Synthesis and in vitro antiproliferative activity against human cancer cell lines of novel 5-(4-methyl-benzylidene)-thiazolidine-2,4-diones.

abstract：OBJECTIVE:Axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptors 1, 2, and 3, is metabolized primarily by cytochrome P450 (CYP) 3A with minor contributions from CYP1A2, CYP2C19, and glucuronidation. Co-administration with CYP inhibitors may increase systemic expos...

journal_title：Investigational new drugs

authors： Pithavala YK,Tong W,Mount J,Rahavendran SV,Garrett M,Hee B,Selaru P,Sarapa N,Klamerus KJ

更新日期：2012-02-01 00:00:00

abstract：:Purpose Anticancer agents are known to increase cancer-associated thrombosis (CAT) onset. CAT onset rate is reported to be 1.92% in cisplatin-based therapy, 6.1% in paclitaxel plus ramucirumab combination therapy, and 11.9% in bevacizumab monotherapy. Because immune checkpoint inhibitors (ICIs) cause a sudden increase...

journal_title：Investigational new drugs

authors： Ando Y,Hayashi T,Sugimoto R,Nishibe S,Ito K,Kawada K,Ikeda Y,Yamada S,Imaizumi K

更新日期：2020-08-01 00:00:00

abstract：:Drug lag, which delays patients' access to medicinal products, is typically associated with pharmaceutical regulations. To shorten drug lag, health authorities may establish new policies to liberalize the regulations, a step that is important in countries, such as Taiwan, with consumer demand for imported novel therap...

journal_title：Investigational new drugs

authors： Sun IC

更新日期：2019-10-01 00:00:00

abstract：:Sorafenib, an orally active multi-kinase inhibitor approved for the treatment of hepatocellular carcinoma (HCC), is primarily metabolized both via cytochrome P450 3A4 isoform (CYP3A4) and UGT1A9. Due to the contribution of these two biotransformation pathways, sorafenib is considered to be less susceptible than other ...

journal_title：Investigational new drugs

authors： Gomo C,Coriat R,Faivre L,Mir O,Ropert S,Billemont B,Dauphin A,Tod M,Goldwasser F,Blanchet B

更新日期：2011-12-01 00:00:00

abstract：PURPOSE:To assess the maximum well-tolerated dose (MWTD), dose limiting toxicity (DLT), pharmacokinetics (PK) and pharmacodynamics of zibotentan, a novel specific endothelin-A receptor antagonist, in patients with metastatic prostate cancer. METHODS:Patients with metastatic, castrate-resistant prostate cancer (CRPC) w...

journal_title：Investigational new drugs

authors： Schelman WR,Liu G,Wilding G,Morris T,Phung D,Dreicer R

更新日期：2011-02-01 00:00:00

abstract：:Background This open-label, first-in-human, phase 1 study evaluated AMG 232, an oral selective MDM2 inhibitor in patients with TP53 wild-type (P53WT), advanced solid tumors or multiple myeloma (MM). Methods In the dose escalation (n = 39), patients with P53WT refractory solid tumors enrolled to receive once-daily AMG ...

journal_title：Investigational new drugs

authors： Gluck WL,Gounder MM,Frank R,Eskens F,Blay JY,Cassier PA,Soria JC,Chawla S,de Weger V,Wagner AJ,Siegel D,De Vos F,Rasmussen E,Henary HA

更新日期：2020-06-01 00:00:00

abstract：:Crizotinib is a receptor tyrosine kinase inhibitor that has several targets, including c-ros oncogene 1 and the MET proto-oncogene. Considering its known cardiac toxicity, bradycardia is often investigated following treatment with crizotinib. Our patients had bradycardia, QT prolongation, ventricular rhythm, ventricul...

journal_title：Investigational new drugs

authors： Oyakawa T,Muraoka N,Iida K,Kusuhara M,Kawamura T,Naito T,Takahashi T

更新日期：2018-10-01 00:00:00

abstract：:Idarubicin, a new analogue of daunorubicin, was administered to 27 patients with advanced breast cancer in a phase II trial. The drug was given orally at a dose of 30-35 mg/m2 every 3 weeks. Twenty-two patients were evaluable for response. All evaluable patients were previously treated with one or more chemotherapeuti...

