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 favorable pharmacokinetic attributes to exert its action as long as possible in the extravascular compartment of the extracellular space, with a short action intravascularly, avoiding bleeding and/or other undesirable side-effects. None of the thrombin inhibitors in clinical use has these properties. Here, we report for first time a direct thrombin inhibitor, named dipetarudin that could be very useful in antitumor therapy because of its pharmacokinetic behavior characterized by a rapid distribution in the extravascular space with a slow elimination from this compartment.

journal_name

Anticancer Drugs

journal_title

Anti-cancer drugs

authors

López ML,Nowak G

doi

10.1097/00001813-200402000-00007

subject

Has Abstract

pub_date

2004-02-01 00:00:00

pages

145-9

issue

2

eissn

0959-4973

issn

1473-5741

pii

00001813-200402000-00007

journal_volume

15

pub_type

杂志文章
  • Current chemotherapy of advanced non-small cell lung cancer.

    abstract::Systemic chemotherapy for patients with a good performance status and advanced non-small cell lung cancer may result in prolonged survival and improved quality of life. However, few single agents have an activity of more than 15% and they have significant toxicity. Cisplatin is widely regarded as the single agent of c...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章,评审

    doi:10.1097/00001813-199512006-00003

    authors: Abratt RP

    更新日期:1995-12-01 00:00:00

  • Synergistic killing effect of imatinib and simvastatin on imatinib-resistant chronic myelogenous leukemia cells.

    abstract::The antiproliferative effect of simvastatin on tumor cells has been speculated to be by intracellular signal inhibition through 3-hydroxy-3-methylglutaryl acetyl coenzyme A reductase. We examined the killing effect of simvastatin on imatinib-sensitive and resistant chronic myelogenous leukemia (CML) cells (three kinds...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0b013e32835a0fbd

    authors: Oh B,Kim TY,Min HJ,Kim M,Kang MS,Huh JY,Kim Y,Lee DS

    更新日期:2013-01-01 00:00:00

  • Effects of oxymatrine on the apoptosis and proliferation of gallbladder cancer cells.

    abstract::Gallbladder carcinoma is the most common malignancy of the biliary tract and is associated with a very poor outcome. The aim of the present study was to investigate the effects of oxymatrine (OM) on gallbladder cancer cells and the possible mechanism of its effects. The effects of OM on the proliferation of gallbladde...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000124

    authors: Wu XS,Yang T,Gu J,Li ML,Wu WG,Weng H,Ding Q,Mu JS,Bao RF,Shu YJ,Cao Y,Wang XA,Ding QC,Dong P,Xie SF,Liu YB

    更新日期:2014-10-01 00:00:00

  • D-TRP-6-LHRH (Triptorelin) is not effective in ovarian carcinoma: an EORTC Gynaecological Cancer Co-operative Group Study.

    abstract::Between March and September 1988, 74 patients with progressive ovarian cancer after prior platinum-based therapy were treated with the luteinizing hormone-releasing hormone (LHRH) agonist Triptorelin (Decapeptyl degrees). Treatment consisted of i.m. injection of 3.75 mg of microencapsulated Triptorelin on days 1, 8 an...

    journal_title:Anti-cancer drugs

    pub_type: 临床试验,杂志文章,多中心研究

    doi:10.1097/00001813-200102000-00010

    authors: Duffaud F,van der Burg ME,Namer M,Vergote I,Willemse PHB,ten Bokkel Huinink W,Guastalla JP,Nooij,Kerbrat P,Piccart M,Tumolo S,Favalli G,van der Vange N,Lacave AJ,Wils J,Splinter TA,Einhorn N,Roozendaal KJ,Rosso R,Ve

    更新日期:2001-02-01 00:00:00

  • Increased SPK1 expression promotes cell growth by activating the ERK1/2 signaling in non-small-cell lung cancer.

    abstract::Lung cancer remains the leading cause of cancer-associated mortality in China and the world. Increasing numbers of studies have reported that sphingosine kinase 1 (SPK1) is frequently highly expressed in tumors of various origins, including lung cancer, and its high expression contributes toward tumor progression. How...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000733

    authors: Yang Y,Zhao J,Hao D,Wang X,Wang T,Li H,Lv B

    更新日期:2019-06-01 00:00:00

  • MicroRNA-301b and its target gene synaptosome-associated protein 91 as important modulators in esophageal cancer: functional experiments.

