotecan, are integral components of cancer chemotherapy, often used in combination therapies. This meta-analysis evaluates the efficacy of CPT-based combination treatments in cancer patients. Methods: We systematically searched the literature database using the Preferred Reporting Items for Systematic Reviews and Meta-Analyses checklist for articles published between 2000 and 2022. Published studies were retrieved through an electronic search on the Web of Science, PubMed, and Google Scholar databases. A total of 1
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Gonzalez-Baron, M., M. Blanco, J. Feliu, et al. "Cetuximab and irinotecan in patients with colorectal cancer refractory to oxaliplatin and irinotecan." Journal of Clinical Oncology 25, no. 18_suppl (2007): 14600. http://dx.doi.org/10.1200/jco.2007.25.18_suppl.14600.

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14600 Background: Patients with chemotherapy-resistant metastasic colorectal cancer have a poor prognosis with few therapeutic options. The purpose of this work is to evaluate the results of treatment with cetuximab and irinotecan in this group of patients. Methods: Between January 01 and July 06, 24 patients were treated in our centre with cetuximab. 19 patients received irinotecan 180 mg/m2 every two weeks with cetuximab at standard doses: 400 mg/m2 loading dose over 2 hours, then 250 mg/m2 over 1 hour weekly, and 5 patients received FOLFIRI schedule and cetuximab at the same doses as previo
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Almasmoum, Hussain. "Characterization of mucin 2 expression in colorectal cancer with and without chemotherapies, in vivo and in vitro study." Journal of Umm Al-Qura University for Medical Sciences 7, no. 1 (2021): 18–22. http://dx.doi.org/10.54940/ms28179947.

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Background: Colorectal cancer (CRC) is the third and second most prevalent cancer affecting males and females, respectively. 5-fluorouracil (5-FU) and irinotecan are the main chemotherapies for CRC. Down regulation of mucin 2 (MUC2) expression is associated with poor prognosis. Aim: This study examines the expression levels of MUC2 in response to treatment with 5-FU and/or irinotecan in vivo and in vitro. Method: HT29 CRC cells were treated with 5- FU and/or irinotecan, and the expression of MUC2 at mRNA and protein levels was examined by real-time polymerase chain reaction (PCR) and immunohis
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Janjigian, Yelena Yuriy, Laura H. Tang, Stephen Shibata, et al. "A multicenter random assignment phase II study of irinotecan and flavopiridol versus irinotecan alone for patients with p53 wild-type gastric adenocarcinoma (NCI 8060)." Journal of Clinical Oncology 30, no. 15_suppl (2012): e14586-e14586. http://dx.doi.org/10.1200/jco.2012.30.15_suppl.e14586.

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e14586 Background: Preclinical studies demonstrate that tumors wild-type for p53 (p53wt) are refractory to irinotecan relative to non-functional or mutant p53, and that sequential therapy with flavopiridol, a cyclin dependent kinase inhibitor that inhibits homologous recombination and DNA repair, and irinotecan overcomes p53 mediated drug resistance in vivo. This phase II study is designed to assess cell cycle mediated drug resistance in p53wt gastric cancer, and test the hypothesis that administration of flavopiridol following irinotecan can overcome resistance to irinotecan. Methods: Pts wit
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Lal, Rohit, James Dickson, David Cunningham, et al. "A Randomized Trial Comparing Defined-Duration With Continuous Irinotecan Until Disease Progression in Fluoropyrimidine and Thymidylate Synthase Inhibitor—Resistant Advanced Colorectal Cancer." Journal of Clinical Oncology 22, no. 15 (2004): 3023–31. http://dx.doi.org/10.1200/jco.2004.01.005.

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Purpose Irinotecan given until disease progression is an accepted standard treatment for advanced colorectal cancer (CRC) resistant to fluoropyrimidines. It is not known whether a predefined period of irinotecan treatment would result in similar duration of disease control. We performed a multicenter phase III trial to compare the two policies of defined-duration versus continuous irinotecan treatment. Patients and Methods Three hundred thirty-three eligible patients with advanced CRC progressing on or within 24 weeks of completing fluoropyrimidine-based chemotherapy were prospectively registe
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Saurav, Shashank, Sourajeet Karfa, Trung Vu, et al. "Overcoming Irinotecan Resistance by Targeting Its Downstream Signaling Pathways in Colon Cancer." Cancers 16, no. 20 (2024): 3491. http://dx.doi.org/10.3390/cancers16203491.