journal_title：Investigational new drugs

authors： Lopez M,Di Lauro L,Papaldo P,Lazzaro B,Ganzina F,Di Pietro N

更新日期：1986-01-01 00:00:00

abstract：:Standard therapy for advanced or metastatic non-small cell lung cancer (NSCLC) has primarily consisted of traditional cytotoxic chemotherapy, although use of targeted therapies has been approved in specific settings. Antiangiogenic agents represent a promising therapeutic strategy for treatment of advanced NSCLC. Beva...

journal_title：Investigational new drugs

authors： Blumenschein GR Jr

更新日期：2012-08-01 00:00:00

abstract：:Aims A primary objective of this study was to investigate the effect of single and multiple doses of alisertib, an investigational Aurora A kinase inhibitor, on the QTc interval in patients with advanced malignancies. The dose regimen used was the maximum tolerated dose which was also the recommended phase 3 dose (50 ...

journal_title：Investigational new drugs

authors： Zhou X,Nemunaitis J,Pant S,Bauer TM,Patel M,Sarantopoulos J,Craig Lockhart A,Goodman D,Huebner D,Mould DR,Venkatakrishnan K

更新日期：2018-04-01 00:00:00

abstract：:Thirty-three patients with advanced colorectal carcinoma were entered on a phase II trial of weekly IV aminothiadiazole (175 mg/m2 escalated to 200 mg/m2) with concomitant allopurinol and non-steroidal anti-inflammatory agents (NSAID's). Toxicity was predominantly GI, cutaneous, and chest pain/dyspnea. Twenty-five per...

journal_title：Investigational new drugs

authors： Locker GY,Kilton L,Khandekar JD,Lad TE,Knop RH,Albain K,Blough R,French S,Benson AB 3rd

更新日期：1994-01-01 00:00:00

abstract：:Castrate-Resistant Prostate-Cancer (CRPC) is one of the most common malignancies occurring in men. Unfortunately, even if several recently approved agents clinically improved the outcome of CRPC patients, none of these is curative especially for a splice version of the Androgen Receptor (AR) AR-V7, which is a variant ...

journal_title：Investigational new drugs

authors： Sobhani N,Generali D,D'Angelo A,Aieta M,Roviello G

更新日期：2018-12-01 00:00:00

abstract：:Mitoxantrone (Novantrone) and prednimustine (Sterecyt) are both active as single agents in the treatment of unfavorable non-Hodgkin lymphoma (UNHL). The efficacy and toxicity of the combination of these agents (NOSTE) was evaluated in 28 patients with advanced histopathologically proven UNHL who were not eligible for ...

journal_title：Investigational new drugs

authors： Landys KE

更新日期：1988-06-01 00:00:00

abstract：:The matrix metalloproteinases (MMPs) are a family of at least fifteen secreted and membrane-bound zinc-endopeptidases. Collectively, these enzymes can degrade all of the components of the extracellular matrix, including fibrallar and non-fibrallar collagens, fibronectin, laminin and basement membrane glycoproteins. MM...

journal_title：Investigational new drugs

authors： Wojtowicz-Praga SM,Dickson RB,Hawkins MJ

更新日期：1997-01-01 00:00:00

abstract：:A Phase II study of Didemnin-B, a marine cyclic depsipeptide, was undertaken in patients with progressive epithelial ovarian cancer. The starting dose was 2.6 mg/m2. Fifteen patients received the drug, of whom twelve were evaluable. There were no responses observed in the twelve patients. The two most frequent toxicit...

journal_title：Investigational new drugs

authors： Cain JM,Liu PY,Alberts DE,Gallion HH,Laufman L,O'Sullivan J,Weiss G,Bickers JN

