In the treatment of colorectal cancer, ovarian cancer, and non‐small cell lung cancer, the use of Topo I inhibitors, either alone or in combination with other chemotherapeutic agent(s) or modalities of therapy, have shown encouraging outcomes.
Topotecan is another semi‐synthetic analogue of camptothecin.
By stabilising Top 1-DNA complexes, irinotecan generates Top …
Phase II trial of CPT‐11 in patients with advanced pancreatic cancer, an EORTC early clinical trials group studySynergism between cisplatin and topoisomerase I inhibitors, NB‐506 and SN‐38, in human small cell lung cancer cellsPharmacokinetics (PK) of the irinotecan/oxaliplatin (LOHP) combination: preliminary data of an ongoing phase I trialA phase I and pharmacokinetic (PK) study of CPT‐11 (C) and 5‐FU (F) combinationA phase II multicenter trial of alternating cycles of irinotecan (CPT‐11) and 5‐FU/LV in patients with previously untreated metastatic colorectal cancer (CRC)Phase I dose finding and pharmacokinetic (PK) study of docetaxel (D) in combination with irinotecan (I) in advanced solid tumorsPopulation pharmacokinetics and pharmacodynamics of irinotecan (CPT‐11) and active metabolite SN‐38 during phase I trialsInfluence of age on the pharmacokinetics of irinotecan (CPT‐11) and its metabolites, SN‐38 and SN‐38 glucuronide (SN‐38G) in patients with previously treated colorectal cancerPhase I trial of irinotecan (CPT‐11) in childhood tumorsPhase I and pharmacokinetic (PK) study of irinotecan (CPT‐11) with a prolonged (14D) infusion scheduleConversion of CPT‐11 to its active form, SN‐38, by carboxylesterase of non‐small cell lung cancerPopulation pharmacokinetics and pharmacodynamics of irinotecan (CPT‐11) and active metabolite SN‐38 during phase I trialsNo alteration in DNA topoisomerase I gene related to CPT‐11 resistance in human lung cancerDeterminants of drug response in camptothecin‐11‐resistant glioma cell linesIrinotecan (CPT‐11) high dose escalation using intensive high‐dose loperamide to control diarrheaRelationship between the pharmacokinetics of irinotecan and diarrhea during combination chemotherapy with cisplatinCholinergic symptoms following CPT‐11 infusion in a phase II multicenter trial of 250 mg/mReduced albumin binding promotes the stability and activity of topotecan in human bloodActivity of topotecan, a new topoisomerase inhibitor, against human tumor colony forming units in vitroConcentration and timing dependence of lethality enhancement between topotecan, a topoisomerase I inhibitor and ionizing radiationEvaluation of 9 dimethyl amino methyl 10 hydroxy camptothecin (topotecan) against xenografts derived from adult and childhood tumorsEfficacy of topoisomerase I inhibitors, topotecan and irinotecan, administered at low dose levels in protracted schedules to mice bearing xenografts of human tumorsTopotecan, a topoisomerase I inhibitor, is active in the treatment of myelodysplastic syndrome and chronic myelomonocytic leukemiaIn vitro and in vivo activity of topotecan against human B‐lineage acute lymphoblastic leukemia cellsTopoisomerase I inhibitors: topotecan and irinotecanPhase II study of topotecan in metastatic non small cell lung cancerA phase I and pharmacologic study of a combination of cyclophosphamide (CY) and topotecan (TOPO) in patients (pts) with refractory leukemiaNew options for the treatment of advanced ovarian cancerThe potential of topoisomerase I inhibitors in the treatment of CNS malignancies: report of a synergistic effect between topotecan and radiationTopoisomerase I interactive drugs in children with cancerThe significance of the sequence of administration of topotecan and etoposidePharmacokinetically guided dose adjustment reduces variability in topotecan (TPT) systemic exposure in children with solid tumorsPharmacokinetics and pharmacodynamics of topotecan given on a daily‐times‐five schedule in phase II clinical trials using a limited‐sampling procedureBioavailability and pharmacokinetics of oral topotecan: a new topoisomerase I inhibitorPhenytoin increases topotecan (TPT) clearance in a patient with medulloblastoma (MB)In vivo antitumor activity of two new seven‐substituted water soluble camptothecin analoguesChemotherapy and Transplantation: The Role of Immunosuppression in Malignancy and a Review of Antineoplastic Agents in Solid Organ Transplant Recipients, MRP1 expression in CTCs confers resistance to irinotecan‐based chemotherapy in metastatic colorectal cancer, Studies on pyrrolidinones.
Topoisomerase I inhibitors are a new class of anticancer agents with a mechanism of action aimed at interrupting DNA replication in cancer cells, the result of which is cell death.
Nuclear DNA topoisomerase I (TOP1) is an essential human enzyme.