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Among the most popular chemotherapeutic agents, irinotecan, regarded as a prodrug belonging to the camptothecin family that inhibits topoisomerase I, is widely used to treat metastatic colorectal cancer (CRC). Although immunotherapy is promising for several cancer types, only microsatellite-instable (~7%) and not microsatellite-stable CRCs are responsive to it. Therefore, it is important to investigate the mechanism of irinotecan function to identify cellular proteins and/or pathways that could be targeted for combination therapy. Here, we have determined the effect of irinotecan treatment on
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Kawabata, Ryohei, Daisuke Sakai, Shigenori Kadowaki, et al. "Subgroup analyses of the effect of ramucirumab in pretreatment with immune checkpoint inhibitor in RINDBeRG: A randomized clinical trial in third- or further-line treatment of gastric cancer." Journal of Clinical Oncology 42, no. 3_suppl (2024): 339. http://dx.doi.org/10.1200/jco.2024.42.3_suppl.339.

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339 Background: To confirm synergistic effect of immune checkpoint blockade and anti-angiogenesis in cancer treatment, we evaluated the effect of pretreatment with immune checkpoint inhibitors to ramucirumab plus irinotecan versus irinotecan in the third or later line treatment beyond progression after ramucirumab for advanced gastric cancer from the RINDBeRG trial. Methods: Patients received ramucirumab at 8 mg/kg plus irinotecan at 150 mg/m2 or irinotecan alone. End points were compared between treatment arms and pretreatments with nivolumab (NIVO+, n = 226) or without nivolumab (NIVO-, n =
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Paulík, Adam, Jiří Grim, and Stanislav Filip. "Predictors of Irinotecan Toxicity and Efficacy in Treatment of Metastatic Colorectal Cancer." Acta Medica (Hradec Kralove, Czech Republic) 55, no. 4 (2012): 153–59. http://dx.doi.org/10.14712/18059694.2015.39.

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The colorectal cancer ranks high among the malignant tumours in incidence and mortality and irinotecan is standardly used in palliative treatment of metastatic disease in every therapeutic line. Unfortunately, the treatment with irinotecan is often associated with severe toxicities, especially neutropenia and diarrhea. The majority of the toxic manifestation is caused by the insufficient deactivation (glucuronidation) of irinotecan active metabolite SN-38 by UGT1A enzyme. The elevated SN-38 plasma concentration is responsible for the hematological and gastrointestinal toxicity that can become
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Ishii, Takahiro, Akihito Kawazoe, Akinori Sasaki, et al. "Clinical and molecular factors for selection of nivolumab or irinotecan as third-line treatment for advanced gastric cancer." Therapeutic Advances in Medical Oncology 12 (January 2020): 175883592094237. http://dx.doi.org/10.1177/1758835920942377.

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Background: The use of nivolumab or irinotecan as the third-line treatment for patients with advanced gastric cancer (AGC) remains controversial. Methods: This study analyzed patients with AGC treated with nivolumab or irinotecan (nivolumab group or irinotecan group, respectively) from May 2016 to April 2019 following two or more previous lines of chemotherapy. Univariate survival analysis was conducted to identify the clinical and molecular factors associated with progression-free survival (PFS). Results: A total of 156 patients (74 treated with nivolumab and 82 treated with irinotecan) were
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Haller, Daniel G., Mace L. Rothenberg, Alfred O. Wong, et al. "Oxaliplatin Plus Irinotecan Compared With Irinotecan Alone as Second-Line Treatment After Single-Agent Fluoropyrimidine Therapy for Metastatic Colorectal Carcinoma." Journal of Clinical Oncology 26, no. 28 (2008): 4544–50. http://dx.doi.org/10.1200/jco.2008.17.1249.

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Purpose To determine whether irinotecan plus oxaliplatin (IROX) is superior to irinotecan alone in patients with metastatic colorectal cancer (CRC) previously treated with single-agent fluoropyrimidines. Patients and Methods A phase III, randomized, open-label, multicenter study of patients with metastatic or recurrent CRC that had progressed or recurred during or after adjuvant or first-line fluoropyrimidines (fluorouracil/leucovorin or capecitabine, the latter only for metastatic CRC). Patients received IROX (irinotecan 200 mg/m2 plus oxaliplatin 85 mg/m2) or irinotecan alone (350 mg/m2) eve
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Kawakami, Takeshi, Nozomu Machida, Masahiro Kawahira, et al. "Efficacy and safety of irinotecan monotherapy as third line treatment for advanced gastric cancer." Journal of Clinical Oncology 34, no. 4_suppl (2016): 113. http://dx.doi.org/10.1200/jco.2016.34.4_suppl.113.

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113 Background: Several randomized trials demonstrated the survival benefit in advanced gastric cancer patients (AGC pts) receiving irinotecan or taxanes as second-line chemotherapy (SLC). Taxanes are used for SLC in daily clinical practice in Japan because of its less toxicity, especially in AGC pts with peritoneal dissemination, compared with irinotecan. Although irinotecan is often administered after refractory or intolerant to taxanes as SLC, the efficacy and safety of irinotecan as third-line chemotherapy (TLC) is still unclear. Methods: We retrospectively investigated the data of AGC pts
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Hutchcraft, Megan L., Nan Lin, Shulin Zhang, et al. "Real-World Evaluation of Universal Germline Screening for Cancer Treatment-Relevant Pharmacogenes." Cancers 13, no. 18 (2021): 4524. http://dx.doi.org/10.3390/cancers13184524.