    abstract::The aim of this study was to probe the influence of microRNA-301b (miR-301b) in esophageal cancer pathogenesis. Based on the data acquired from The Cancer Genome Atlas database, we found that miR-301b was highly expressed in esophageal cancer tissues and high expression of miR-301b was related to worse prognosis in pa...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000893

    authors: Pan F,Chen M,Song XY,Yang JD

    更新日期:2020-04-01 00:00:00

  • Dexmedetomidine suppresses the progression of esophageal cancer via miR-143-3p/epidermal growth factor receptor pathway substrate 8 axis.

    abstract::Esophageal cancer is one of the fatal cancers around the world. Dexmedetomidine (DEX) is widely used during anesthesia of esophageal cancer surgery. Nevertheless, the role of DEX in the progression of esophageal cancer remains barely known. The proliferation, apoptosis and metastasis of esophageal cancer cells were de...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000934

    authors: Zhang P,He H,Bai Y,Liu W,Huang L

    更新日期:2020-08-01 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

  • 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

  • In vitro and in vivo suppression of growth of hepatocellular carcinoma cells by novel traditional Chinese medicine-platinum anti-cancer agents.

    abstract::Protein phosphatase 2A (PP2A) is a new target for platinum (Pt)-based cancer chemotherapeutic agents. A series of novel Pt complexes containing demethylcantharidin, a modified component of a traditional Chinese medicine (TCM), [Pt(C8H8O5)(NH2R)2] 1-5 have been shown to inhibit PP2A both in its purified form and in cel...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/01.cad.0000175586.31940.50

    authors: To KK,Ho YP,Au-Yeung SC

    更新日期:2005-09-01 00:00:00

  • The immunocytokine L19-TNF eradicates sarcomas in combination with chemotherapy agents or with immune check-point inhibitors.

    abstract::Antibody-cytokine fusion proteins (also called 'immunocytokines') represent an emerging class of biopharmaceutical products, which are being considered for cancer immunotherapy. When used as single agents, pro-inflammatory immunocytokines are rarely capable of inducing complete and durable cancer regression in mouse m...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000938

    authors: Corbellari R,Nadal L,Villa A,Neri D,De Luca R

    更新日期:2020-09-01 00:00:00

  • Selenium and prevention of prostate cancer in high-risk men: the Negative Biopsy Study.

    abstract::Epidemiological and clinical studies suggesting a significant inverse relationship between intake of dietary selenium and overall cancer risk have led to initiation of a randomized, placebo-controlled, phase III clinical trial testing the safety and efficacy of selenized yeast as a chemopreventive agent for prostate c...

    journal_title:Anti-cancer drugs

    pub_type: 临床试验,杂志文章,多中心研究,随机对照试验

    doi:10.1097/00001813-200309000-00003

    authors: Stratton MS,Reid ME,Schwartzberg G,Minter FE,Monroe BK,Alberts DS,Marshall JR,Ahmann FR

    更新日期:2003-09-01 00:00:00

  • Comparison of the effect of the antiandrogen apalutamide (ARN-509) versus bicalutamide on the androgen receptor pathway in prostate cancer cell lines.

    abstract::Apalutamide (ARN-509) is an antiandrogen that binds selectively to androgen receptors (AR) and does not show antagonist-to-agonist switch like bicalutamide. We compared the activity of ARN versus bicalutamide on prostate cancer cell lines. The 22Rv1, PC3, and DU145 cell lines were used to study the effect of ARN and b...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000592

    authors: Koukourakis MI,Kakouratos C,Kalamida D,Mitrakas A,Pouliliou S,Xanthopoulou E,Papadopoulou E,Fasoulaki V,Giatromanolaki A

    更新日期:2018-04-01 00:00:00

  • The TYMS-TSER polymorphism is associated with toxicity of low-dose capecitabine in patients with advanced gastrointestinal cancer.

    abstract::Low doses of drugs delivered at close, regular intervals are increasingly being used to manage patients with different neoplasms. Despite the good tolerability, treatment-related adverse events still occur following metronomic protocols. The aim of this study was to retrospectively investigate whether polymorphisms of...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000429

    authors: Romiti A,Roberto M,D'Antonio C,Onesti CE,Barucca V,Milano A,Gentile G,Lionetto L,Medda E,Mazzuca F,Botticelli A,Falcone R,Simmaco M,Marchetti P

    更新日期:2016-11-01 00:00:00

  • Schlafen-11 sensitizes colorectal carcinoma cells to irinotecan.

