Novel acridine-based agents with topoisomerase II inhibitor activity suppress mesothelioma cell proliferation and induce apoptosis.

abstract：:PA-U2, an engineered anthrax protective antigen that is activated by urokinase was combined with wildtype lethal factor in the treatment of Colo205 colon adenocarcinoma in vitro and B16-BL6 mouse melanoma in vitro and in vivo. This therapy was also tested in combination with the small molecule paclitaxel, based on pri...

journal_title：Investigational new drugs

authors： Wein AN,Liu S,Zhang Y,McKenzie AT,Leppla SH

更新日期：2013-02-01 00:00:00

abstract：:Studies with CGP 41 251 (I), an N-benzoylstaurosporine derivative and PKC-alpha inhibitor, revealed that oral administration of 400 microg/day of the compound to wild type mice on four successive days reversed multi drug resistance (Killion et al. Oncology Research 7: 453-459, 1995). In our study, the same regimen of ...

journal_title：Investigational new drugs

authors： van Gijn R,van Tellingen O,Haverkate E,Kettenes-van den Bosch JJ,Bult A,Beijnen JH

更新日期：1999-01-01 00:00:00

abstract：:Drug discovery involves various steps and is a long process being even more demanding for complex diseases such as cancer. Tumors are ensembles of subpopulations with different mutations, require very specific and effective strategies. Conventional drug screening technologies may not be adequate and efficient anymore....

journal_title：Investigational new drugs

authors： Kadioglu O,Efferth T

更新日期：2014-12-01 00:00:00

abstract：BACKGROUND:Docetaxel-prednisone (DP) is an approved therapy for metastatic castration-resistant prostate cancer (mCRPC). Orteronel (TAK-700) is an investigational, selective, non-steroidal inhibitor of 17,20-lyase, a key enzyme in androgenic hormone production. This phase 1/2 study evaluated orteronel plus DP in mCRPC ...

journal_title：Investigational new drugs

authors： Petrylak DP,Gandhi JG,Clark WR,Heath E,Lin J,Oh WK,Agus DB,Carthon B,Moran S,Kong N,Suri A,Bargfrede M,Liu G

更新日期：2015-04-01 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：:We have recently developed a liposomal nanoparticle (LNP) formulation of irinotecan based on loading method that involves formation of a complex between copper and the water soluble camptothecin. The loading methodology developed for irinotecan was evaluated to develop a LNP topotecan formulation (referred to herein a...

journal_title：Investigational new drugs

authors： Patankar NA,Waterhouse D,Strutt D,Anantha M,Bally MB

更新日期：2013-02-01 00:00:00

abstract：:A series of 96 diarylamidine (and diarylimidazoline) derivatives were evaluated for their inhibitory effects on the growth and DNA synthesis of murine leukemia L1210 cells. The amidino- and imidazolino-substituted aryl moieties of the compounds consisted of phenyl, indole, indene, benzofuran, benzo[b]thiophene or benz...

journal_title：Investigational new drugs

authors： Balzarini J,de Clercq E,Dann O

更新日期：1983-01-01 00:00:00

abstract：:Chloroquinoxaline sulfonamide (CQS) has been developed to the clinical trial stage based on its activity in the Human Tumor Colony Forming Assay (HTCFA). In the HTCFA, CQS demonstrated inhibition of colony formation against breast, lung, melanoma and ovarian carcinomas. The mechanism of action of CQS is unknown. It do...

journal_title：Investigational new drugs

authors： Fisherman JS,Osborn BL,Chun HG,Plowman J,Smith AC,Christian MC,Zaharko DS,Shoemaker RH

更新日期：1993-02-01 00:00:00

abstract：:Cribrostatin 6 is a quinone-containing natural product that induces the death of cancer cell lines in culture, and its mechanism of action and scope of activity are unknown. Here we show that cribrostatin 6 has broad anticancer activity, potently inducing apoptotic cell death that is not preceded by any defined cell c...

journal_title：Investigational new drugs

authors： Hoyt MT,Palchaudhuri R,Hergenrother PJ

更新日期：2011-08-01 00:00:00

abstract：BACKGROUND:This study investigated the activity of MK-2206, an AKT inhibitor, in metastatic or recurrent nasopharyngeal carcinoma (NPC). METHOD:Oral MK-2206 at a dose of 200 mg was administered on days 1, 8, 15 and 22 of a 28-day cycle until progression. Plasma EBV DNA clearance during the first month of treatment was...

