Developmental antiangiogenic agents for the treatment of non-small cell lung cancer (NSCLC).

abstract：:The poor prognosis of children with high-grade glioma (HGG) and high-risk neuroblastoma, despite multidisciplinary therapeutic approaches, demands new treatments for these indications. F14512 is a topoisomerase II inhibitor containing a spermine moiety that facilitates selective uptake by tumor cells via the Polyamine...

journal_title：Investigational new drugs

authors： Leblond P,Boulet E,Bal-Mahieu C,Pillon A,Kruczynski A,Guilbaud N,Bailly C,Sarrazin T,Lartigau E,Lansiaux A,Meignan S

更新日期：2014-10-01 00:00:00

abstract：:Therapies which target VEGF and mTOR are now available for patients with metastatic renal cell carcinoma, but there is a continued need to develop agents for patients who become refractory to these initial agents. Tandutinib is a relatively selective inhibitor of type III tyrosine kinase receptor kinases with promisin...

journal_title：Investigational new drugs

authors： Shepard DR,Cooney MM,Elson P,Bukowski RM,Dreicer R,Rini BI,Garcia JA

更新日期：2012-02-01 00:00:00

abstract：INTRODUCTION:Heat shock protein 90 (Hsp90) has been studied as a therapeutic target in many cancers. In preclinical trials, the Hsp90 ATPase inhibitor ganetespib demonstrated potent inhibition of solid tumor growth, with superior potency than prior Hsp90 inhibitors. Given the promising preclinical outcome and favorable...

journal_title：Investigational new drugs

authors： Thakur MK,Heilbrun LK,Sheng S,Stein M,Liu G,Antonarakis ES,Vaishampayan U,Dzinic SH,Li X,Freeman S,Smith D,Heath EI

更新日期：2016-02-01 00:00:00

abstract：:The novel compound N-benzoxazol-2-yl-N'-1-(isoquinolin-3-yl-ethylidene)-hydrazine (EPH136) has been shown to exhibit antitumor activity in vitro and in vivo. A COMPARE analysis showed that the patterns of cellular effects of EPH136 are not related to any of 175 standard antitumor agents with a known mechanism of actio...

journal_title：Investigational new drugs

authors： Hofmann J,Easmon J,Puerstinger G,Heinisch G,Jenny M,Shtil AA,Hermann M,Condorelli DF,Sciré S,Musumarra G

更新日期：2009-06-01 00:00:00

abstract：:This dose-escalating phase I clinical trial was designed to determine the recommended dose (RD) and to assess the safety and feasibility of weekly plitidepsin (1-hour i.v. infusion, Days 1, 8 and 15) combined with carboplatin (1-hour i.v. infusion, Day 1, after plitidepsin) in 4-week (q4wk) cycles given to patients wi...

journal_title：Investigational new drugs

authors： Salazar R,Plummer R,Oaknin A,Robinson A,Pardo B,Soto-Matos A,Yovine A,Szyldergemajn S,Calvert AH

更新日期：2011-12-01 00:00:00

abstract：:The Eastern Cooperative Oncology Group undertook a limited institution phase II study of PCNU in advanced, metastatic breast cancer. The study was limited to patients treated with 1 to 2 prior chemotherapy regimens. Accrual goals were 30 patients but the study was terminated after 10 patients had no response, with a r...

journal_title：Investigational new drugs

authors： Rubins JM,Taylor SG 4th

更新日期：1989-07-01 00:00:00

abstract：:An inflammatory myofibroblastic tumor (IMT) is a rare mesenchymal neoplasm that typically develops in the lungs and seldom in the head and neck region. It is often related to the anaplastic lymphoma kinase (ALK) fusion gene. Crizotinib, a first-generation ALK inhibitor, has been shown to have a notable response in pat...

journal_title：Investigational new drugs

authors： Honda K,Kadowaki S,Kato K,Hanai N,Hasegawa Y,Yatabe Y,Muro K

更新日期：2019-08-01 00:00:00

abstract：:Imidazolium-trans-dimethylsulfoxideimidazoletetrachlororuthenate (NAMI-A) is a ruthenium compound effective on solid tumor metastases. In this study, we evaluated the effects of different routes of administration of NAMI-A on the distribution to primary tumor, lungs and kidneys in BD2F1 hybrids with Lewis lung carcino...

journal_title：Investigational new drugs

authors： Cocchietto M,Zorzet S,Sorc A,Sava G

更新日期：2003-02-01 00:00:00

abstract：:Pre-clinical and clinical studies have shown that trifluoperazine (TFP) can modulate multidrug resistance. We have performed a Phase II trial of TFP and doxorubicin in doxorubicin-naive patients with metastatic breast cancer. We hypothesized that TFP would inhibit the development of doxorubicin resistance, resulting i...

