Cytotoxic flavonoids and isoflavonoids from Erythrina sigmoidea towards multi-factorial drug resistant cancer cells.

abstract：:Hexamethylenebisacetamide (HMBA), an in vitro differentiating agent, was studied for its pharmacodynamic actions in animals. Plasma stability, organ distribution, excretion, oral bioavailability, and estimates of pharmacokinetic parameters and acute lethality were determined in rats. The single dose intraperitoneal LD...

journal_title：Investigational new drugs

authors： Litterst CL,Roth JS,Kelley JA

更新日期：1985-01-01 00:00:00

abstract：BACKGROUND:Alterations in retinoid signaling appear to be involved in the pathogenesis of small cell lung cancer (SCLC). Fenretinide [N-(4-hydroxyphenyl)retinamide], a synthetic retinoid, inhibits the growth of SCLC cells in vitro via the induction of apoptosis. Since these data suggested that SCLC is the adult solid t...

journal_title：Investigational new drugs

authors： Schneider BJ,Worden FP,Gadgeel SM,Parchment RE,Hodges CM,Zwiebel J,Dunn RL,Wozniak AJ,Kraut MJ,Kalemkerian GP

更新日期：2009-12-01 00:00:00

abstract：:Twenty-four patients with acute leukemia or blast crisis (BC) of chronic myelocytic leukemia (CML) in relapse or refractory to standard chemotherapy, were eligible for treatment with mitoxantrone. Mitoxantrone (Novantrone; dihydroxyanthracenedione) was administered in a dose of 8-13 mg/m2 on five consecutive days. Fiv...

journal_title：Investigational new drugs

authors： Meyer P,Ho AD,Ehninger G,Mjaaland I,Heidemann E,Seither E

更新日期：1985-01-01 00:00:00

abstract：PURPOSE:Hepatobiliary cancers respond poorly to cytotoxic chemotherapy. We evaluated the activity and safety of ixabepilone, an epothilone B analogue which stabilizes microtubules, in a phase II trial in patients with advanced cancers of the gallbladder, bile duct, and liver. METHODS:Eligible patients had previously-u...

journal_title：Investigational new drugs

authors： Nimeiri HS,Singh DA,Kasza K,Taber DA,Ansari RH,Vokes EE,Kindler HL

更新日期：2010-12-01 00:00:00

abstract：OBJECTIVE:The anti-vascular endothelial growth factor (VEGF) antibody bevacizumab has received considerable attention as a first-line treatment of advanced colorectal cancers. Difficulties associated with effectively monitoring the activity of this drug have prompted us to seek a pharmacodynamic marker suitable for def...

journal_title：Investigational new drugs

authors： Shin SJ,Hwang JW,Ahn JB,Rha SY,Roh JK,Chung HC

更新日期：2013-02-01 00:00:00

abstract：:The neurotransmitter serotonin is involved in numerous bodily functions via seven different serotonin receptor subfamilies. Serotonin plays a role in gastrointestinal functions like intestinal secretion or peristalsis and neuropsychiatric events like depression or migraine. One of these subtypes has been found on glio...

journal_title：Investigational new drugs

authors： Sturzu A,Sheikh S,Klose U,Echner H,Kalbacher H,Deeg M,Nägele T,Horger M,Ernemann U,Heckl S

更新日期：2012-12-01 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：:Antiprogestins have been largely utilized in reproductive medicine, yet their repositioning for oncologic use is rapidly emerging. In this study we investigated the molecular mediators of the anti-ovarian cancer activity of the structurally related antiprogestins RU-38486, ORG-31710 and CDB-2914. We studied the respon...

journal_title：Investigational new drugs

authors： Goyeneche AA,Seidel EE,Telleria CM

更新日期：2012-06-01 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：:Herein we describe a series of multifunctional 5-aminolevulinic-acid (ALA) prodrugs for photodynamic dependent and independent cancer therapy (PDT). We studied the cell-death mechanisms in glioblastoma U251 cells treated with four ALA-prodrugs: (1) AlaAcBu, that releases ALA, acetaldehyde, and butyric acid; (2) AlaFaB...

journal_title：Investigational new drugs

authors： Berkovitch-Luria G,Weitman M,Nudelman A,Rephaeli A,Malik Z

更新日期：2012-06-01 00:00:00

abstract：:We explored whether barasertib (AZD1152), a selective Aurora B kinase inhibitor, is a substrate for P-glycoprotein (Pgp, MDR1), breast cancer resistance protein (BCRP), and multidrug resistance protein 2 (MRP2) in vitro. Cell survival, drug transport, and competition experiments with barasertib pro-drug and the more a...

