Abstract:
:13,14-Dihydro-15-deoxy-Delta7-prostaglandin A1 methyl ester (TEI-9826), an antitumor prostaglandin analog, is a candidate for clinical trial. In the present study, we examined its biological stability in vitro, antitumor activity in vitro and in vivo, and pharmacokinetics. Although TEI-9826 was rapidly hydrolyzed to the carboxylic acid form (TOK-4528), TOK-4528 as well as Delta12-prostaglandin J2 (PGJ2) were found to be stable in rat, mouse and human serum in vitro. TEI-9826 exhibited nearly identical or greater potential antitumor activity compared to Delta12-PGJ2 and Delta7-PGA1 in vitro against Colon26 tumor cells. Further evaluation of TEI-9826 using the 38 human cancer cell lines panel and COMPARE analysis suggested that its mode of action is quite different from other anticancer agents that are currently used. TEI-9826 was integrated into lipid microspheres (Lipo TEI-9826) for dosing. Growth inhibition by Lipo TEI-9826 against Colon26 tumor inoculated s.c. in mice depended on administration route, i.e. at 80 mg/kg, no growth suppressive effect was observed for daily bolus i.v., but significant growth suppressive effect was observed for daily i.p., daily s.c. every other day s.c. and 4 times a day continuous (5 min) i.v. These tumor growth-suppressive effects were cytostatic and the tumor started to regrow at the end or a few days after the end of administration. The pharmacokinetic study suggested that maintaining the blood level of TEI-9826 and/or TOK-4528 was essential for their antitumor effects. These results show that continuous i.v. infusion might be the most suitable administration method of Lipo TEI-9826 for clinical trial.
journal_name
Anticancer Drugsjournal_title
Anti-cancer drugsauthors
Fukushima S,Takeuchi Y,Kishimoto S,Yamashita S,Uetsuki K,Shirakawa S,Suzuki M,Furuta K,Noyori R,Sasaki H,Kikuchi Y,Kita T,Yamori T,Sawada J,Kojima M,Hazato A,Kurozumi S,Fukushima Mdoi
10.1097/00001813-200103000-00008subject
Has Abstractpub_date
2001-03-01 00:00:00pages
221-34issue
3eissn
0959-4973issn
1473-5741journal_volume
12pub_type
杂志文章abstract::Verapamil, cyclosporin A (CsA), the cyclosporin derivative SDZ PSC 833 and the novel cyclopeptolide SDZ 280-446 were tested for their capacity to chemosensitize a P-glycoprotein (Pgp)-expressing multi-drug resistant (MDR) variant of the CEM human T lymphoblastoid cell subline (CCRF ACTD 400+). That MDR-CEM cell sublin...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:
更新日期:1993-12-01 00:00:00
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
更新日期:2008-03-01 00:00:00
abstract::Marine alkaloid meridianin G derivatives, substituted on the pyrimidine ring by aryl groups, were evaluated for their kinase inhibitory potencies and their in-vitro antiproliferative activities. The derivatives were tested toward a panel of nine protein kinases (KDR, IGF-1R, c-Met, RET, c-Src, c-Abl, PKA, CDK2/cyclin ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e32830ce4d8
更新日期:2008-09-01 00:00:00
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
更新日期:2003-09-01 00:00:00
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
更新日期:2007-06-01 00:00:00
abstract::To compare the mechanical and chemical properties of three commercially available microspheres loaded with irinotecan. LifePearl (200 µm), DC Bead (100-300 µm), and Tandem (100 µm) microspheres were loaded with irinotecan. For loading, elution, and stability determinations, irinotecan concentrations were quantified us...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000408
更新日期:2016-10-01 00:00:00
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
更新日期:2019-10-01 00:00:00
abstract::Results are summarized for two phase II studies of docetaxel as first-line therapy for advanced squamous cell carcinoma of the head and neck (SCCHN) and one study of docetaxel as second-line therapy for advanced soft tissue sarcomas. In all three studies, docetaxel was administered at a dose of 100 mg/m2 by intravenou...
journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章,多中心研究
doi:10.1097/00001813-199507004-00004
更新日期:1995-07-01 00:00:00
abstract::At the present time, there is not a standard regimen in upfront metastatic setting for breast cancer. A wide variety of regimens which includes anthracyclines, taxanes, gemcitabine or capecitabine are currently used, however, there is evidence to support the use of many of these drugs in early breast cancer and conseq...
journal_title:Anti-cancer drugs
pub_type:
doi:10.1097/CAD.0b013e3280bad81a
更新日期:2007-08-01 00:00:00
abstract::Oxaliplatin (L-OHP), irinotecan (CPT-11) and 5-fluorouracil (5-FU) have shown their efficacy in metastatic colorectal cancer. The synergism of these drugs has been demonstrated in vivo and in vitro. The aim of this study was to determine the recommended dose of the triple combination of L-OHP, CPT-11 and CI 5-FU for a...
journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章
doi:10.1097/01.cad.0000127146.50172.8a
更新日期:2004-06-01 00:00:00
abstract::Neoadjuvant TPF (docetaxel, cisplatin, 5-fluorouracil), followed by radiotherapy or chemoradiotherapy with weekly carboplatin, increases overall survival and organ preservation. We assessed whether TPF could be used in routine practice and whether radiotherapy potentiated with cisplatin or cetuximab was feasible and c...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,多中心研究
doi:10.1097/CAD.0b013e328360b9d6
更新日期:2013-07-01 00:00:00
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
更新日期:1996-09-01 00:00:00
abstract::Cerebral gliomas have a poor survival time even after multimodal treatment, because of the unavoidable recurrence of tumor. Several trials with a combination of old and new chemotherapics have been performed, but survival time remains generally less than 12 months. Tamoxifen (TAM) has recently been shown to inhibit th...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
doi:10.1097/00001813-199808000-00001
更新日期:1998-08-01 00:00:00
abstract::Combretastatin A4 phosphate (CA4P) is a prodrug that selectively destroys tumor blood vessels, and has shown efficacy as a targeted anticancer drug in both animal models and clinical trials. The aims of this single-center, open label, phase I clinical trial were to investigate the safety and tolerability of CA4P admin...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000070
更新日期:2014-04-01 00:00:00
abstract::Trimetrexate (TMQ), a non-classical folate antagonist, was studied in a randomized controlled trial in patients with advanced colorectal cancer and without prior chemotherapy. Patients were randomly assigned to one of three treatments: TMQ at 200 mg/m2 i.v. q 2 weeks, TMQ at 12 mg/m2 i.v. daily x 5 or 5-fluorouracil (...
journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1097/00001813-199504000-00004
更新日期:1995-04-01 00:00:00
abstract::It is well known that the anti-cancer drug cisplatin has an ototoxic property; however, the details are not yet evident. In this study, the expression of inducible nitric oxide synthase (INOS/NOS II) in the vestibule of guinea pigs after i.p. injections of cisplatin was examined immunohistochemically. Three days after...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200001000-00005
更新日期:2000-01-01 00:00:00
abstract::The antitumor effect of etoposide (ETO) may be related to duration of exposure to a relatively low serum level while myelosuppression may be dependent on peak ETO serum levels. With regard to such therapeutic ranges, duration of exposure to predefined plasma ETO concentration ranges and the related AUC (expressed as p...
journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章
doi:10.1097/00001813-199910000-00003
更新日期:1999-10-01 00:00:00
abstract::The purpose of the current study was to develop and test a theoretical model that could explain the mechanism of action of gallic acid (GA) in the oral squamous cell carcinoma context for the first time. The theoretical model was developed using bioinformatics and interaction network analysis to evaluate the effect of...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000342
更新日期:2016-06-01 00:00:00
abstract::One hundred and thirty-one children with a median age of 5 years were administered Navoban (tropisetron), a selective antagonist of the serotonin receptor (5-HT3), dosed once daily at 0.2 mg/kg (with a maximum of 5 mg daily) in a study aimed at evaluating the prevention of nausea and vomiting induced by anti-cancer ch...
journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章,多中心研究
doi:10.1097/00001813-199502001-00003
更新日期:1995-02-01 00:00:00
abstract::Octreotide appears to have a major therapeutic effect in the management of diarrhoea related to cancer therapy. This effect is seen in the acute diarrhoea following radiation therapy and chemotherapy, and also in late radiation enteritis. As well as providing improved symptom control, early treatment can prevent poten...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
doi:10.1097/00001813-199601001-00003
更新日期:1996-01-01 00:00:00
abstract::Amifostine is a broad-spectrum cytoprotective agent approved for protection against cisplatin toxicities and radiation-induced xerostomia; strong clinical evidence exists that amifostine protects normal mucosa and lung from radiation damage. Hypotension, nausea/vomiting, fatigue and fever/rash are the main side-effect...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
doi:10.1097/00001813-200602000-00003
更新日期:2006-02-01 00:00:00
abstract::Management of gastric cancer in older adults is challenging. Perioperative treatment with epirubicin, cisplatin, and 5-fluorouracil combination chemotherapy and surgery is considered the standard treatment of locally advanced gastric adenocarcinoma. However, this chemotherapy regimen is not well tolerated in older adu...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e32834a2c16
更新日期:2011-11-01 00:00:00
abstract::Although baseline plasma homocysteine levels are related to pemetrexed toxicities in patients treated without folate supplementation, the relationship between these parameters in patients treated with folate supplementation is not well understood. The pretreatment plasma homocysteine levels were measured in non-small-...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000220
更新日期:2015-06-01 00:00:00
abstract::Bifunctional chloroethylating cytostatic agents produce lethal DNA lesions, as a result of the formation of O6-alkylguanines. These lesions can be repaired by O6-methylguanine-DNA methyltransferase (MGMT). This ubiquitous nuclear and cytosolic enzyme removes the alkyl group by accepting it to the cysteine residue of i...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199608000-00012
更新日期:1996-08-01 00:00:00
abstract::Hemolytic uremic syndrome (HUS) is a rare clinical and biological entity. HUS has been reported after several anticancer chemotherapies and most often after mitomycin C-based chemotherapy regimens. Little information is available concerning the occurrence and outcome of this syndrome after administration of more recen...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199907000-00004
更新日期:1999-07-01 00:00:00
abstract::To devise a meaningful nutritional therapy in cancer, a greater understanding of nutritional dimensions as well as of expectations of patients and disease impact is essential. We have shown that nutritional deterioration in patients with gastrointestinal and head and neck cancer was multifactorial and mainly determine...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
doi:10.1097/CAD.0b013e328345b4c5
更新日期:2011-08-01 00:00:00
abstract::Tumor-to-tumor metastasis is a rare phenomenon, with around 150 cases being reported in the literature. Breast cancer is the second most commonly reported donor tumor after lung cancer, but thymic epithelial tumors have never been reported as recipient tumors. Furthermore, the thymus is rarely affected by metastases. ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e328362a68b
更新日期:2013-08-01 00:00:00
abstract::A functionalized poly(amidoamine) (PAMAM) nanocarrier was designed and prepared to deliver anticancer drugs. The nanocarrier is a copolymer with a core-shell structure with 3.0 G PAMAM as the core and sequentially conjugated poly(2-(N,N-diethylamino)ethyl methacrylate) (pDEA) and methoxy-poly(ethylene glycol) 2000 (mP...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e32835920fa
更新日期:2013-02-01 00:00:00
abstract::Two young adults that presented with intra-abdominal desmoplastic small cell tumors (DSCT) without any evidence of a primary site are described. Both cases share the clinical characteristic features of this rare tumor which include predominant intra-abdominal location as initial presentation, nesting pattern of growth...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:
更新日期:1996-02-01 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