Ex vivo effects of the dual topoisomerase inhibitor tafluposide (F 11782) on cells isolated from fresh tumor samples taken from patients with cancer.

Abstract:

:Tafluposide (F 11782), a novel epipodophylloid with a unique mechanism of interaction with both topoisomerase I and II, has shown outstanding antitumor activity in vivo against a panel of experimental human tumor xenografts. The aim of this study was to evaluate its cytotoxicity against fresh tumor cells taken from patients. Cells derived from bone marrow, peripheral blood, malignant effusions or solid biopsies from 84 patients with either hematological or solid tumors were exposed continuously to 0.8-100 nuM tafluposide for 48 h, 96 h or 7 days. Cell survival was measured using an MTT assay or the ATP assay and LC(50) values (drug concentration required for 50% cell kill) were calculated. Tafluposide showed significant cytotoxicity against cells derived from either hematological or solid tumors, with a marked inter-patient variation. There was no significant difference between the effect of tafluposide in samples from untreated or previously treated patients (p>0.05 for all cancer types). Whilst tafluposide appeared to show weak (p<0.05) cross-resistance with the topoisomerase II inhibitor etoposide in acute myeloid leukemia (AML), there did not appear to be any correlation with the effect of the topoisomerase I inhibitor topotecan (p>0.05) in either hematological or solid malignancies. True synergism was identified when combining tafluposide with cisplatin in ovarian cancer [combination index (CI)=0.14, 0.79] and with etoposide in AML (CI=0.49, 0.63 and 0.78). Our results suggest that tafluposide is a strong candidate for inclusion in clinical trials, particularly in hematological malignancies.

journal_name

Anticancer Drugs

journal_title

Anti-cancer drugs

authors

Sargent JM,Elgie AW,Williamson CJ,Hill BT

doi

10.1097/00001813-200307000-00013

subject

Has Abstract

pub_date

2003-07-01 00:00:00

pages

467-73

issue

6

eissn

0959-4973

issn

1473-5741

journal_volume

14

pub_type

杂志文章
  • Successful treatment with personalized dosage of imatinib in elderly patients with gastrointestinal stromal tumors.

    abstract::Imatinib is the standard first-line therapy for metastatic gastrointestinal stromal tumors. It has markedly improved the prognosis and outcome of patients affected by gastrointestinal stromal tumors, especially in the case of exon 11 KIT mutations. Imatinib-associated adverse events are generally mild to moderate; how...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000331

    authors: Saponara M,Gatto L,Di Nunno V,Tabacchi E,Fanti S,Di Scioscio V,Nannini M,Gruppioni E,Altimari A,Fiorentino M,Santini D,Ceccarelli C,Zompatori M,Biasco G,Pantaleo MA

    更新日期:2016-04-01 00:00:00

  • Anorectal adenocarcinoma recurrence successfully treated with electrochemotherapy: a case report.

    abstract::Anal canal adenocarcinoma is generally treated like rectal cancer. Surgery is the standard treatment in early stages and neoadjuvant chemoradiation in locally advanced tumors. Local recurrences treatment paradigm often depends on the previous therapies of either surgery or radiotherapy or systemic therapy. We present ...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000838

    authors: Ferioli M,Guido A,Buwenge M,Coe M,Galuppi A,de Terlizzi F,Poggioli G,Morganti AG

    更新日期:2020-01-01 00:00:00

  • Interactions of interferon and vinblastine on experimental tumor model melanoma B-16 in vitro.

    abstract::In this study, we tried to define in vitro interactions of two antitumor agents that have different sites and different mechanisms of action. Vinblastine (VLB) in combination with human recombinant interferon-alpha A/D (rHuIFN-alpha A/D) and in combination with murine recombinant interferon-gamma (rMuIFN-gamma) was st...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/00001813-199402000-00008

    authors: Jezersek B,Novaković S,Sersa G,Auersperg M,Fleischmann WR Jr

    更新日期:1994-02-01 00:00:00

  • FOLFIRI in patients with locally advanced or metastatic pancreatic or biliary tract carcinoma: a monoinstitutional experience.

