Phase II trial of didemnin-B in advanced epithelial ovarian cancer. A Southwest Oncology Group study.

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：:Withaferin A (WA), a steroidal lactone derived from the plant Vassobia breviflora, has been reported to have anti-proliferative, pro-apoptotic, and anti-angiogenic properties against cancer growth. In this study, we identified several key underlying mechanisms of anticancer action of WA in glioblastoma cells. WA was f...

journal_title：Investigational new drugs

authors： Grogan PT,Sleder KD,Samadi AK,Zhang H,Timmermann BN,Cohen MS

更新日期：2013-06-01 00:00:00

abstract：BACKGROUND:Relatively few studies have examined the activity of alkylating agents in the treatment of advanced colorectal adenocarcinoma. Recent reports have suggested possible therapeutic activity for high-dose intravenous melphalan administered with autologous bone marrow transplantation (BMT) support. We conducted a...

journal_title：Investigational new drugs

authors： Moore DF Jr,Pazdur R,Abbruzzese JL

更新日期：1994-01-01 00:00:00

abstract：BACKGROUND:Gemcitabine is a pro-drug that has to be phosphorylated to gemcitabine-triphosphate in order to exhibit its antineoplastic activity. This reaction involves the enzyme deoxycytidine kinase which is saturated at plasma concentrations following standard 30-min infusions. Pharmacological studies indicate that pr...

journal_title：Investigational new drugs

authors： Schmid P,Schweigert M,Beinert T,Flath B,Sezer O,Possinger K

更新日期：2005-03-01 00:00:00

abstract：:Ninety per cent of pancreatic adenocarcinomas (PC) contain mutations of the K-Ras proto-oncogene resulting in constitutively activated Ras protein. A critical step in Ras activation is farnesylation of Ras protein. Farnesyl transferase inhibitors are compounds that inhibit farnesylation. We report the results of a pha...

journal_title：Investigational new drugs

authors： Macdonald JS,McCoy S,Whitehead RP,Iqbal S,Wade JL 3rd,Giguere JK,Abbruzzese JL

更新日期：2005-10-01 00:00:00

abstract：INTRODUCTION:This multicenter, open-label, phase II study was carried out to compare the efficacy and safety of cilengitide (EMD 121974), a selective inhibitor of the cell-surface integrins αVβ3 and αVβ5, with that of docetaxel in patients with advanced non-small-cell lung cancer (NSCLC). METHODS:Patients (n = 140) wi...

journal_title：Investigational new drugs

authors： Manegold C,Vansteenkiste J,Cardenal F,Schuette W,Woll PJ,Ulsperger E,Kerber A,Eckmayr J,von Pawel J

更新日期：2013-02-01 00:00:00

abstract：:SHetA2 is a small molecule flexible heteroarotinoid (Flex-Het) with promising cancer prevention and therapeutic activity. Extensive preclinical testing documented lack of SHetA2 toxicity at doses 25 to 150 fold above effective doses. Knowledge of the SHetA2 molecular target(s) that mediate(s) the mechanism of SHetA2 a...

journal_title：Investigational new drugs

authors： Benbrook DM,Nammalwar B,Long A,Matsumoto H,Singh A,Bunce RA,Berlin KD

更新日期：2014-06-01 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：: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：:Idarubicin (DMDR), a new analogue of daunorubicin, was administered orally once every 3 weeks at the dose of 40 to 45 mg/m2 to 20 evaluable patients with non-Hodgkin's lymphomas (NHL). Eighty-six percent of patients with favorable histology and 54% with unfavorable histology (intermediate and high grade as IWF) achiev...

journal_title：Investigational new drugs

authors： Lopez M,Di Lauro L,Papaldo P

更新日期：1986-01-01 00:00:00

abstract：:We investigated proliferation and apoptosis induction in Jurkat T-leukemia cells by the new isothiocyanate 4-(methylthio)butylisothiocyanate (MTBITC). To help elucidate whether the effects of MTBITC are specific for cancer cells, we tested MTBITC on freshly isolated, non-transformed human peripheral T lymphocytes. The...

journal_title：Investigational new drugs

authors： Fimognari C,Nüsse M,Iori R,Cantelli-Forti G,Hrelia P

更新日期：2004-04-01 00:00:00

abstract：:Indibulin is a synthetic small molecule which antitumor activity is based upon destabilization of microtubules. The primary study objectives were to determine the impact of fasted and fed condition on pharmacokinetic parameters, as well as the maximum tolerated dose of the oral drinking solution of indibulin administe...