journal_title：Investigational new drugs

authors： Budd GT,Bukowski RM,Lichtin A,Bauer L,Van Kirk P,Ganapathi R

更新日期：1993-02-01 00:00:00

abstract：:Fourteen patients with active chronic lymphocytic leukemia who had failed prior therapy were treated with progressive doses of weekly intravenous colchicine beginning at 2 mg and escalating as high as 7 mg in a single injection. Responses were seen in two of 14, with a lessening of adenopathy and splenomegaly. Toxicit...

journal_title：Investigational new drugs

authors： Weick JK,Livingston RB,Van Slyck EJ

更新日期：1983-01-01 00:00:00

abstract：:Ergot alkaloids are psychoactive and vasoconstricting agents of the fungus Claviceps purpurea causing poisoning such as ergotism in medieval times (St. Anthony's Fire). This class of substances also inhibits tumor growth in vitro and in vivo, though the underlying mechanisms are unclear as yet. We investigated six erg...

journal_title：Investigational new drugs

authors： Mrusek M,Seo EJ,Greten HJ,Simon M,Efferth T

更新日期：2015-02-01 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：:The study investigated possible mechanisms by which second-generation taxanes, established as significantly more effective than paclitaxel in vitro, suppress a rat lymphoma model in vivo. The studied mechanisms included taxane pharmacokinetics, expression of genes dominating their metabolism (Cyp3a1/2) and transport (...

journal_title：Investigational new drugs

authors： Otová B,Ojima I,Václavíková R,Hrdý J,Ehrlichová M,Souček P,Vobořilová J,Němcová V,Zanardi I,Horský S,Kovář J,Gut I

更新日期：2012-06-01 00:00:00

abstract：BACKGROUND:Although bevacizumab plus FOLFOX is a standard treatment for metastatic colorectal cancer, oxaliplatin must be withdrawn in many patients because of cumulative neurotoxicity. We postulated that a reduced dose of oxaliplatin and modified treatment schedule would prolong the time to treatment failure and evalu...

journal_title：Investigational new drugs

authors： Nakayama N,Sato A,Tanaka S,Shimada K,Konishi K,Sasaki E,Hibi K,Ichikawa H,Kikuchi Y,Sakuyama T,Sekikawa T,Hayashi K,Nishina H,Tokyo Cooperative Oncology Group, Tokyo, Japan.

更新日期：2015-08-01 00:00:00

abstract：:Background High-risk neuroblastoma has poor outcomes with high rates of relapse despite aggressive treatment, and novel therapies are needed to improve these outcomes. Ponatinib is a multi-tyrosine kinase inhibitor that targets many pathways implicated in neuroblastoma pathogenesis. We hypothesized that ponatinib woul...

journal_title：Investigational new drugs

authors： Whittle SB,Patel K,Zhang L,Woodfield SE,Du M,Smith V,Zage PE

更新日期：2016-12-01 00:00:00

abstract：:In this study, 30 evaluable patients with advanced carcinoma of the breast were treated with cyclophosphamide 600 mg/m2 i.v. followed one day later with mitoxantrone (Novantrone; dihydroxyanthracenedione) 16 mg/m2 i.v. Drug treatment was repeated every 3-4 weeks, for a maximum of 12 cycles. The overall response rate w...

journal_title：Investigational new drugs

authors： Periti P,della Cuna GR,Pannuti F,Mazzei T,Preti P,Martoni A,Mini E

更新日期：1985-01-01 00:00:00

abstract：PURPOSE:Epidermal growth factor receptor (EGFR) inhibition may overcome chemotherapy resistance by inhibiting important anti-apoptotic signals that are constitutively activated by an overstimulated EGFR pathway. METHODS:This phase I dose escalation trial assessed the safety and efficacy of vinflunine, a novel vinca al...

journal_title：Investigational new drugs

authors： Sanoff HK,Davies JM,Walko C,Irvin W,Buie L,Keller K,Ivanova A,Chiu WK,O'Neil BH,Stinchcombe TE,Dees EC

更新日期：2011-10-01 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：:CC-1065 is a unique alkylating agent that preferentially binds in the minor groove of double-stranded DNA at adenine-thymine-rich sites. Although it has broad antitumor activity in preclinical models its development was discontinued because of deaths observed during preclinical toxicology studies. Adozelesin is a pote...

journal_title：Investigational new drugs

authors： Foster BJ,LoRusso PM,Poplin E,Zalupski M,Valdivieso M,Wozniak A,Flaherty L,Kasunic DA,Earhart RH,Baker LH

更新日期：1996-01-01 00:00:00

abstract：:Receptor tyrosine kinases (RTKs) modulate a variety of cellular events, including cell proliferation, differentiation, mobility and apoptosis. In addition, RTKs have been validated as targets for cancer therapies. Microtubules are another class of proven targets for many clinical anticancer drugs. Here, we report that...

