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 the present study, several in vitro studies were conducted to determine the administration parameters for use in the forthcoming phase I clinical trial. The stability of Imexon in the reconstituted solution and infusion solutions was investigated, including its tendency to degrade to its main degradation product BM41.209, and to its hydroxy and chloride adducts. The compatibility of the infusion solution with glass, low-density polyethylene and freeflex polyolefin containers, and its potency to cause vascular irritation and hemolysis upon i.v. infusion were investigated. Imexon was found to be stable for 8 h in the reconstituted product and for 2 h after dilution to infusion solution concentrations in normal saline. The infusion solution was compatible with the freeflex polyolefin container and polyvinylchloride infusion lining, showing no sorption of Imexon during a 15-min infusion duration and no release of the plasticizer diethylhexyl phthalate. Furthermore, Imexon infusion solution showed no indication for vascular irritation or hemolysis upon i.v. infusion, as measured with a static in vitro model with incubation with whole blood. In conclusion, Imexon should be administered using a freeflex polyolefin infusion container within 2 h after preparation and a 15-min infusion duration. The results obtained with an in vitro model show that no vascular irritation or hemolysis is expected upon i.v. infusion.
journal_name
Anticancer Drugsjournal_title
Anti-cancer drugsauthors
den Brok MW,Nuijen B,Challa EE,Lutz C,Opitz HG,Beijnen JHdoi
10.1097/01.cad.0000172833.70444.basubject
Has Abstractpub_date
2005-08-01 00:00:00pages
727-32issue
7eissn
0959-4973issn
1473-5741pii
00001813-200508000-00005journal_volume
16pub_type
杂志文章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
更新日期:1990-10-01 00:00:00
abstract::Targeted agents such as sunitinib, an oral, multitargeted receptor tyrosine kinase inhibitor, have greatly improved the prognosis for patients with metastatic renal cell carcinoma (mRCC). In this review we analyse data from sunitinib preclinical and clinical studies in detail and consider the key implications for the ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
doi:10.1097/CAD.0b013e3283442039
更新日期:2011-06-01 00:00:00
abstract::In an effort to develop new agents and molecular targets for the treatment of cancer, aspargine-glycine-arginine (NGR)-targeted liposomal doxorubicin (TVT-DOX) is being studied. The NGR peptide on the surface of liposomal doxorubicin (DOX) targets an aminopeptidase N (CD13) isoform, specific to the tumor neovasculatur...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e3282a213ce
更新日期:2007-11-01 00:00:00
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
更新日期:2016-09-01 00:00:00
abstract::Since the number of patients seen in a pediatric oncology center is relatively small, it is difficult to perform single drug phase two studies, even on a national base. This also probably explains the lack of information on ifosfamide, despite the fact that it has now been used for more than 10 years in pediatrics. As...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
doi:10.1097/00001813-199108000-00002
更新日期:1991-08-01 00:00:00
abstract::Metformin, an oral antidiabetic agent, has been reported to potentiate chemotherapeutic-induced cytotoxicity. In this study, we investigated the effects and molecular mechanisms of metformin in sensitizing tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-induced apoptosis in human bladder cancer cells. ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000116
更新日期:2014-09-01 00:00:00
abstract::Neuroblastoma is one of the most common cancers in infancy, arising from the neuroblasts during embryonic development. This cancer is difficult to treat and resistance to chemotherapy is often found; therefore, clinical trials of novel therapeutic approaches, such as targeted-cancer signaling, could be an alternative ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000478
更新日期:2017-06-01 00:00:00
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journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e32832fe48f
更新日期:2009-10-01 00:00:00
abstract::Gossypol [(2,2'-binaphthalene)-8,8'-dicarboxaldehyde-1,1',6,6',7,7'-hexahydroxy-5,5'-diisopropyl-3,3'-dimethyl] 1a is a naturally occurring compound extracted from the cotton plant and has been extensively studied as an oral male contraceptive. Its favorable toxicity profile, and the more recent demonstration of anti-...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200003000-00009
更新日期:2000-03-01 00:00:00
abstract::Irinotecan (CPT-11) is a camptothecin analog with low (about 10--20%) and variable oral bioavailability in animal models. Here, Caco-2 cells were used to evaluate the transepithelial transport of CPT-11 and its metabolites. Caco-2 cells demonstrated significant expression of P-glycoprotein (P-gp), multidrug resistance...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200106000-00003
更新日期:2001-06-01 00:00:00
abstract::Desmoid tumour/aggressive fibromatosis (DT/AF) is a rare soft-tissue neoplasm that is locally aggressive but does not metastasize. There is no standard systemic treatment for symptomatic patients, although a number of agents are used. Tyrosine kinase inhibitors have recently been reported to show useful activity. We r...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000474
更新日期:2017-04-01 00:00:00