    abstract::Pancreatic and biliary tract carcinomas are very chemoresistant. After a first-line treatment with a gemcitabine-based regimen, no second-line scheme is consolidated in clinical practice. The aim of this study was to evaluate the toxicity and the activity of the FOLFIRI regimen as first-line or second-line chemotherap...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0b013e328364e66b

    authors: Moretto R,Raimondo L,De Stefano A,Cella CA,Matano E,De Placido S,Carlomagno C

    更新日期:2013-10-01 00:00:00

  • A retrospective study of paclitaxel combining nedaplatin chemotherapy for esophageal cancer.

    abstract::The aim of this study was to evaluate the efficacy and tolerability of the combination of paclitaxel and nedaplatin in patients with advanced esophageal cancer. Patients (n = 310) with recurrent or metastatic esophageal squamous cell carcinoma, who had a maximum of one previous chemotherapy regimen, were enrolled in t...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000170

    authors: Du J,Hu C,Zhang Y,Hu B,Wang F,Zhang Y

    更新日期:2015-01-01 00:00:00

  • Cytotoxic effects and pharmacokinetic analysis of combined adriamycin and X-ray treatments in human organotypic cell cultures.

    abstract::Organotypic cultures of human A549 cells were used as a tumor model to investigate sequence effects for combination treatments with adriamycin (ADR) and X-irradiation. Initial drug exposure led to the greatest cytotoxic effect especially when X-rays were delivered 24 h later and this subsequent irradiation did not sig...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/00001813-199204000-00010

    authors: Chevillard S,Vielh P,Campana F,Bastian G,Coppey J

    更新日期:1992-04-01 00:00:00

  • Antiproliferative and apoptotic effects of paeonol on human hepatocellular carcinoma cells.

    abstract::Paeonol, a major phenolic component of Moutan Cortex, is known to have antitumor effects through an unknown mechanism. In this study, we tried to elucidate the anticancer effects of paeonol on human hepatocellular carcinoma (HCC) cell lines BEL-7404, SMMC-7721, and MHCC97-H in vitro. Using the 3-[4,5-dimethylthiazol-2...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0b013e3282f7f4eb

    authors: Chunhu Z,Suiyu H,Meiqun C,Guilin X,Yunhui L

    更新日期:2008-04-01 00:00:00

  • Blockade of GLUT1 by WZB117 resensitizes breast cancer cells to adriamycin.

    abstract::The tolerance to adriamycin of cancer as a common and stubborn obstacle occurred during curing breast cancer patients needs to be overcome. In the present study, we explored whether inhibiting the glucose transporter 1 (GLUT1) could restore the activity of adriamycin in breast cancer cell line MCF-7 resistant to adria...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000529

    authors: Chen Q,Meng YQ,Xu XF,Gu J

    更新日期:2017-09-01 00:00:00

  • Doxycycline and other tetracyclines in the treatment of bone metastasis.

    abstract::The tetracycline family includes tetracycline, doxycycline and minocycline, all of which have been used as antibiotics effectively for decades. New uses emerged for these compounds after their effect on mitochondrial function was discovered. Cytostatic and cytotoxic activity of these compounds was shown against cell l...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章,评审

    doi:10.1097/00001813-200311000-00001

    authors: Saikali Z,Singh G

    更新日期:2003-11-01 00:00:00

  • Mechanism of action of rituximab.

    abstract::The CD20 antigen is strongly and stably expressed on cells of the B-cell lineage, but not on stem cells, and is thus an ideal target antigen for antibody therapy of B-cell malignancies. Rituximab is a human-mouse chimeric monoclonal antibody to the CD20 antigen that kills B-cells by a number of different effector mech...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章,评审

    doi:

    authors: Maloney DG

    更新日期:2001-06-01 00:00:00

  • Generation of DNA damage by anti-neoplastic agents.