journal_title：Investigational new drugs

authors： Kuppens IE,Witteveen PO,Schot M,Schuessler VM,Daehling A,Beijnen JH,Voest EE,Schellens JH

更新日期：2007-06-01 00:00:00

abstract：:An inflammatory myofibroblastic tumor (IMT) is a rare invasive soft tissue mass with intramuscular penetration that is primarily treated via a surgical procedure. However, with unclear boundaries and a high rate of relapse, there is no standard treatment for recurrence or unresectable tumors. It is noteworthy that app...

journal_title：Investigational new drugs

authors： Liu W,Duan Q,Gong L,Yang Y,Huang Z,Guo H,Niu X

更新日期：2020-09-11 00:00:00

abstract：:Antiproliferative factor (APF) is a potent frizzled protein 8-related sialoglycopeptide inhibitor of bladder epithelial cell proliferation that mediates its activity by binding to cytoskeletal associated protein 4 in the cell membrane. Synthetic asialylated APF (as-APF) (Galβ1-3GalNAcα-O-TVPAAVVVA) was previously show...

journal_title：Investigational new drugs

authors： Koch KR,Zhang CO,Kaczmarek P,Barchi J Jr,Guo L,Shahjee HM,Keay S

更新日期：2012-10-01 00:00:00

abstract：:SJG-136 is a synthetic pyrrolobenzodiazepine (PBD) dimer in which two DNA-alkylating subunits are linked through an inert propanedioxy tether. Biophysical and biochemical studies of SJG-136 have shown a remarkable affinity for DNA and potent cytotoxicity in vitro. On this basis, together with its unique sequence selec...

journal_title：Investigational new drugs

authors： Wilkinson GP,Taylor JP,Shnyder S,Cooper P,Howard PW,Thurston DE,Jenkins TC,Loadman PM

更新日期：2004-08-01 00:00:00

abstract：BACKGROUND:This Phase-I-study aimed to determine the recommended Phase-II-dosing-schedule of LY2334737, an oral gemcitabine prodrug, in patients with advanced/metastatic solid tumors. Pharmacokinetics, cytokeratin-18 (CK18) levels, genetic polymorphisms, and antitumor activity were additionally evaluated. METHODS:Pati...

journal_title：Investigational new drugs

authors： Faivre SJ,Olszanski AJ,Weigang-Köhler K,Riess H,Cohen RB,Wang X,Myrand SP,Wickremsinhe ER,Horn CL,Ouyang H,Callies S,Benhadji KA,Raymond E

更新日期：2015-12-01 00:00:00

abstract：:Background AR-67 is a novel camptothecin analogue at early stages of drug development. The phase 1 clinical trial in cancer patients with solid tumors was completed and a population pharmacokinetic model (POP PK) was developed to facilitate further development of this investigational agent. Methods Pharmacokinetic dat...

journal_title：Investigational new drugs

authors： Tang F,Tsakalozou E,Arnold SM,Ng CM,Leggas M

更新日期：2019-12-01 00:00:00

abstract：:Certain toxic effects of cytotoxic anticancer agents typically evolve over weeks. When such agents are administered weekly, these effects are cumulative. With such schedules, good medical practice mandates dose modifications with mild or moderate toxicity in order to avoid progression to serious or life-threatening to...

journal_title：Investigational new drugs

authors： McClish DK,Roberts JD

更新日期：2003-08-01 00:00:00

abstract：:Sixteen patients with stage IV melanoma, who were heavily pretreated, received 11 mg/m2/day of intravenous Irofulven for five consecutive days every 28 days. There were no objective tumor responses, although one patient exhibited stable disease after 4 cycles. The most common toxicities were grade 1/2 nausea, vomiting...

journal_title：Investigational new drugs

authors： Pierson AS,Gibbs P,Richards J,Russ P,Eckhardt SG,Gonzalez R

更新日期：2002-08-01 00:00:00

abstract：:In a previous study we reported on the synthesis of 1,4-naphthoquinone-sulfides by thiolation of 1,4-naphthohydroquinones with primary aryl and alkyl thiols using laccase as catalyst. These compounds were synthesized as Vitamin K3 analogues. Vitamin K3 (VK3; 2-methyl-1,4-naphthoquinone; menadione) is known to have pot...

