Topoisomerase Inhibitors

Compounds that inhibit the activity of DNA TOPOISOMERASES.

Also Known As:

DNA Topoisomerase Inhibitors; Inhibitor, DNA Topoisomerase; Inhibitor, Topoisomerase; Inhibitors, DNA Topoisomerase; Inhibitors, Topoisomerase; Topoisomerase Inhibitor, DNA; Topoisomerase Inhibitors, DNA; DNA Topoisomerase Inhibitor; Topoisomerase Inhibitor

Networked: 373 relevant articles (24 outcomes, 40 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Chemical Actions and Uses
- Pharmacologic Actions: 160
  - Therapeutic Uses: 47080
    - Antineoplastic Agents: 20689
      - Topoisomerase Inhibitors: 373
        Topoisomerase I Inhibitors: 694
        Topoisomerase II Inhibitors: 562
  - Molecular Mechanisms of Pharmacological Action: 24
    - Enzyme Inhibitors: 1659
      - Topoisomerase Inhibitors: 373
        Topoisomerase I Inhibitors: 694
        Topoisomerase II Inhibitors: 562

Experts

1.	Pommier, Yves: 8 articles (01/2021 - 01/2010)
2.	Clement, Bernd: 4 articles (01/2022 - 01/2017)
3.	Scangarella-Oman, Nicole E: 4 articles (10/2020 - 01/2016)
4.	Bauerschlag, Dirk O: 3 articles (01/2022 - 01/2021)
5.	Steinhauer, Tamara N: 3 articles (12/2021 - 01/2017)
6.	Wang, Wenjie: 3 articles (12/2020 - 01/2019)
7.	Hossain, Mohammad: 3 articles (01/2020 - 08/2016)
8.	Kantarjian, Hagop: 3 articles (01/2011 - 07/2009)
9.	Ravandi, Farhad: 3 articles (01/2011 - 07/2009)
10.	Innocenti, Federico: 2 articles (07/2022 - 04/2009)