    abstract::DNA has been one of the major targets of cancer chemotherapy. A variety of anti-neoplastic agents can cause different types of DNA lesions, including base alterations, single- or double-strand DNA breaks, DNA-DNA cross-links and DNA-protein cross-links. The exact processes by which these DNA lesions lead to cell death...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章,评审

    doi:10.1097/00001813-199112000-00003

    authors: Kubota M

    更新日期:1991-12-01 00:00:00

  • Phase I/II study of irinotecan (CPT-11) and S-1 in the treatment of advanced gastric cancer.

    abstract::A phase I/II study to determine the recommended dose for combination therapy with CPT-11 (irinotecan hydrochloride) and S-1 (tegafur, gimestat and otastat potassium) for advanced or recurrent gastric cancer, and to assess the safety and efficacy of this therapy. In the phase I portion of the study, S-1 was administere...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0b013e3280262460

    authors: Katsube T,Ogawa K,Ichikawa W,Fujii M,Tokunaga A,Takagi Y,Kochi M,Hayashi K,Kubota T,Aiba K,Arai K,Terashima M,Kitajima M

    更新日期:2007-06-01 00:00:00

  • Anticancer properties of thiophene derivatives in breast cancer MCF-7 cells.

    abstract::Substitutions in thiophene structure give rise to new derivatives with different biological and pharmacological activities. The present study investigated the cytotoxicity activity of some thiophene derivatives in breast cancer cells maintained in two-dimensional (2D) or in three-dimensional (3D) culture and evaluated...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000581

    authors: Dos Santos FA,Pereira MC,de Oliveira TB,Mendonça Junior FJB,de Lima MDCA,Pitta MGDR,Pitta IDR,de Melo Rêgo MJB,da Rocha Pitta MG

    更新日期:2018-02-01 00:00:00

  • Special pharmacokinetics of dipetarudin suggests a potential antitumor activity of this thrombin inhibitor.

    abstract::Thrombin is a potent mitogen for many tumor cells, suggesting that this enzyme may be involved in tumor genesis and metastasis. Inhibition of thrombin expressed on the surface of tumor cells may improve outcomes in some tumor cases. For this reason, a thrombin inhibitor to be applied in antitumor therapy must have fav...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/00001813-200402000-00007

    authors: López ML,Nowak G

    更新日期:2004-02-01 00:00:00

  • A clinical armamentarium of marine-derived anti-cancer compounds.

    abstract::The sea, covering 70% of the Earth's surface, offers a considerably broader spectrum of biological diversity than terra firma. Containing approximately 75% of all living organisms, the marine environment offers a rich source of natural products with potential therapeutic application. Marine organisms have evolved the ...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章,评审

    doi:

    authors: Jimeno JM

    更新日期:2002-05-01 00:00:00

  • Apoptosis of human prostate cancer cells induced by marine actinomycin X2 through the mTOR pathway compounded by MiRNA144.

    abstract::The present study aimed to determine whether actinomycin X2 (AX2) intercepted the mTOR/PTEN/PI3K/Akt signaling pathway to inhibit human prostate cancer cells (PC-3) in vitro. The effects of AX2 on mTOR, PTEN, PI3K, and Akt at the protein level and mRNA were determined by western blotting and real-time reverse transcri...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000309

    authors: Liu J,Xie S,Wu Y,Xu M,Ao C,Wang W,Zeng Q,Hu W,Li M

    更新日期:2016-03-01 00:00:00

  • Severe bladder contracture leading to cystectomy after intravesical mitoxantrone chemotherapy.

    abstract::Since the early 1990s, mitoxantrone has been used as a chemotherapeutic agent for adjuvant intravesical treatment following transurethral resection of superficial transitional cell carcinomas of the bladder. Although its efficacy as adjuvant intravesical therapy remains questionable and its use has not gained wide acc...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/cad.0b013e3282f421fe

    authors: Giannakopoulos S,Pantazis T,Kalaitzis C,Antoniou D,Patris E,Touloupidis S