journal_title：Investigational new drugs

authors： Wellington KW,Hlatshwayo V,Kolesnikova NI,Saha ST,Kaur M,Motadi LR

更新日期：2020-04-01 00:00:00

abstract：:Tyrosine kinase inhibitors (TKI) or monoclonal antibodies targeting EGFR, HER2 or VEGFR receptors have demonstrated substantial clinical benefit in patients with advanced breast cancer, colon cancer, head and neck cancer, non-small cell lung cancer, and renal cell carcinoma. Nevertheless, these drugs have some target ...

journal_title：Investigational new drugs

authors： Bahleda R,Massard C,Soria JC,Izzedine H,Cohen A,Ederhy S

更新日期：2010-06-01 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：:Ninhydrin (2,2-dihydroxy-1,3-indane dione) was evaluated for its antitumor and cytotoxic properties in Ehrlich ascites carcinoma cell (EAC Cell)-bearing mice. The rationale behind this study has been mainly the literature reports of its characteristic interference with DNA synthesis and calcium homeostasis. Antitumor ...

journal_title：Investigational new drugs

authors： Qureshi S,Al-Shabanah OA,Al-Bekairi AM,Al-Harbi MM,Al-Gharably NM,Raza M

更新日期：2000-08-01 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：:Background To determine the feasibility and efficacy of olanzapine, which is approved by the Pharmaceuticals and Medical Devices Agency as multi acting receptor targeted antipsychotic agent of the thienobenzodiazepine class, for prevention of chemotherapy-induced nausea and vomiting (CINV) in patients undergoing conti...

journal_title：Investigational new drugs

authors： Bun S,Yonemori K,Akagi T,Noguchi E,Shimoi T,Shimomura A,Yunokawa M,Shimizu C,Fujiwara Y,Makino Y,Hayashi Y,Tamura K

更新日期：2018-02-01 00:00:00

abstract：:4-demethoxydaunorubicin (4-dm DNR), a new analog of daunorubicin, was tested at an every 3-week dose schedule in 63 evaluable patients with various forms of disseminated malignancy. Utilizing the intravenous (i.v.) route of administration, the maximum tolerated dose (MTD) was 15-18 mg/m2; with the oral route the MTD w...

journal_title：Investigational new drugs

authors： Bonfante V,Ferrari L,Villani F,Bonadonna G

更新日期：1983-01-01 00:00:00

abstract：PURPOSE:This phase I study aims at assessing the safety and tolerability of LY2603618, a selective inhibitor of Checkpoint Kinase 1, in combination with pemetrexed and determining the maximum tolerable dose and the pharmacokinetic parameters. EXPERIMENTAL DESIGN:This was an open-label, multicenter, dose-escalation stu...

journal_title：Investigational new drugs

authors： Weiss GJ,Donehower RC,Iyengar T,Ramanathan RK,Lewandowski K,Westin E,Hurt K,Hynes SM,Anthony SP,McKane S

更新日期：2013-02-01 00:00:00

abstract：:Radioactive iodine-refractory [(18)F] fluorodeoxy-glucose-positron emission tomography-positive thyroid carcinomas represent especially aggressive tumors. Targeting glucose metabolism by the transketolase isoenzyme transketolase like 1 (TKTL-1) which is over-expressed in various neoplasms, may be effective. The correl...

journal_title：Investigational new drugs

authors： Fröhlich E,Fink I,Wahl R

更新日期：2009-08-01 00:00:00

abstract：:We performed a single-institution phase II study to evaluate the efficacy and toxicities of vinorelbine monotherapy in patients previously treated with anthracyclines and taxanes. Vinorelbine was administered at a dose level of 25 mg/m² intravenously on days 1, 8, 15 and 22, every four weeks, and responses were assess...

journal_title：Investigational new drugs

authors： Seo HY,Lee HJ,Woo OH,Park KH,Woo SU,Yang DS,Kim AR,Lee JB,Lee ES,Kim YH,Kim JS,Seo JH

更新日期：2011-04-01 00:00:00

abstract：:Fifteen patients with recurrent and/or metastatic squamous cell carcinoma of the head and neck received a 5 day continuous I.V. infusion of 6-thioguanine repeated every five weeks. Dose limiting toxicity was primarily hematological with grade III/IV leucopenia and thrombocytopenia seen in seven patients. Nausea and vo...

journal_title：Investigational new drugs

authors： Kruter F,Eisenberger M,Sinibaldi V,Engstrom C,Jacobs M,Abrams J,Belani C,Gray W,Krasnow S

更新日期：1992-07-01 00:00:00