journal_title：Investigational new drugs

authors： Ma BB,Goh BC,Lim WT,Hui EP,Tan EH,Lopes Gde L,Lo KW,Li L,Loong H,Foster NR,Erlichman C,King AD,Kam MK,Leung SF,Chan KC,Chan AT

更新日期：2015-08-01 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：:HDAC inhibitors (HDACI) are now emerging as one of the most promising new classes of drugs for the treatment of select forms of non-Hodgkin's lymphoma (NHL). They are particularly active in T-cell lymphomas, possibly hodgkin's lymphoma and indolent B cell lymphomas. Presently, two of these agents, vorinostat and romid...

journal_title：Investigational new drugs

authors： Zain J,O'Connor OA

更新日期：2010-12-01 00:00:00

abstract：PURPOSE:To summarize the safety experience obtained from phase II clinical trials conducted with trabectedin as single-agent therapy in patients with advanced solid tumors. METHODS:This retrospective analysis includes 1,132 patients exposed to trabectedin in 19 phase II trials carried out between February 1999 and Apr...

journal_title：Investigational new drugs

authors： Le Cesne A,Yovine A,Blay JY,Delaloge S,Maki RG,Misset JL,Frontelo P,Nieto A,Jiao JJ,Demetri GD

更新日期：2012-06-01 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：:Introduction In preclinical data, the combination therapy with S-1 and epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) had a synergistic antitumor effect on non-small cell lung cancer (NSCLC), regardless of the EGFR mutation status. Patients and Methods Patients with previously treated NSCLC an...

journal_title：Investigational new drugs

authors： Nakahara Y,Shimokawa T,Misumi Y,Nogami N,Shinkai T,Seki N,Hosomi Y,Hida N,Okamoto H

更新日期：2020-08-15 00:00:00

abstract：:Background It would be useful to have criteria for predicting long-term treatment responses to immune checkpoint inhibitors (ICIs). Maximum depth of response correlates with treatment outcomes among patients receiving programmed death protein 1 axis inhibitors for non-small cell lung cancer (NSCLC). We investigated as...

journal_title：Investigational new drugs

authors： Kawachi H,Fujimoto D,Morimoto T,Hosoya K,Sato Y,Kogo M,Nagata K,Nakagawa A,Tachikawa R,Tomii K

更新日期：2019-12-01 00:00:00

abstract：:Rolapitant is a neurokinin-1 receptor antagonist that is approved in combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting (CINV) associated with initial and repeat courses of emetogenic cancer chemotherapy, including but not limited to highly emetogenic chemotherapy. Her...

journal_title：Investigational new drugs

authors： Zhang ZY,Wang J,Kansra V,Wang X

更新日期：2019-02-01 00:00:00

abstract：:Seventeen patients with small cell lung cancer entered a phase II trial testing the feasibility of adding high dose epirubicin (100-120 mg/m2, day 1) in combination with etoposide (60-80 mg/m2, days 1-5) and cisplatin (70 mg/m2, day 1) courses repeated every three weeks. Complete responders received thoracic (40 Gy) a...

journal_title：Investigational new drugs

authors： Rosell R,Carles J,Abad A,Jimeno JM,Moreno I,Barnadas A,Ribelles N,Haboubi N

更新日期：1992-07-01 00:00:00

abstract：PURPOSE:To evaluate the response to oral Etoposide when combined with mesna, ifosfamide, and mitoxantrone in patients with relapsed and/or refractory lymphoma. To evaluate response and its duration after administration of intravenous Etoposide, methylprednisolone, high-dose cytosine arabinoside, and cisplatin (ESHAP) a...

journal_title：Investigational new drugs

authors： Romaguera JE,Rodriguez MA,Hagemeister FB,McLaughlin P,Swan F,Moore DF Jr,Sarris AH,Younes A,Hill D,Cabanillas F

更新日期：1994-01-01 00:00:00

abstract：PURPOSE:Vincristine sulfate liposomes injection (VSLI, Marqibo®) is an FDA approved encapsulated preparation of standard vincristine in sphingomyelin/cholesterol liposomes. Clinical pharmacokinetics show VSLI to be a long-circulating, slow release formulation that is confined to plasma, and prior data on cerebrospinal ...