    更新日期:2008-03-01 00:00:00

  • Evaluations of biomarkers associated with sensitivity to 5-fluorouracil and taxanes for recurrent/advanced breast cancer patients treated with capecitabine-based first-line chemotherapy.

    abstract::The aim of the present study was to investigate the gene expression of biomarkers associated with the sensitivity to fluoropyrimidine and taxanes in recurrent/advanced breast cancer patients treated with first-line capecitabine chemotherapy. We evaluated the clinicopathological/prognostic significance of thymidylate s...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0b013e32834f7ef4

    authors: Zhao HY,Huang H,Hu ZH,Huang Y,Lin SX,Tian Y,Lin TY

    更新日期:2012-06-01 00:00:00

  • New formulation of 5-fluorouracil in microspheres reduces toxicity in mice.

    abstract::A new dosage formulation of 5-fluorouracil incorporated in microspheres (5-FU-MS) was developed for the treatment of peritoneal carcinomatosis. We studied the acute toxicity and side effects of i.p. 5-FU-MS in mice. The 50% lethal dose value for 5-FU-MS was 535.4 mg/kg of 5-FU, which was 2.22 times that of the aqueous...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/00001813-199609000-00010

    authors: Hagiwara A,Sakakura C,Tsujimoto H,Ohgaki M,Imanishi T,Yamazaki J,Sawai K,Takahashi T,Yamamoto A,Muranishi S,Tabata Y,Ikada Y

    更新日期:1996-09-01 00:00:00

  • Radiation recall dermatitis triggered by multi-targeted tyrosine kinase inhibitors: sunitinib and sorafenib.

    abstract::Small molecule tyrosine kinase inhibitors are rapidly being integrated into the management of cancer. This is the first report of sorafenib and sunitinib, both small molecule tyrosine kinase inhibitors of vascular endothelial growth factor and platelet-derived growth factor receptors, triggering radiation recall derma...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0b013e328333d679

    authors: Chung C,Dawson LA,Joshua AM,Brade AM

    更新日期:2010-02-01 00:00:00

  • Inhibition of laryngeal cancer stem cells by tetrandrine.

    abstract::Cancer stem cells play a fundamental role in the growth, metastasis, recurrence, and chemoresistance of cancers of various origins; therefore, targeting these cells may prospectively help to eradicate cancer cells from patients. In this study, the effect of tetrandrine on the proliferation of CD133-positive (CD133) He...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000803

    authors: Cui X,Xiao D,Wang X

    更新日期:2019-10-01 00:00:00

  • The effects of sex steroids on colon carcinogenesis.

    abstract::Numerous reports on colon carcinogenesis reveal gender differences in the incidence and location of tumors. A large number of the presented studies suggest that sex-steroids have a considerable effect on tumorigenesis of the large bowel. To clarify the, so far, not fully understood mechanisms and somewhat conflicting ...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章,评审

    doi:10.1097/00001813-199010000-00003

    authors: Dornschneider G,Izbicki JR,Wilker DK,Schweiberer L

    更新日期:1990-10-01 00:00:00

  • Effect of membrane active 1-alkylpiperidine N-oxides on glycolysis, respiration and ATP level in tumor cells.

    abstract::The aim of this study was to study the effect of the homologous series of 1-alkylpyrrolidine N-oxides on ATP-producing processes in Ehrlich ascites and L1210 murine leukemia cells. 1-Decylpiperidine N-oxide (deP-NO), one of the active compounds, significantly stimulated the course of aerobic glycolysis of Ehrlich cell...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/00001813-199308000-00008

    authors: Miko M,Devinsky F

    更新日期:1993-08-01 00:00:00

  • Real-world healthcare costs of ipilimumab in patients with advanced cutaneous melanoma in The Netherlands.