abstract::Our previous studies have shown that arsenic trioxide (As2O3), a novel anti-cancer agent, may be active against urothelial carcinomas. A series of bladder urothelial carcinoma cells with progressive As2O3 resistance were established and studied to reveal molecular events in relation to the mechanisms of resistance to ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200409000-00007
更新日期:2004-09-01 00:00:00
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
更新日期:1991-12-01 00:00:00
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
更新日期:2018-04-01 00:00:00
abstract::Macroautophagy (hereafter referred to as autophagy) plays essential roles in cellular and organismal homeostasis. Transcription factor EB (TFEB) is a master regulator of autophagy and lysosome biogenesis. It is not fully understood how the function of TFEB in autophagy pathway is regulated. Here, we show that Rac1 GTP...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000816
更新日期:2019-11-01 00:00:00
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
更新日期:2005-09-01 00:00:00
abstract::Since their addition to paclitaxel in the oncologists' armamentarium in the early 1990s, several new taxane formulations have been developed. Besides docetaxel and nab-paclitaxel, new analogs with better therapeutic profiles are being investigated. The goals of this next generation of taxanes are to improve the toxici...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
doi:10.1097/CAD.0000000000000053
更新日期:2014-05-01 00:00:00
abstract::Our previous studies have demonstrated the in-vitro and in-vivo targeting of a generation-5 (G5) dendrimer-based multifunctional conjugate, which used folic acid (FA) as the targeting agent and methotrexate (MTX) as the chemotherapeutic drug. For the synthesized G5-FA-MTX nanodevice conjugate to be clinically applicab...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e3282f28842
更新日期:2008-02-01 00:00:00
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:
更新日期:1996-08-01 00:00:00
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journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200507000-00006
更新日期:2005-07-01 00:00:00
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journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199204000-00008
更新日期:1992-04-01 00:00:00
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journal_title:Anti-cancer drugs
pub_type: 杂志文章
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更新日期:2016-11-01 00:00:00
abstract::In a recent study we demonstrated that recombinant human growth hormone (r-hGH; Saizen) delayed tumor-induced cachexia in human tumor xenografts in vivo. Such a therapeutic effect could have a great impact in the supportive care of advanced cancer patients. Before large clinical studies are initiated possible growth s...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200009000-00011
更新日期:2000-09-01 00:00:00
abstract::The efficacy of trastuzumab beyond metastatic disease progression (PD) is controversial. We retrospectively analyzed 213 patients with HER2-positive metastatic breast cancer treated with trastuzumab-based therapies between November 1998 and December 2010. Out of 213 patients, 134 (58%) had received trastuzumab consecu...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e32835679d3
更新日期:2012-11-01 00:00:00
abstract::Topoisomerase IIα is a nuclear enzyme that alters DNA topology. It is a well-known anticancer target and related to cell differentiation status. All-trans retinoic acid (ATRA), an important active metabolite of vitamin A, is a promising anticancer agent in numerous malignancies. However, there are little data on the e...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000241
更新日期:2015-08-01 00:00:00
abstract::A new dosage form (ACR-CH) comprising aclarubicin adsorbed on activated carbon particles was designed to sustain release of aclarubicin. ACR-CH or aclarubicin aqueous solution (ACR-sol) was injected subcutaneously into the fore foot-pads of rats. ACR-CH distributed a statistically significantly higher level of aclarub...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199106000-00006
更新日期:1991-06-01 00:00:00
abstract::The role and regulation of the c-myc protooncogene in breast and ovarian neoplasms is receiving increased attention. The downregulation of the c-myc protooncogene by 1,25-dihydroxyvitamin D3 (calcitriol), retinoic acid (RA) and dexamethasone (Dex) is closely associated with growth inhibition in leukemic cells. Calcitr...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199304000-00012
更新日期:1993-04-01 00:00:00
abstract::Chemotherapy for breast cancer is given on the basis of empirical information from clinical trials, an approach which falls to take into account the known heterogeneity of chemosensitivity between patients. Previous attempts to determine chemosensitivity ex vivo have been disappointing, but in this study results from ...
journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章
doi:10.1097/00001813-199608000-00002
更新日期:1996-08-01 00:00:00
abstract::The epithelial-mesenchymal transition (EMT) plays an important role in inducing cancer metastasis. Baicalin, a flavone derivative isolated from Scutellaria spp., shows a series of pharmacological and physiological activities. However, the possible role of baicalin in the EMT is unclear. In this study, we attempted to ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000495
更新日期:2017-07-01 00:00:00
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
更新日期:2015-01-01 00:00:00