更新日期：1992-04-01 00:00:00

abstract：:The aim of this study was to determine the antitumor activity of irofulven when administered in combination with a variety of antimitotic agents. Irofulven in combination with either paclitaxel or docetaxel demonstrated synergistic activity in both the in vitro and in vivo studies. The majority of xenograft bearing an...

journal_title：Investigational new drugs

authors： Kelner MJ,McMorris TC,Rojas RJ,Trani NA,Velasco TR,Estes LA,Suthipinijtham P

更新日期：2002-08-01 00:00:00

abstract：:Objective The aim of the current study was to examine the anticancer activity and the detailed mechanism of novel diisoquinoline derivatives in human gastric cancer cells (AGS). Methods The viability of AGS cells was measured by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. Cell cycle analy...

journal_title：Investigational new drugs

authors： Pawłowska N,Gornowicz A,Bielawska A,Surażyński A,Szymanowska A,Czarnomysy R,Bielawski K

更新日期：2018-12-01 00:00:00

abstract：:This study aimed to analyze the oncology "drug lag" (i.e., the delay in time required for the approval of oncology drugs) in Japan compared with that in the United States of America (US) or the European Union (EU) and to identify the factors associated with this lag. Using publicly available information, we collected ...

journal_title：Investigational new drugs

authors： Yonemori K,Hirakawa A,Ando M,Hirata T,Yunokawa M,Shimizu C,Katsumata N,Tamura K,Fujiwara Y

更新日期：2011-08-01 00:00:00

abstract：:Fluorouracil (5-FU) plus irinotecan combined with bevacizumab has significant activity in metastatic colorectal cancer (mCRC), but S-1 has become a substitute for continuous infusion of 5-FU and has a very low incidence of hand-foot syndrome. With the S-1 plus irinotecan regimen (SIR), the response rate was 62.5%, and...

journal_title：Investigational new drugs

authors： Yamada Y,Yamaguchi T,Matsumoto H,Ichikawa Y,Goto A,Kato K,Hamaguchi T,Shimada Y

更新日期：2012-08-01 00:00:00

abstract：:We previously found that the novel histone deacetylase inhibitor (HDACI) butyroyloxymethyl diethylphosphate (AN-7) had greater selectivity against cutaneous T-cell lymphoma (CTCL) than SAHA. AN-7 synergizes with doxorubicin (Dox), an anthracycline antibiotic that induces DNA breaks. This study aimed to elucidate the m...

journal_title：Investigational new drugs

authors： Moyal L,Goldfeiz N,Gorovitz B,Rephaeli A,Tal E,Tarasenko N,Nudelman A,Ziv Y,Hodak E

更新日期：2018-02-01 00:00:00

abstract：:Twenty-six patients with advanced, measurable epithelial carcinoma of the ovary were treated with 76 courses of esorubicin at doses ranging from 20-30 mg/m2 every 3 weeks. All patients are evaluable for toxicity and response. All patients had received prior therapy including radiation therapy in 9, non-anthracycline c...

journal_title：Investigational new drugs

authors： McGuire WP,Blessing JA,Berman ML

更新日期：1989-11-01 00:00:00

abstract：INTRODUCTION:Multidrug resistance in cancer represents a major problem in chemotherapy. The present study was designed to assess the cytotoxicity of anthraquinones from Pentas schimperi, namely damnacanthal (1), damnacanthol (2), 3-hydroxy-2-hydroxymethyl anthraquinone (3) and schimperiquinone B (4) against nine drug-s...

journal_title：Investigational new drugs

authors： Kuete V,Donfack AR,Mbaveng AT,Zeino M,Tane P,Efferth T

更新日期：2015-08-01 00:00:00

abstract：:Menogarol is a new anthracycline undergoing phase I clinical trial. We report here the lethality after 2 hr exposure to 2 drug combinations of menogarol and several antitumor agents. A new statistical procedure was used to identify synergistic combinations. Most of these combinations were additive, except for menogaro...