    abstract::There is limited evidence on the costs associated with ipilimumab. We investigated healthcare costs of all Dutch patients with advanced cutaneous melanoma who were treated with ipilimumab. Data were retrieved from the nation-wide Dutch Melanoma Treatment Registry. Costs were determined by applying unit costs to indivi...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000628

    authors: Franken MG,Leeneman B,Jochems A,Schouwenburg MG,Aarts MJB,van Akkooi ACJ,van den Berkmortel FWPJ,van den Eertwegh AJM,de Groot JWB,van der Hoeven KJM,Hospers GAP,Kapiteijn E,Koornstra R,Kruit WHJ,Louwman MWJ,Piersma D,van

    更新日期:2018-07-01 00:00:00

  • The antitumor drug candidate 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole induces NF-kappaB activity in drug-sensitive MCF-7 cells.

    abstract::2-(4-Amino-3-methylphenyl)-5-fluoro-benzothiazole (5F 203) potently inhibits MCF-7 breast cancer cell growth in part by activating the aryl hydrocarbon receptor (AhR) signaling pathway. Ligands for the AhR (i.e. dioxin) have also been shown to modulate the NF-kappaB signaling cascade, affecting physiological processes...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/00001813-200502000-00004

    authors: Brantley E,Patel V,Stinson SF,Trapani V,Hose CD,Ciolino HP,Yeh GC,Gutkind JS,Sausville EA,Loaiza-Pérez AI

    更新日期:2005-02-01 00:00:00

  • Seven low-mass ions in pretreatment serum as potential predictive markers of the chemoradiotherapy response of rectal cancer.

    abstract::Preoperative chemoradiotherapy (CRT) is generally performed for locally advanced rectal cancer (LARC, cStage 2 or 3) to improve local disease control and patient survival. The pathological tumor response to CRT is a surrogate marker that is associated with oncological outcome. Thus, markers that predict the response t...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000391

    authors: Roh K,Yeo SG,Yoo BC,Kim KH,Kim SY,Kim MJ

    更新日期:2016-09-01 00:00:00

  • Pharmacokinetics of cabozantinib tablet and capsule formulations in healthy adults.

    abstract::Cabozantinib capsules (COMETRIQ) are approved for the treatment of patients with progressive metastatic medullary thyroid cancer. Cabozantinib tablets are investigational drug products considered to be potentially preferred pharmaceutical dosing forms. Two phase I open-label single-dose studies in healthy individuals ...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章,随机对照试验

    doi:10.1097/CAD.0000000000000366

    authors: Nguyen L,Benrimoh N,Xie Y,Offman E,Lacy S

    更新日期:2016-08-01 00:00:00

  • Tumour flare reaction in cancer treatments: a comprehensive literature review.

    abstract::In the past decade, tumour flare reaction (TFR) was considered as a new side effect associated with immunomodulatory agents (IMiDs) and as a condition of chronic lymphocytic leukaemia (CLL). However, this phenomenon is also observed with immune checkpoint inhibitors in solid tumours. It is still poorly understood and ...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章,评审

    doi:10.1097/CAD.0000000000000814

    authors: Taleb B A

    更新日期:2019-10-01 00:00:00

  • A phase I dose-escalation study of S-1 plus carboplatin in patients with advanced non-small-cell lung cancer.

    abstract::We conducted a phase I study to determine the maximum tolerated dose, the recommended dose and the safety profile of S-1 and carboplatin combination regimen in the treatment of patients with advanced non-small-cell lung cancer. Chemotherapy-naive patients with advanced non-small-cell lung cancer were treated with S-1 ...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0b013e32801265eb

    authors: Kaira K,Sunaga N,Yanagitani N,Imai H,Utsugi M,Shimizu Y,Iijima H,Tomizawa Y,Hisada T,Ishizuka T,Saito R,Mori M

    更新日期:2007-04-01 00:00:00

  • The clinical rationale for developing docetaxel (Taxotere).

    abstract::Clinical empiricism has recognized resistant breast cancer as a privileged target for docetaxel (Taxotere). This worldwide registration will offer medical oncologists the opportunity to develop new indications for docetaxel. Pharmacokinetics, preclinical optimal combination and clinical practice will constitute the ra...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章,评审

    doi:

    authors: Armand JP

    更新日期:1996-08-01 00:00:00