    abstract::Schlafen-11 (SLFN11) showed a highly significant positive correlation with the response of topoisomerase inhibitors in cancer cell lines derived from prostate, lung, etc. However, this finding has not been validated in colorectal cancers (CRCs). Although irinotecan (CPT-11), a topoisomerase inhibitor, is one of the mo...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000151

    authors: Tian L,Song S,Liu X,Wang Y,Xu X,Hu Y,Xu J

    更新日期:2014-11-01 00:00:00

  • Phase II study of docetaxel in combination with oxaliplatin in patients with metastatic or locally advanced esophagogastric cancer previously untreated with chemotherapy for advanced disease: results of the Central European Cooperative Oncology Group Stud

    abstract::A phase II trial was performed to determine the efficacy and tolerance of docetaxel plus oxaliplatin with hematopoietic growth factor support in previously untreated patients with advanced gastroesophageal adenocarcinoma. Thirty-five patients were entered in this trial. Treatment consisted of 3-weekly docetaxel 80 mg/...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0b013e3282fb178a

    authors: Hejna M,Raderer M,Zacherl J,Ba-Ssalamah A,Püspök A,Schmidinger M,Pluschnig U,Brodowicz T,Zielinski CC

    更新日期:2008-06-01 00:00:00

  • The relationship between the antitumor activity and the ribonucleotide reductase inhibitory activity of (E)-2'-deoxy-2'-(fluoromethylene) cytidine, MDL 101,731.

    abstract::(E)-2'-deoxy-2'-(fluoromethylene) cytidine (MDL101,731) is a new deoxycytidine analog which shows potent antitumor activity against several human tumor models. We previously showed that MDL101,731 inhibited human ribonucleotide reductase (RNR) in HeLa S3 human cervical carcinoma cells. Recently, it has been reported t...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/00001813-199808000-00011

    authors: Kanazawa J,Takahashi T,Akinaga S,Tamaoki T,Okabe M

    更新日期:1998-08-01 00:00:00

  • Targeted therapy for lung cancer.

    abstract::Lung cancer is considered the number one killer among all cancers. Recent observations have altered the treatment paradigm for non-small-cell lung cancer (NSCLC). The discovery of activating mutations in the epidermal growth factor receptor and anaplastic lymphoma kinase positivity has made personalized treatment for ...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章,评审

    doi:10.1097/CAD.0b013e3283585149

    authors: Petrosyan F,Daw H,Haddad A,Spiro T

    更新日期:2012-11-01 00:00:00

  • Effect of a combination of S-1 and gemcitabine on cell cycle regulation in pancreatic cancer cell lines.

    abstract::In a previous study, we showed that a combination of an oral fluoropyrimidine anticancer agent (S-1) and gemcitabine (GEM) had synergistic effects on cell growth and cell cycle arrest in the pancreatic cancer cell line MIA PaCa-2. Therefore, we conducted further mechanistic studies using the pancreatic cancer cell lin...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0b013e328350e8c7

    authors: Morimoto Y,Takeuchi O,Takizawa A,Yoneyama H,Asanuma F,Suzuki Y,Atsuda K,Yamada Y

    更新日期:2012-06-01 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

  • Anticancer activities of alkylating pyrrole-imidazole polyamides with specific sequence recognition.

    abstract::In recent years, many diseases including cancer and hereditary and viral diseases have been understood at the DNA sequence level. Direct control of the expression level of a specific gene would provide a promising approach for knowledge-based therapy. N-methylpyrrole and N-methylimidazole polyamides are a new type of ...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章,评审

    doi:10.1097/CAD.0b013e328334d8f9

    authors: Shinohara K,Bando T,Sugiyama H

    更新日期:2010-03-01 00:00:00

  • A phase I study of paclitaxel, estramustine phosphate and vinorelbine (Pacl-E-Vin) in advanced malignancies: triple tubulin targeting.

    abstract::Anti-tubulin couplets have activity in hormone-resistant prostate cancer. This study was designed to define the dose-limiting toxicity (DLT) and recommended phase II dose (RPTD) of the unique triplet combination of paclitaxel, estramustine phosphate (EMP) and vinorelbine (Pacl-E-Vin). Patients with advanced malignanci...

    journal_title:Anti-cancer drugs

    pub_type: 临床试验,杂志文章

    doi:10.1097/00001813-200301000-00009

    authors: Sewak S,Chachoua A,Hamilton A,Taneja S,Lee J,Utate M,Sorich J,Muggia FM

    更新日期:2003-01-01 00:00:00

  • Bufalin enhances TRAIL-induced apoptosis by redistributing death receptors in lipid rafts in breast cancer cells.

