The molecular mechanism of anticancer action of novel octahydropyrazino[2,1-a:5,4-a']diisoquinoline derivatives in human gastric cancer cells.

abstract：PURPOSE:A phase I study of intraperitoneal paclitaxel (ip PTX) combined with gemcitabine (GEM) plus nab-paclitaxel (nab-PTX) (GnP) was conducted to determine the maximum tolerated dose (MTD) and the recommended dose (RD) in pancreatic cancer patients with peritoneal metastasis in first-line setting. METHODS:Based on t...

journal_title：Investigational new drugs

authors： Takahara N,Nakai Y,Ishigami H,Saito K,Sato T,Hakuta R,Ishigaki K,Saito T,Hamada T,Mizuno S,Kogure H,Yamashita H,Isayama H,Seto Y,Koike K

更新日期：2020-08-08 00:00:00

abstract：:Mitoxantrone (Novantrone; 1, 4-dihydroxy-5, 8-bis [[2-[(2-hydroxyethyl) amino]ethyl]amino-] 9, 10 anthracenedione dihydrochloride (NSC 301739] is a synthetic anthracenedione with intercalating properties. Activity has been shown in preclinical studies in mice bearing intraperitoneal P388 and L1210 leukaemias, ADJ-Pc6 ...

journal_title：Investigational new drugs

authors： Prentice HG,Wimperis JZ,Robbins G

更新日期：1985-01-01 00:00:00

abstract：:This study was designed to test the hypothesis that specific inhibition of cathepsins B and L will cause death of neuroblastoma cells. Five compounds that differ in mode and rate of inhibition of these two enzymes were all shown to cause neuroblastoma cell death. Efficacy of the different compounds was related to thei...

journal_title：Investigational new drugs

authors： Cartledge DM,Colella R,Glazewski L,Lu G,Mason RW

更新日期：2013-02-01 00:00:00

abstract：:Spirogermanium (NSC 192965) is a new metallic investigational anticancer drug of novel heterocyclic structure. Although its mode of action has not been fully elucidated, it appears that spirogermanium is not a phase or cell cycle specific drug and inhibits DNA, RNA and protein synthesis, the protein synthesis being th...

journal_title：Investigational new drugs

authors： Slavik M,Blanc O,Davis J

更新日期：1983-01-01 00:00:00

abstract：:Twenty-four patients with a variety of solid tumors entered a Phase I trial with 4-demethoxydaunorubicin, a new analogue of daunorubicin. The drug was given as a single oral dose of 10-60 mg/m2 repeated every 3-4 weeks. Leukopenia was the dose-limiting toxicity. Other toxic effects included mild to moderate nausea and...

journal_title：Investigational new drugs

authors： Kaplan S,Sessa C,Willems Y,Pacciarini MA,Tamassia V,Cavalli F

更新日期：1984-01-01 00:00:00

abstract：:Based on the high response rates seen among patients with colon cancer receiving high dose Melphalan with autologous marrow infusion, the Southwest Oncology Group conducted a Phase II trial of the compound at a conventional dose. The initial starting dose of 40 mg/m2 was reduced to 30 mg/m2 after severe myelotoxicity ...

journal_title：Investigational new drugs

authors： Knight WA 3rd,Goodman P,Taylor SA,Macdonald JS,Coltman CA Jr,Constanzi JJ,Baker LH

更新日期：1990-01-01 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：:Phosphatidylserine (PS) and other anionic phospholipids, which become exposed on the surface of proliferating endothelial cells, tumor cells and certain leukocytes, have been used as targets for the development of clinical-stage biopharmaceuticals. One of these products (bavituximab) is currently being investigated in...

journal_title：Investigational new drugs

authors： Bujak E,Pretto F,Neri D

更新日期：2015-08-01 00:00:00

abstract：:Major discrepancies concerning risk-benefit assessments and regulatory actions are frequent among regulatory agencies. We explored the differences by scrutinizing a case of gemtuzumab ozogamicin (GO) in patients with acute myeloid leukaemia (AML). Assessment reports of GO were retrieved form the websites of the US Foo...

journal_title：Investigational new drugs

authors： Tanimoto T,Tsubokura M,Mori J,Pietrek M,Ono S,Kami M

更新日期：2013-04-01 00:00:00

abstract：:Background C-Met, which is frequently activated in multiple cancers, has been implicated in tumor formation, progression, metastasis, angiogenesis, and resistance to multiple therapies. MK-8033 is a small-molecule inhibitor of c-Met that binds preferentially to the activated conformation, and has demonstrated anti-tum...

journal_title：Investigational new drugs

authors： Keedy VL,Lenz HJ,Saltz L,Whisenant JG,Berlin JD,Camacho LH

更新日期：2018-10-01 00:00:00

abstract：:Estrogens play a central role in reproductive physiology. The cellular effects of estrogens are mediated by binding to nuclear receptors (ER) which activate transcription of genes involved in cellular growth control. At least two such receptors, designated ERalpha and ERbeta, mediate these effects in conjunction with ...

journal_title：Investigational new drugs

authors： Dhingra K

更新日期：1999-01-01 00:00:00

abstract：:Gemcitabine is a nucleoside analogue with excellent clinical activity against solid tumors. Within the cell, gemcitabine is rapidly phosphorylated to its active di- and triphosphate metabolites. Cytotoxicity with gemcitabine appears to be related to multiple effects on DNA replication, where gemcitabine triphosphate c...

