Abstract:
:Declopramide (3-chloroprocainamide) has been identified in previous studies as a representative of a new class of chemosensitizers. In this study, the toxicity and pharmacokinetics of declopramide have been investigated and compared with a structural analog, metoclopramide (MCA). Declopramide has not induced central nervous system (CNS)-related side effects in rats at doses up to 200 mg/kg, whereas MCA does at 12.5 mg/kg. In addition, declopramide did not bind to dopamine D2 receptors in subcellular preparations at doses up to 100 microM, whereas MCA showed affinity at 1 microM. Declopramide bound with affinity to 5-hydroxytryptamine3 receptors which are important in controlling vomiting. In contrast to MCA, declopramide has a rapid clearance from serum, a lower tissue concentration (about 15-fold lower than MCA) and a lower oral bioavailability (about 6-fold lower than MCA). However, declopramide was shown in vitro to possess a higher tumor cell absorption rate. One of the main metabolites of declopramide was identified as N-acetyl declopramide. Taken together, these data suggest that the clinical development of declopramide as a sensitizer of radio- and chemotherapies is an improvement over MCA, because it can be administered in a high dose and is devoid of CNS side effects.
journal_name
Anticancer Drugsjournal_title
Anti-cancer drugsauthors
Hua J,Pero RW,Kane Rdoi
10.1097/00001813-199901000-00010subject
Has Abstractpub_date
1999-01-01 00:00:00pages
79-88issue
1eissn
0959-4973issn
1473-5741journal_volume
10pub_type
杂志文章abstract::C-reactive protein (CRP) is an independent prognostic factor for renal cell carcinoma (RCC). The aim of the present study was to investigate the overall prognostic impact of CRP in patients with metastatic RCC treated with sorafenib. Between April 2008 and December 2014, 40 consecutive patients with metastatic RCC wer...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000417
更新日期:2016-11-01 00:00:00
abstract::Fifty-five consecutive patients with metastatic breast cancer (MBC) (n = 57) were treated with a combination of levofolinic acid (I-FA) 100 mg/m2 plus 5-fluorouracil (5-FU) 340 mg/m2 i.v. on day 1-3, cyclophosphamide (CTX) 600 mg/m2 i.v. on day 1 and mitoxantrone (DHAD) 12 mg/m2 i.v. on day 1. DHAD dose was progressiv...
journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章,多中心研究
doi:10.1097/00001813-199703000-00006
更新日期:1997-03-01 00:00:00
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
更新日期:2014-07-01 00:00:00
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
更新日期:1996-05-01 00:00:00
abstract::The co-operative effects of recombinant human tumor necrosis factor (rH-TNF) and CPT-11, a new derivative of camptothecin, against the proliferation of human gynecologic tumor cell lines were examined in vitro. The ishikawa cells were responsive to rH-TNF, the HHUA cells exhibited a minimal degree of responsiveness to...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199110000-00006
更新日期:1991-10-01 00:00:00
abstract::An i.v. formulation of rubitecan (9-nitrocamptothecin) was evaluated in five human solid tumor xenograft models. Rubitecan in IDD-P, a particulate suspension of the insoluble analog, produced significant tumor growth delay in athymic nude mice bearing A375 melanoma, and MX-1 breast, SKMES non-small-cell lung, Panc-1 p...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200210000-00009
更新日期:2002-10-01 00:00:00
abstract::High expression of vascular endothelial growth factor (VEGF) in patients with breast cancer has been associated with a poor prognosis, indicating that VEGF could be linked to the efficacy of chemotherapy and radiotherapy. It has also been suggested that radiation resistance is partly due to tumour cell production of a...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e32834ea5b3
更新日期:2012-06-01 00:00:00
abstract::The recombinant monoclonal antibody trastuzumab has antiproliferative effect on breast cancer (BC) cells with ErbB2 overexpression. We postulated that a mechanism able to modify ErbB2 expression enhances the antitumor effect of trastuzumab. We analyzed whether granulocyte-colony stimulating factor (G-CSF), widely used...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e3283050083
更新日期:2008-08-01 00:00:00
abstract::Treatment failure of surgically treated gastric cancer is attributed to the spread of gastric cancer cells into the abdominal cavity and lymphatic or hematogenic canals. In the present study, local injection of mitomycin C bound to activated carbon (M-CH) combined with i.p. hyperthermic hypo-osmolar infusion (IPHHOI) ...
journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1097/00001813-200204000-00013
更新日期:2002-04-01 00:00:00
abstract::Apoptosis is important for normal development and removal of damaged cells. Evasion of apoptosis by cancer cells is one of the key characteristics of many tumor types. Thus, discovering agents that promote apoptosis in tumor cells could have great therapeutic value. Marine natural products have demonstrated great pote...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e32832ae55f
更新日期:2009-07-01 00:00:00
abstract::The therapeutic effects of the new anti-angiogenesis factor TNP-470 were examined against carcinomatous peritonitis in mice. In the first experiment using carcinomatous peritonitis caused by i.p. inoculation of 10(6) M5076 tumor cells, TNP-470 solution was injected i.p. in a bolus of 50 mg/kg body weight into two grou...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199506000-00012
更新日期:1995-06-01 00:00:00
abstract::9-Nitrocamptothecin (9NC) is a water-insoluble topoisomerase I inhibitor with a broad antitumor activity in animal models. To determine the maximum tolerated oral dose (MTD), a phase I study was performed in patients with advanced cancer refractory to conventional chemotherapy. 9NC was administered orally with escalat...
journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章
doi:10.1097/00001813-199801000-00004
更新日期:1998-01-01 00:00:00
abstract::We evaluated the therapeutic activity and safety of continuously infused mitomycin C in patients with metastatic colorectal cancer who had recurred (less than 3 months) or progressed following first- or second-line 5-fluorouracil-based chemotherapy. Treatment consisted of mitomycin C 20 mg/m2 i.v. given over 120 h (5 ...
journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章
doi:10.1097/00001813-199806000-00009
更新日期:1998-06-01 00:00:00
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
更新日期:2019-10-01 00:00:00
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
更新日期:2014-10-01 00:00:00
abstract::Overexpression of the multidrug resistance MDR1 gene product P-glycoprotein and/or the multidrug resistance-associated protein MRP confers multidrug resistance to cancer cells. The pipecolinate derivative VX-710 has previously been demonstrated to reverse MDR1-mediated multidrug resistance at concentrations of 0.5-2.5...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199702000-00005
更新日期:1997-02-01 00:00:00
abstract::Targeted cancer chemotherapy is a novel approach developed for the specific delivery of anticancer drugs. Tumour targeting can be achieved by combining a chemotherapeutic agent with a targeting moiety that recognizes tumour-specific or highly expressed receptors on cancer cells. We used the gonadotropin-releasing horm...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e32834bb6b4
更新日期:2012-01-01 00:00:00
abstract::We have established estrogen-independent and antiestrogen-resistant cell lines from hormone-dependent MCF-7 breast cancer cells by long-term culture in the absence of estrogen, or in the presence of antiestrogen toremifene, respectively. By using a cDNA microarray we compared gene expression profiles among estrogen-in...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e32831845e1
更新日期:2009-01-01 00:00:00
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journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000031
更新日期:2014-02-01 00:00:00
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journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199208000-00015
更新日期:1992-08-01 00:00:00
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:
更新日期:2002-05-01 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::The aim of this study was to evaluate whether radiolabeled iodoerythronitroimidazole (IETNIM) could predict the radiosensitization effect on tumors. Tumor-bearing mice were irradiated at a dose of 25, 31 and 37 Gy after the injection of IETNIM. They were also exposed to 37 Gy radiation at 35, 70, 140 and 240 min after...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199611000-00007
更新日期:1996-11-01 00:00:00
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journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
doi:10.1097/CAD.0b013e3283585149
更新日期:2012-11-01 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
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journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章
doi:10.1097/00001813-199707000-00003
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journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
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journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章
doi:10.1097/00001813-200206000-00007
更新日期:2002-06-01 00:00:00
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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
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journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e32834f7ef4
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