journal_title：Investigational new drugs

authors： Marchetti S,Pluim D,van Eijndhoven M,van Tellingen O,Mazzanti R,Beijnen JH,Schellens JH

更新日期：2013-10-01 00:00:00

abstract：BACKGROUND AND RATIONALE:Bortezomib (PS-341, VELCADE®) is a selective inhibitor of the 26S proteasome, an integral component of the ubiquitin-proteasome pathway. This phase II study evaluated the activity and tolerability of bortezomib in unresectable hepatocellular carcinoma (HCC) patients. METHODS:The primary endpoi...

journal_title：Investigational new drugs

authors： Kim GP,Mahoney MR,Szydlo D,Mok TS,Marshke R,Holen K,Picus J,Boyer M,Pitot HC,Rubin J,Philip PA,Nowak A,Wright JJ,Erlichman C

更新日期：2012-02-01 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：:Background The MAPK pathway plays a central role in regulation of several cellular processes, and its dysregulation is a hallmark of biliary tract cancer (BTC). Binimetinib (MEK162), a potent, selective oral MEK1/2 inhibitor, was assessed in patients with advanced BTC. Patients and Methods An expansion cohort study in...

journal_title：Investigational new drugs

authors： Finn RS,Ahn DH,Javle MM,Tan BR Jr,Weekes CD,Bendell JC,Patnaik A,Khan GN,Laheru D,Chavira R,Christy-Bittel J,Barrett E,Sawyer MB,Bekaii-Saab TS

更新日期：2018-12-01 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：: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：:In vitro antitumor effects of human recombinant tumor necrotizing factor (rH-TNF) were examined against nine lung cancer cell lines including six non small and three small cell lung cancer, four stomach cancer cell lines and 30 freshly isolated lung cancer cell samples by the human tumor clonogenic assay. rH-TNF did n...

journal_title：Investigational new drugs

authors： Sasaki Y,Kanzawa F,Takahashi H,Matsushima Y,Nakano H,Nakagawa K,Hong WS,Minato K,Fujiwara Y,Saijo N

更新日期：1987-12-01 00:00:00

abstract：:We studied the effect of riccardin D, a macrocyclic bisbibenzyl, which was isolated from the Chinese liverwort plant, on human leukemia cells and the underlying molecular mechanism. Riccardin D had a significant antiproliferative effect on human leukemia cell lines HL-60, K562 and its multidrug resistant (MDR) counter...

journal_title：Investigational new drugs

authors： Xue X,Qu XJ,Gao ZH,Sun CC,Liu HP,Zhao CR,Cheng YN,Lou HX

更新日期：2012-02-01 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：: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: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：:This report shows that N-acylation of the protein kinase C (PKC) substrate Arg-Lys-Arg-Thr-Leu-Arg-Arg-Leu (RKRTLRRL) provides it with a potent inhibitory activity against PKC. N-myristoyl-RKRTLRRL inhibited Ca2(+)- and phosphatidylserine (PS)-dependent histone phosphorylation catalyzed by PKC with a 50% inhibitory co...

journal_title：Investigational new drugs

authors： O'Brian CA,Ward NE,Liskamp RM,de Bont DB,Earnest LE,van Boom JH,Fan D

更新日期：1991-05-01 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：:Pictilisib (GDC-0941) is an oral class I phosphatidylinositol-3-phosphate kinase inhibitor. This phase Ia/Ib study investigated the safety, tolerability, pharmacokinetics, and pharmacodynamics of pictilisib in monotherapy or in combination with carboplatin-paclitaxel and bevacizumab (CP + BEV) in Japanese patients wit...

journal_title：Investigational new drugs

authors： Yamamoto N,Fujiwara Y,Tamura K,Kondo S,Iwasa S,Tanabe Y,Horiike A,Yanagitani N,Kitazono S,Inatani M,Tanaka J,Nishio M

更新日期：2017-02-01 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：: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：:Preclinical studies, along with Phase I, II, and III clinical trials demonstrate the pharmacokinetics, pharmacodynamics, safety and efficacy of a new drug under well controlled circumstances in relatively homogeneous populations. However, these types of studies generally do not answer important questions about variabi...

journal_title：Investigational new drugs

authors： Blesch KS,Gieschke R,Tsukamoto Y,Reigner BG,Burger HU,Steimer JL

更新日期：2003-05-01 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：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：:Colon cancer is the third most malignant neoplasm in the world and it remains today an important cause of death, especially in western countries. In this study, we have evaluated the chemopreventive efficacy of morin on tissue lipid peroxidation and antioxidant status, which are used as biomarkers in 1,2-dimethylhydra...

journal_title：Investigational new drugs

authors： Sreedharan V,Venkatachalam KK,Namasivayam N

更新日期：2009-02-01 00:00:00