journal_title：Investigational new drugs

authors： Shah NN,Cole DE,Lester-McCully CM,Wayne AS,Warren KE,Widemann BC

更新日期：2016-02-01 00:00:00

abstract：:Artemisinin and its derivatives are well known antimalarial drugs, particularly useful after resistance to traditional antimalarial pharmaceuticals has started to occur in Plasmodium falciparum. In recent years, anticancer activity of artemisinin has been reported both in vitro and in vivo. Artemisinin has inhibitory ...

journal_title：Investigational new drugs

authors： Buommino E,Baroni A,Canozo N,Petrazzuolo M,Nicoletti R,Vozza A,Tufano MA

更新日期：2009-10-01 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：BACKGROUND:This phase I, dose-finding study evaluated the maximum tolerated dose (MTD), safety, pharmacokinetics, and antitumor activity of sunitinib plus S-1/cisplatin in Japanese patients with advanced/metastatic gastric cancer. PATIENTS AND METHODS:Patients received oral sunitinib on a continuous daily dosing (CDD)...

journal_title：Investigational new drugs

authors： Boku N,Muro K,Machida N,Hashigaki S,Kimura N,Suzuki M,Lechuga M,Miyata Y

更新日期：2014-04-01 00:00:00

abstract：BACKGROUND:The primary objective of this Phase I study was to determine the maximum tolerated dose (MTD) and recommended phase II dose for Tomudex and Doxorubicin when given in combination to patients with advanced metastatic cancer. The secondary objective was to assess the toxicity profile. PATIENTS AND METHODS:Star...

journal_title：Investigational new drugs

authors： Bjarnason GA,Charpentier D,Wong R,Goel R,Douglas L,Walsh W,Matthews S,Dent S,Seymour L,Winquist E

更新日期：2005-01-01 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：:Background The hexapeptide 4A6 (Ac-Thr(tBu)-His(Bzl)-Thr(Bzl)-Nle-Glu(OtBu)-Gly-Bza) was isolated from a peptide library constructed to identify peptide-based transport inhibitors of multidrug resistance (MDR) efflux pumps including P-glycoprotein and Multidrug Resistance-associated Protein 1. 4A6 proved to be a subst...

journal_title：Investigational new drugs

authors： Oerlemans R,Berkers CR,Assaraf YG,Scheffer GL,Peters GJ,Verbrugge SE,Cloos J,Slootstra J,Meloen RH,Shoemaker RH,Dijkmans BAC,Scheper RJ,Ovaa H,Jansen G

更新日期：2018-10-01 00:00:00

abstract：:3-Deazaguanine (Dezaguanine), a purine antimetabolite, was evaluated in a phase I trial in 42 patients with advanced solid tumors. Dezaguanine was given as a weekly intravenous infusion for three consecutive weeks of a four-week cycle. The dose ranged from 30 to 2000 mg/m2; no consistent dose-limiting hematologic or g...

journal_title：Investigational new drugs

authors： Margolin K,Doroshow J,Leong L,Akman S,Carr B,Odujinrin O,Flanagan B,Grove W,DeLap R,Goldberg D

更新日期：1990-11-01 00:00:00

abstract：:Up to 30% of patients with advanced germ cell tumors will fail induction chemotherapy or will relapse. New agents with activity in this still potentially curable subgroup of patients are needed. Edatrexate (10-ethyl, 10-deaza-aminopterin) is a methotrexate analogue that has preclinical and clinical activity in breast,...

journal_title：Investigational new drugs

authors： Meyers FJ,Lew D,Lara PN Jr,Williamson S,Marshall E,Balcerzak SP,Rivkin SE,Samlowski W,Crawford ED

更新日期：1998-01-01 00:00:00

abstract：:AZQ was given intravenously to 23 patients with mixed mesodermal sarcoma of the uterus refractory to conventional treatment at a dose of 22.5-30 mg/m2 q three weeks. There was one partial response lasting seven weeks and one drug-related death. Based upon the activity observed in this trial, there does not appear to b...

journal_title：Investigational new drugs

authors： Slayton RE,Blessing JA,Clarke-Pearson D

更新日期：1991-02-01 00:00:00

abstract：:Coptis chinensis Franch. has been extensively used in traditional Chinese medicine. The chemical structure of oxyepiberberine, as an alkaloid isolated from Coptis chinensis Franch., has been previously studied. However, anti-cancer effects and underlying mechanisms of oxyepiberberine need to be explored. This study ai...

journal_title：Investigational new drugs

authors： Ning H,Lu W,Jia Q,Wang J,Yao T,Lv S,Li Y,Wen H

更新日期：2020-09-30 00:00:00