Topoisomerase I inhibitors: the relevance of prolonged exposure for present clinical development

Arrest of replication forks by drug-stabilized topoisomerase I-DNA cleavable complexes as a mechanism of cell killing by camptothecin.

1989 • 1,030 citations

Induction of endonucleolytic DNA cleavage in human acute myelogenous leukemia cells by etoposide, camptothecin, and other cytotoxic anticancer drugs: a cautionary note.

1989 • 937 citations

Intracellular roles of SN-38, a metabolite of the camptothecin derivative CPT-11, in the antitumor effect of CPT-11.

1991 • 855 citations

Identification of mammalian DNA topoisomerase I as an intracellular target of the anticancer drug camptothecin.

1988 • 843 citations

DNA Topoisomerase I—Targeted Chemotherapy of Human Colon Cancer in Xenografts

1989 • 645 citations

DNA topoisomerase-targeting antitumor drugs can be studied in yeast.

1988 • 490 citations

Structure-activity study of the actions of camptothecin derivatives on mammalian topoisomerase I: evidence for a specific receptor site and a relation to antitumor activity.

1989 • 445 citations

Topoisomerase-targeting antitumor drugs

1989 • 441 citations

Involvement of nucleic acid synthesis in cell killing mechanisms of topoisomerase poisons.

1990 • 427 citations

Topotecan, an active drug in the second-line treatment of epithelial ovarian cancer: results of a large European phase II study.

1996 • 384 citations

Efficacy of topoisomerase I inhibitors, topotecan and irinotecan, administered at low dose levels in protracted schedules to mice bearing xenografts of human tumors

1995 • 378 citations

Phase I and pharmacologic study of topotecan: a novel topoisomerase I inhibitor.

1992 • 363 citations

Eukaryotic DNA topoisomerases: two forms of type I DNA topoisomerases from HeLa cell nuclei.

1981 • 350 citations

Phase I clinical trial of weekly and daily treatment with camptothecin (NSC-100880): correlation with preclinical studies.

1972 • 315 citations

Evidence that DNA topoisomerase I is necessary for the cytotoxic effects of camptothecin.

1988 • 314 citations

Characterization of a mammalian mutant with a camptothecin-resistant DNA topoisomerase I.

1987 • 291 citations

Involvement of DNA topoisomerase I in transcription of human ribosomal RNA genes.

1988 • 282 citations

Phase II study of camptothecin (NSC-100880) in the treatment of advanced gastrointestinal cancer.

1972 • 271 citations

Preliminary pharmacologic and clinical evaluation of camptothecin sodium (NSC-100880).

1970 • 246 citations

Protein-linked DNA strand breaks induced in mammalian cells by camptothecin, an inhibitor of topoisomerase I.

1989 • 243 citations

An early phase II study of CPT-11: a new derivative of camptothecin, for the treatment of leukemia and lymphoma.

1990 • 234 citations

Evaluation of 9-dimethylaminomethyl-10-hydroxycamptothecin against xenografts derived from adult and childhood solid tumors

1992 • 231 citations

Decreased expression of DNA topoisomerase I in camptothecin-resistant tumor cell lines as determined by a monoclonal antibody.

1990 • 226 citations

Effect of P-glycoprotein expression on the accumulation and cytotoxicity of topotecan (SK&F 104864), a new camptothecin analogue.

1992 • 212 citations

Complete growth inhibition of human cancer xenografts in nude mice by treatment with 20-(S)-camptothecin.

1991 • 179 citations

Activity of Topotecan, a New Topoisomerase I Inhibitor, Against Human Tumor Colony-Forming Units In Vitro

1992 • 174 citations

Establishment of a camptothecin analogue (CPT-11)-resistant cell line of human non-small cell lung cancer: Characterization and mechanism of resistance

1991 • 168 citations

Phase I trial of low-dose continuous topotecan infusion in patients with cancer: an active and well-tolerated regimen.

1994 • 166 citations

Camptothecin overcomes MDR1-mediated resistance in human KB carcinoma cells.

1991 • 159 citations

Treatment of malignant melanoma with camptothecin (NSC-100880).

1972 • 158 citations

Camptothecin-induced in vivo topoisomerase I cleavages in the transcriptionally active tyrosine aminotransferase gene

1987 • 150 citations

Studies on camptothecin. I. Effects of nucleic acid and protein synthesis.

1971 • 146 citations

Effects of camptothecin on the breakage and repair of DNA during the cell cycle.

1973 • 140 citations

Phase I study of Topotecan, a new topoisomerase I inhibitor, in patients with refractory or relapsed acute leukemia

1993 • 133 citations

Phase I study of topotecan for pediatric patients with malignant solid tumors.

1994 • 132 citations

Bioavailability and pharmacokinetics of oral topotecan: a new topoisomerase I inhibitor

1996 • 132 citations

Camptothecin-resistant mutants of Chinese hamster ovary cells containing a resistant form of topoisomerase I.

1988 • 125 citations

Phase I and pharmacokinetics study of topotecan, a new topoisomerase I inhibitor

1993 • 123 citations

Phase I Study and Pharmacokinetics of CPT-11 With 5-Day Continuous Infusion

1992 • 122 citations

Camptothecin, teniposide, or 4'-(9-acridinylamino)-3-methanesulfon-m-anisidide, but not mitoxantrone or doxorubicin, induces degradation of nuclear DNA in the S phase of HL-60 cells.

1991 • 109 citations

Phase I and pharmacokinetic study of irinotecan (CPT-11) administered daily for three consecutive days every three weeks in patients with advanced solid tumors

1995 • 107 citations

Analysis of topoisomerase I/DNA complexes in patients administered topotecan.