journal_title：Investigational new drugs

authors： Bhuyan BK,Adams EG,Johnson M,Crampton SL

更新日期：1985-01-01 00:00:00

abstract：:Hepatocellular carcinoma (HCC) is the most prevalent type of tumor among primary liver tumors and is the second highest cause of cancer-related deaths worldwide. Current therapies are controversial, and more research is needed to identify effective treatments. A new synthetic compound, potassium 5-cyano-4-methyl-6-oxo...

journal_title：Investigational new drugs

authors： da Silva EFG,Lima KG,Krause GC,Haute GV,Pedrazza L,Catarina AV,Gassen RB,de Souza Basso B,Dias HB,Luft C,Garcia MCR,Costa BP,Antunes GL,Basso LA,Donadio MVF,Machado P,de Oliveira JR

更新日期：2020-12-01 00:00:00

abstract：:The effect of the single-chain alkylphospholipid perifosine was analyzed in p53(wild-type) (SKW6.4, OCI and MOLM), p53(mutated) (BJAB, MAVER) and p53(null) (HL-60) leukemic cell lines. Perifosine promoted cytotoxicity with a combination of apoptosis induction in all cell lines and cell cycle block at the G(2)M checkpo...

journal_title：Investigational new drugs

authors： Celeghini C,Voltan R,Rimondi E,Gattei V,Zauli G

更新日期：2011-04-01 00:00:00

abstract：:Although immune checkpoint inhibitors have improved the survival of small cell lung cancer (SCLC) patients, their efficacy in SCLC patients who relapsed after systemic chemotherapy is unclear. This retrospective study aimed to investigate the utility of treatment with atezolizumab plus carboplatin and etoposide in SCL...

journal_title：Investigational new drugs

authors： Ishii H,Azuma K,Kawahara A,Matsuo N,Tokito T,Hoshino T

更新日期：2020-08-11 00:00:00

abstract：:A novel schedule of 5-fluorouracil administration has been developed for biochemical modulation studies. In combination with the pyrimidine synthesis inhibitor PALA, 5-fluorouracil has been given as a 24-hour infusion, repeated weekly: a dose of 2600 mg/m2 is well tolerated. To identify a suitable dose of 5-fluorourac...

journal_title：Investigational new drugs

authors： Haas NB,Hines JB,Hudes GR,Johnston N,Ozols RF,O'Dwyer PJ

更新日期：1993-05-01 00:00:00

abstract：:Survivin is expressed in tumor cells, including acute myeloid leukemia (AML), regulates mitosis, and prevents tumor cell death. The antisense oligonucleotide sodium LY2181308 (LY2181308) inhibits survivin expression and may cause cell cycle arrest and restore apoptosis in AML. In this study, the safety, pharmacokineti...

journal_title：Investigational new drugs

authors： Erba HP,Sayar H,Juckett M,Lahn M,Andre V,Callies S,Schmidt S,Kadam S,Brandt JT,Van Bockstaele D,Andreeff M

更新日期：2013-08-01 00:00:00

abstract：:Background Treatment of recurrent, unresectable granulosa cell tumor (GCT) of the ovary can be challenging. Given the rarity of the tumor, alternative therapies have been difficult to evaluate in large prospective clinical trials. Currently, to our knowledge, there are no reports of the use of immune checkpoint inhibi...

journal_title：Investigational new drugs

authors： How JA,Jazaeri A,Westin SN,Sood AK,Ramondetta LM,Xu M,Abonofal A,Karp DD,Subbiah V,Stephen B,Rodon JA,Yang F,Naing A

更新日期：2021-01-07 00:00:00

abstract：PURPOSE:To compare two different infusion schedules of phenylacetate (PA) in patients with primary brain tumors and to assess the feasibility of the administration in a multi-institutional setting. PATIENTS AND METHODS:Adult patients with recurrent primary brain tumors were treated with PA on two different schedules. ...

journal_title：Investigational new drugs

authors： Chang SM,Kuhn JG,Ian Robins H,Clifford Schold S,Spence AM,Berger MS,Mehta MP,Pollack I,Gilbert M,Prados MD

更新日期：2003-11-01 00:00:00