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The purpose of this study was to determine the frequency of clinically actionable treatment-relevant germline pharmacogenomic variants in patients with cancer and assess the real-world clinical utility of universal screening using whole-exome sequencing in this population. Cancer patients underwent research-grade germline whole-exome sequencing as a component of sequencing for somatic variants. Analysis in a clinical bioinformatics pipeline identified clinically actionable pharmacogenomic variants. Clinical Pharmacogenetics Implementation Consortium guidelines defined clinical actionability. W
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Scheithauer, Werner, Gabriela V. Kornek, Markus Raderer, et al. "Randomized Multicenter Phase II Trial of Oxaliplatin Plus Irinotecan Versus Raltitrexed as First-Line Treatment in Advanced Colorectal Cancer." Journal of Clinical Oncology 20, no. 1 (2002): 165–72. http://dx.doi.org/10.1200/jco.2002.20.1.165.

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PURPOSE: Irinotecan and oxaliplatin are two new agents with promising activity in advanced colorectal cancer. Based on preclinical and clinical evidence that both drugs act synergistically, a randomized phase II study was initiated to investigate the therapeutic potential and tolerance of this combination in the front-line setting. PATIENTS AND METHODS: Ninety-two patients with previously untreated, measurable disease were randomized to receive biweekly oxaliplatin 85 mg/m2 plus irinotecan 175 mg/m2 or raltitrexed 3 mg/m2 given on day 1 every 3 weeks. Upon development of progressive disease, s
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Yu, Kenneth H., Andrew Eugene Hendifar, Olatunji B. Alese, et al. "A multicenter chart review study of patients with metastatic pancreatic ductal adenocarcinoma receiving liposomal irinotecan after gemcitabine-based therapy." Journal of Clinical Oncology 38, no. 15_suppl (2020): e16733-e16733. http://dx.doi.org/10.1200/jco.2020.38.15_suppl.e16733.

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e16733 Background: Real-world data allows healthcare decision-makers to assess and manage therapeutic and economic options for patients, including those who would and would not have met eligibility criteria for randomized control trials (RCT) and are instead managed under usual care. This retrospective multi-academic center chart review study describes real-world characteristics and outcomes of US patients receiving liposomal irinotecan for the management of metastatic pancreatic ductal adenocarcinoma (mPDAC). Methods: Patients with mPDAC treated with liposomal irinotecan were eligible. Initia
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Kehrer, Diederik F. S., Ron H. J. Mathijssen, Jaap Verweij, Peter de Bruijn, and Alex Sparreboom. "Modulation of Irinotecan Metabolism by Ketoconazole." Journal of Clinical Oncology 20, no. 14 (2002): 3122–29. http://dx.doi.org/10.1200/jco.2002.08.177.

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PURPOSE: Irinotecan (CPT-11) is a prodrug of SN-38 and has been registered for the treatment of advanced colorectal cancer. It is converted by the cytochrome P450 3A4 isozyme (CYP3A4) into several inactive metabolites, including 7-ethyl-10-[4-N-(5-aminopentanoic acid)-1-piperidino]-carbonyloxycamptothecin (APC). To investigate the role of CYP3A4 in irinotecan pharmacology, we evaluated the consequences of simultaneous treatment of irinotecan with a potent enzyme inhibitor, ketoconazole, in a group of cancer patients. PATIENTS AND METHODS: A total of seven assessable patients was treated in a r
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Ebrahimpour, Mahnaz, Mahshid Mohammadian, Bagher Pourheydar, Zhino Moradi, and Zhaleh Behrouzkia. "Effects of Radiotherapy in Combination With Irinotecan and 17-AAG on Bcl-2 and Caspase 3 Gene Expression in Colorectal Cancer Cells." Journal of Lasers in Medical Sciences 13, no. 1 (2022): e9-e9. http://dx.doi.org/10.34172/jlms.2022.09.

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Introduction: In this study, the cytotoxic and anti-cancer effects of Irinotecan as a conventional chemotherapeutic agent compared to 17-(allyl amino)-17-demethoxygeldanamycin (17-AAG) as possible radiosensitizers in the HCT-116 cell line were investigated. Methods: HCT-116 cells were treated with various concentrations of irinotecan and 17-AAG and also irradiated with a 2-Gy of X-ray radiation. Then, the cell viability was examined by a water-soluble tetrazolium-1 assay after 24 hours. For single therapies and double and triple combination cases, IC50, 0.5×IC50 and 0.25×IC50 concentrations of
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