journal_title：Investigational new drugs

authors： Zhang J,Zhou J,Ren X,Diao Y,Li H,Jiang H,Ding K,Pei D

更新日期：2012-04-01 00:00:00

abstract：:LY2457546 is a potent and orally bioavailable inhibitor of multiple receptor tyrosine kinases involved in angiogenic and tumorigenic signalling. In biochemical and cellular assays, LY2457546 demonstrates potent activity against targets that include VEGFR2 (KDR), PDGFRβ, FLT-3, Tie-2 and members of the Eph family of re...

journal_title：Investigational new drugs

authors： Burkholder TP,Clayton JR,Rempala ME,Henry JR,Knobeloch JM,Mendel D,McLean JA,Hao Y,Barda DA,Considine EL,Uhlik MT,Chen Y,Ma L,Bloem LJ,Akunda JK,McCann DJ,Sanchez-Felix M,Clawson DK,Lahn MM,Starling JJ

更新日期：2012-06-01 00:00:00

abstract：:Background This first-in-human phase 1 study assessed the safety of TAS-114, a novel deoxyuridine triphosphatase inhibitor, combined with S-1 to determine its maximum tolerated dose (MTD) and recommended dose (RD). Methods In this dose-escalation study with a 3 + 3 design, TAS-114 and S-1 were concurrently administere...

journal_title：Investigational new drugs

authors： Doi T,Yoh K,Shitara K,Takahashi H,Ueno M,Kobayashi S,Morimoto M,Okusaka T,Ueno H,Morizane C,Okano N,Nagashima F,Furuse J

更新日期：2019-06-01 00:00:00

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：: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：:The modulation of intracellular nuclear factor-kappaB (NF-κB) signaling pathway involved in the deregulated expression of cell proliferation and cell cycle regulatory molecules is a pragmatic approach for chemoprevention. Eugenol (4-allyl-1-hydroxy-2-methoxybenzene), a natural phenolic constituent of oils of cloves is...

journal_title：Investigational new drugs

authors： Manikandan P,Vinothini G,Vidya Priyadarsini R,Prathiba D,Nagini S

更新日期：2011-02-01 00:00:00

abstract：:Didemnin B is a depsipeptide derived from a Caribbean tunicate (sea squirt) that has demonstrated antineoplastic activity against a variety of murine tumor models, including the L1210 and P388 leukemia, the B16 melanoma, and M5076 sarcoma cell lines. Based on these data, we designed a phase II trial in which 15 patien...

journal_title：Investigational new drugs

authors： Jones DV Jr,Ajani JA,Blackburn R,Daugherty K,Levin B,Patt YZ,Abbruzzese JL

更新日期：1992-08-01 00:00:00

abstract：:Background To determine the recommended dose (RD) of a combination of PM01183 and gemcitabine in patients with advanced solid tumors. Methods Forty-five patients received escalating doses of PM01183/gemcitabine on Days 1 and 8 every 3 weeks (d1,8 q3wk) following a standard 3 + 3 design. Results PM01183 3.5 mg flat dos...

journal_title：Investigational new drugs

authors： Paz-Ares L,Forster M,Boni V,Szyldergemajn S,Corral J,Turnbull S,Cubillo A,Teruel CF,Calderero IL,Siguero M,Bohan P,Calvo E

更新日期：2017-04-01 00:00:00

abstract：:The current recommendations for Phase I trials should allow more confident interpretation of the toxicity and efficacy of new agents by providing a framework for multicentre and international co-operation. An overview of the aims and designs of Phase I trials is presented, along with a summary of current and recently ...

journal_title：Investigational new drugs

authors： Estlin EJ,Ablett S,Newell DR,Lewis IJ,Lashford L,Pearson AD

更新日期：1996-01-01 00:00:00

abstract：:In an on-going Phase II evaluation, dianhydrogalactitol (NSC 132313) was administered intravenously to 28 patients with advanced or recurrent non-squamous cell carcinoma of the cervix. The initial dosage was 60 mg/m2/wk with escalation to 75 mg/m2/wk if there were no adverse effects. Twenty-seven patients were evaluab...

journal_title：Investigational new drugs

authors： Stehman FB,Blessing JA,Homesley HD,Currie JL,Yordan EL

更新日期：1984-01-01 00:00:00

abstract：:Fifteen patients with advanced, cisplatin-refractory germ cell tumors (GCT) were treated with iproplatin (CHIP). No objective responses were noted in any of the patients treated. By restricting the entry criteria to heavily pre-treated patients, the identification of new active agents in phase II trials may be hindere...

journal_title：Investigational new drugs

authors： Murphy BA,Motzer RJ,Bosl GJ

更新日期：1992-11-01 00:00:00