    abstract::Studies have shown that tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) selectively induces apoptosis in cancer cells. However, breast cancer cells are generally resistant to TRAIL. In the present study, we explored the effect of bufalin on TRAIL-induced breast cancer cell apoptosis. The results showed...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000095

    authors: Yan S,Qu X,Xu L,Che X,Ma Y,Zhang L,Teng Y,Zou H,Liu Y

    更新日期:2014-07-01 00:00:00

  • Phase II study of miltefosine 6% solution as topical treatment of skin metastases in breast cancer patients.

    abstract::Topical treatment of skin metastases with a cytotoxic agent is attractive for its easy self-administration and absence of major systemic interference. Miltefosine exerts its cytotoxicity by acting on cell membrane phospholipids and can be administered topically. Twenty breast cancer patients with progression of skin m...

    journal_title:Anti-cancer drugs

    pub_type: 临床试验,杂志文章

    doi:10.1097/00001813-200011000-00006

    authors: Smorenburg CH,Seynaeve C,Bontenbal M,Planting AS,Sindermann H,Verweij J

    更新日期:2000-11-01 00:00:00

  • Doxorubicin induces apoptosis in Jurkat cells by mitochondria-dependent and mitochondria-independent mechanisms under normoxic and hypoxic conditions.

    abstract::In this study, we investigated the molecular mechanism of doxorubicin (dxr)-induced cytotoxicity on Jurkat cells - a model cell of human acute lymphoblastic leukemia - under normoxic (20% O2) and hypoxic (5% O2) conditions. Using in-cell western analysis, immunofluorescence, flow cytometry analysis, and biochemical in...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000223

    authors: Mendivil-Perez M,Velez-Pardo C,Jimenez-Del-Rio M

    更新日期:2015-07-01 00:00:00

  • Resveratrol inhibits STAT5 activation through the induction of SHP-1 and SHP-2 tyrosine phosphatases in chronic myelogenous leukemia cells.

    abstract::STAT5 is an important transcription factor that is constitutively activated in various types of malignancies, including chronic myelogenous leukemia (CML). Whether the antitumor effects of resveratrol (RES) are linked to its capability to inhibit STAT5 activation in CML cells was investigated. We found that RES inhibi...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000635

    authors: Li Q,Zhang L,Ma L,Bai X,Li X,Zhao M,Sui T

    更新日期:2018-08-01 00:00:00

  • Effect of dolastatin 10 on human non-Hodgkin's lymphoma cell lines.

    abstract::It is crucial to incorporate new and more potent antineoplastic agents in treating non-Hodgkin's lymphoma since standard chemotherapy fails to cause a significant increase in the survival rate. A potential chemotherapeutic agent is dolastatin 10; hence, the objective of our study is to investigate the effect of the an...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/00001813-199605000-00016

    authors: Maki A,Mohammad R,Raza S,Saleh M,Govindaraju KD,Pettit GR,al-Katib A

    更新日期:1996-05-01 00:00:00

  • Pharmacokinetics of methotrexate-albumin conjugates in tumor-bearing rats.

    abstract::Linking chemotherapeutic drugs to a macromolecular carrier system may enhance tumor targeting, reduce toxicity and overcome drug resistance mechanisms. As an elementary model to evaluate the pharmacological properties of macromolecular drug carrier systems we chose rat serum albumin (RSA) for carrier and methotrexate ...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/00001813-199710000-00004

    authors: Stehle G,Wunder A,Sinn H,Schrenk HH,Schütt S,Frei E,Hartung G,Maier-Borst W,Heene DL

    更新日期:1997-10-01 00:00:00

  • Safety of a second-generation tyrosine kinase inhibitor and novel targeted therapy for the treatment of a patient with chronic myeloid leukemia and multiple myeloma.

    abstract::The prevalence of chronic myeloid leukemia and multiple myeloma has increased in recent years partly because of an improved therapeutic armamentarium for both conditions. Likewise, understanding the complexity inherent in designing combination treatment strategies will become increasingly prescient in the coming years...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/CAD.0000000000000262

    authors: Katzel JA,Lee-Ma A,Vesole DH

    更新日期:2015-09-01 00:00:00

  • Compatibility and stability of Imexon in infusion devices and its in vitro biocompatibility.

    abstract::Imexon is an investigational anti-cancer agent, pharmaceutically formulated as a lyophilized solid for i.v. infusion requiring reconstitution and subsequent dilution in infusion fluid before infusion. Imexon contains a highly reactive aziridine ring in its structure, which limits its stability in aqueous solutions. In...

    journal_title:Anti-cancer drugs

    pub_type: 杂志文章

    doi:10.1097/01.cad.0000172833.70444.ba

    authors: den Brok MW,Nuijen B,Challa EE,Lutz C,Opitz HG,Beijnen JH

    更新日期:2005-08-01 00:00:00