1995 • 107 citations

Phase II study of topotecan in patients with advanced non-small-cell lung cancer previously untreated with chemotherapy.

1996 • 105 citations

Evidence for an intermediate with a single-strand break in the reaction catalyzed by the DNA untwisting enzyme.

1976 • 97 citations

Phase II study of topotecan in metastatic non-small-cell lung cancer.

1994 • 97 citations

Effects of camptothecin on RNA synthesis in leukemia L1210 cells

1971 • 94 citations

Pediatric phase I trial and pharmacokinetic study of topotecan administered as a 24-hour continuous infusion.

1993 • 93 citations

Human DNA topoisomerase I is encoded by a single-copy gene that maps to chromosome region 20q12-13.2.

1988 • 93 citations

[A phase II study of CPT-11, a camptothecin derivative, in patients with primary lung cancer. CPT-11 Cooperative Study Group].

1991 • 91 citations

Complete inhibition of growth followed by death of human malignant melanoma cells in vitro and regression of human melanoma xenografts in immunodeficient mice induced by camptothecins.

1992 • 89 citations

Phase I/pharmacokinetic study of topotecan by 24-hour continuous infusion weekly.

1994 • 86 citations

Characterization of a camptothecin-resistant human DNA topoisomerase I.

1988 • 82 citations

Toxicity of camptothecin (NSC-100880).

1974 • 81 citations

In vivo antitumor activity of two new seven-substituted water-soluble camptothecin analogues.

1995 • 79 citations

Topoisomerase I alteration in a camptothecin-resistant cell line derived from Chinese hamster DC3F cells in culture.

1992 • 71 citations

Phase I and pharmacologic study of 9-aminocamptothecin given by 72-hour infusion in adult cancer patients.

1996 • 70 citations

Escalating systemic exposure of continuous infusion topotecan in children with recurrent acute leukemia.

1996 • 69 citations

Plasma camptothecin (NSC-100880) levels during a 5-day course of treatment: relation to dose and toxicity.

1972 • 68 citations

Regression of human breast carcinoma tumors in immunodeficient mice treated with 9-nitrocamptothecin: differential response of nontumorigenic and tumorigenic human breast cells in vitro.

1993 • 66 citations

Camptothecin and its derivatives induce expression of the c-jun protooncogene in human myeloid leukemia cells.

1991 • 66 citations

Camptothecin derivatives induce regression of human ovarian carcinomas grown in nude mice and distinguish between non‐tumorigenic and tumorigenic cells in vitro

1993 • 60 citations

Pharmacokinetics of the in vivo and in vitro conversion of 9-nitro-20(S)-camptothecin to 9-amino-20(S)-camptothecin in humans, dogs, and mice.

1994 • 58 citations

Camptothecin induces differentiation and stimulates the expression of differentiation-related genes in U-937 human promonocytic leukemia cells.

1992 • 57 citations

Studies of topoisomerase-specific antitumor drugs in human lymphocytes using rabbit antisera against recombinant human topoisomerase II polypeptide.

1989 • 56 citations

Lethal activity of camptothecin sodium on human lymphoma cells.

1974 • 54 citations

Antitumor effect of liposome-incorporated camptothecin in human malignant xenografts

1995 • 50 citations

Efficacy of camptothecin congeners in the treatment of human breast carcinoma xenografts.

1993 • 49 citations

Phase I and pharmacological study of the new topoisomerase I inhibitor GI147211, using a daily x 5 intravenous administration

1996 • 45 citations

Phase I and pharmacokinetic studies of topotecan administered as a 72 or 120 h continuous infusion

1994 • 43 citations

DNA topoisomerase I phosphorylation in murine fibroblasts treated with 12-O-tetradecanoylphorbol-13-acetate and in vitro by protein kinase.

1992 • 42 citations

Phorbol Ester Transiently Increases Topoisomerase I mRNA Levels in Human Skin Fibroblasts

1989 • 41 citations

Therapeutic efficacy of camptothecin derivatives against human malignant melanoma xenografts

1994 • 38 citations

[An early phase II study of CPT-11 in primary lung cancer].

1991 • 38 citations

Docetaxel in advanced renal carcinoma

1994 • 36 citations

Topoisomerase-targeting antitumor drugs: mechanisms of cytotoxicity and resistance.

1992 • 36 citations

Induction of differentiation of human and mouse myeloid leukemia cells by camptothecin

1990 • 33 citations

Differential expression of DNA topoisomerase I gene between CPT-11 acquired-and native-resistant human pancreatic tumor cell lines: Detected by RNAPCR-based quantitation assay

1992 • 30 citations

Increased synthesis and degradation of DNA topoisomerase I during the initial phase of human T lymphocyte proliferation.

1993 • 28 citations

Phase II trial of topotecan in patients with cisplatin-refractory germ cell tumors

1995 • 27 citations

[An early phase II study of CPT-11 in gynecologic cancers. Research Group of CPT-11 in Gynecologic Cancers].

1991 • 21 citations

Pharmacologic studies of camptothecin (NSC-100880): distribution, plasma protein binding, and biliary excretion.

1973 • 18 citations

Studies of the differentiation properties of camptothecin in the human leukaemic cells K562

1991 • 13 citations

Differentiation induction of human promyelocytic leukemia cells by 10-hydioxycamptothecin, a DNA topoisomerase I inhibitor

1991 • 13 citations

Effect of camptothecin on mitogenic stimulation of human lymphocytes: Involvement of DNA topoisomerase I in cell transition from G₀ to G₁ phase of the cell cycle and in DNA replication

1992 • 12 citations

Novel inhibitors of RNA synthesis.

1974 • 10 citations