Related Diseases

1.	Neoplasms (Cancer) 02/01/2017 - "Numerous topoisomerase inhibitors with proven efficacy have been used extensively to treat various human neoplasms. " 01/01/2019 - "A strategy of employing the topoisomerase inhibitors in combination with other treatments can potentially sensitize the cancer to increase the therapeutic efficacy and reduce resistance or adverse side effects. " 01/01/2017 - "Cluster analyses of the cytological profiles of the tested compounds suggested that these plants contain possible topoisomerase inhibitors that could be effective in cancer treatment. " 09/01/2004 - "These findings suggest that the combination of AAV-mediated suicide gene therapy and treatment with topoisomerase inhibitors may have synergistic therapeutic effects in the treatment of cancers." 01/01/2019 - "Collectively, a potent DNA topoisomerase inhibitor (8a) was discovered, which exhibited potential as a candidate chemotherapeutic agent for the management of tumors in the present study."
2.	Colonic Neoplasms (Colon Cancer) 10/19/2001 - "Based on this study it is tempting to suggest that combination of EGCG with other conventional topoisomerase inhibitors could be an improved strategy for treatment of colon cancer. " 11/30/2023 - "Overview of the New Bioactive Heterocycles as Targeting Topoisomerase Inhibitors Useful Against Colon Cancer." 01/19/2018 - "The current study demonstrated that human colon cancer HCT116 and HT29 cells became highly susceptible to cell death when being co-treated with PLGL and low dose of camptothecin11 (CPT11, a topoisomerase inhibitor-based drug), the efficacy of which was comparable as that generated by the high dose of CPT11. " 06/01/2013 - "The roles of autophagic cell death and apoptosis induced by topoisomerase inhibitor irinotecan in colon cancer cells with deleted p53 were investigated during 48 h. " 02/01/2018 - "7-Ethyl-10-hydroxy-camptothecin (SN-38), an efficient topoisomerase inhibitor, is the biological metabolite of irinotecan used as the first-line chemotherapy drug for colon cancer. "
3.	Non-Small-Cell Lung Carcinoma (Carcinoma, Non-Small Cell Lung) 01/01/2017 - "In this study, we assessed the association between reduced Smad4 expression and DNA topoisomerase inhibitor sensitivity in human non-small cell lung cancer (NSCLC) patients and evaluated the relationship between genomic alterations of Smad4 and molecular alterations in DNA repair molecules. " 01/01/2017 - "Reduced Smad4 expression and DNA topoisomerase inhibitor chemosensitivity in non-small cell lung cancer." 08/01/2009 - "HIF-1alpha modulation by topoisomerase inhibitors in non-small cell lung cancer cell lines." 12/27/1995 - "Given the differential expression of topoisomerases in normal lung and tumors, research of more potent and specific topoisomerase inhibitors might prove beneficial in non-small cell lung cancer. " 01/01/2017 - "DNA-PK Inhibition by NU7441 Enhances Chemosensitivity to Topoisomerase Inhibitor in Non-Small Cell Lung Carcinoma Cells by Blocking DNA Damage Repair."
4.	Pancreatic Neoplasms (Pancreatic Cancer) 09/01/2018 - "Translating landmark trial-based evidence to the front lines of care for pancreatic cancer: the evolving trial-based and guideline-supported role for nanoliposomal topoisomerase inhibitors in metastatic pancreatic adenocarcinoma." 01/01/2020 - "Liposomal irinotecan (nal-IRI) is a topoisomerase inhibitor proven to improve survival in metastatic pancreatic cancer (mPC). " 04/01/2011 - "This topoisomerase inhibitor exploits solid tumor physiology for improved selectivity and activity against multiple tumor types with particular promise for use in treating pediatric neuroblastoma and pancreatic carcinoma." 12/01/2021 - "PARP inhibitors synergize with topoisomerase inhibitors, and veliparib plus modified (m) FOLFIRI (no 5-FU bolus) had preliminary activity in metastatic pancreatic cancers. " 11/07/2019 - "Pancreatic cancer cell lines, MIA PaCa-2 and PANC-1 were exposed to ICPD47 and ICPD62 alone and in combinations with antimetabolites gemcitabine (GEM), 5-fluorouracil (5-FU) and topoisomerase inhibitor doxorubicin (DOX). "
5.	Gonorrhea 01/01/2016 - "Efficacy of a Novel Tricyclic Topoisomerase Inhibitor in a Murine Model of Neisseria gonorrhoeae Infection." 01/01/2018 - "In this phase 2 study, we evaluated the efficacy and safety of oral gepotidacin, a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor, for the treatment of uncomplicated urogenital gonorrhea. " 01/01/2016 - "Gepotidacin, a novel triazaacenaphthylene antibacterial agent, is the first in a new class of type IIA topoisomerase inhibitors with activity against many biothreat and conventional pathogens, including Neisseria gonorrhoeae To assist ongoing clinical studies of gepotidacin to treat gonorrhea, a multilaboratory quality assurance investigation determined the reference organism (N. " 10/01/2020 - "Gepotidacin (GSK2140944) is a first in class, novel triazaacenaphthylene bacterial type II topoisomerase inhibitor in Phase 3 clinical development for the treatment of gonorrhea and uncomplicated urinary tract infections (acute cystitis). "

Related Drugs and Biologics

1.	Irinotecan (Camptosar)
2.	Etoposide (VP 16)
3.	DNA (Deoxyribonucleic Acid)
4.	Type II DNA Topoisomerases (Topoisomerase II)
5.	Doxorubicin (Adriamycin)
6.	Taxoids (Taxanes)
7.	Gemcitabine
8.	Platinum
9.	Antineoplastic Agents (Antineoplastics)
10.	Anthracyclines

Related Therapies and Procedures

1.	Drug Therapy (Chemotherapy)
2.	Therapeutics
3.	Combination Drug Therapy (Combination Chemotherapy)
4.	Radiotherapy
5.	Combined Modality Therapy