journal_title：Investigational new drugs

authors： Shewach DS,Lawrence TS

更新日期：1996-01-01 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：:A new anthracycline derivative, SM5887, in combination with commonly used anticancer agents was evaluated against T-cell leukemia MOLT-3 and human osteosarcoma MG-63 cell lines in culture. MOLT-3 and MG-63 cells were incubated with various concentrations of 13-hydroxy SM5887 (SM5887-OH, the active metabolite of SM5887...

journal_title：Investigational new drugs

authors： Takagi T,Yazawa Y,Suzuki K,Yamauchi Y,Kano Y

更新日期：1996-01-01 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：:Bombesin/gastrin-releasing peptides (BN/GRP) were shown to bind selectively to cell surface receptors, stimulating the growth of various types of malignancies in murine and human models. The novel BN/GRP synthetic receptor antagonist, RC-3095, was able to produce long-lasting tumor regressions in murine and human tumo...

journal_title：Investigational new drugs

authors： Schwartsmann G,DiLeone LP,Horowitz M,Schunemann D,Cancella A,Pereira AS,Richter M,Souza F,da Rocha AB,Souza FH,Pohlmann P,De Nucci G

更新日期：2006-09-01 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：PURPOSE:ZD0473 (AMD473) [cis-amminedichloro(2-methylpyridine) platinum(II)] is a novel platinum agent of proven activity in vitro against a variety of human tumor-derived cell lines even with intrinsic or acquired resistance to CDDP. The aim of this study is to provide the basis for a rational design of ZD0473-based co...

journal_title：Investigational new drugs

authors： Plasencia C,Abad A,Martinez-Balibrea E,Taron M

更新日期：2004-11-01 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：: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：:An HPLC analytical method was applied to the determination of plasma concentrations of 5,6-dihydro-5-azacytidine (NSC 264880, DHAC) in two foxhounds after a rapid intravenous infusion of 300 mg/kg DHAC. The dose employed is the mouse equivalent LD10 dose which results in mild reversible toxicity in the dog. The declin...

journal_title：Investigational new drugs

authors： Malspeis L,Cheng H,Staubus AE

更新日期：1983-01-01 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：:Introduction BTH1677, a 1,3-1,6 beta-glucan immunomodulator, stimulates a coordinated anti-cancer immune response in combination with anti-tumor antibody therapies. This phase II study explored the efficacy, pharmacokinetics (PK), and safety of BTH1677 combined with cetuximab/carboplatin/paclitaxel in untreated stage ...

journal_title：Investigational new drugs

authors： Thomas M,Sadjadian P,Kollmeier J,Lowe J,Mattson P,Trout JR,Gargano M,Patchen ML,Walsh R,Beliveau M,Marier JF,Bose N,Gorden K,Schneller F 3rd

更新日期：2017-06-01 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：PURPOSE:To evaluate the impact of flutamide on survival of patients with unresectable pancreatic cancer. METHODS:This single institution, randomized, double-blind, placebo controlled study compared flutamide in the dose of 250 mg three times daily (n = 23) versus placebo (n = 23) in patients with histologically proven...

journal_title：Investigational new drugs

authors： Negi SS,Agarwal A,Chaudhary A

更新日期：2006-05-01 00:00:00

abstract：:Compared to doxorubicin, equimolar epirubicin toxicity is reduced by about 50% by the epimerization of a hydrogen and hydroxyl group at the 4' position of the anthracycline sugar moiety. The circadian timing of doxorubicin administration markedly affects its lethal and sub-lethal bone marrow and gut toxicities in mice...

journal_title：Investigational new drugs

authors： Mormont MC,von Roemeling R,Sothern RB,Berestka JS,Langevin TR,Wick M,Hrushesky WJ

更新日期：1988-12-01 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 MET is a tyrosine kinase receptor involved in the regulation of cell proliferation and migration. Reported here are the phase I dose-escalation results for LY2875358, a monoclonal antibody against MET, in Japanese patients with advanced malignancies. Methods The study comprised a 3 + 3 dose-escalation part ...

journal_title：Investigational new drugs

authors： Yoh K,Doi T,Ohmatsu H,Kojima T,Takahashi H,Zenke Y,Wacheck V,Enatsu S,Nakamura T,Turner K,Uenaka K

更新日期：2016-10-01 00:00:00

abstract：:Flavone acetic acid (FAA) was incubated for 1 to 48 hr with 3 established human colon cancer cell lines endowed with distinct degrees of phenotypic properties. All 3 lines responded to FAA in almost identical fashion; when incubated with the drug for only 1 hr, an initial decrease in survival was observed for concentr...

journal_title：Investigational new drugs

authors： Drewinko B,Yang LY

更新日期：1986-01-01 00:00:00

abstract：:N-(phosphonacetyl)-disodium L-aspartic acid (PALA) demonstrates a synergistic antitumor effect when combined with 5-Fluorouracil (5-FU) in in vitro studies. In a Phase II trial, 23 eligible patients with unresectable or metastatic adenocarcinoma of the stomach were treated with weekly i.v. bolus PALA (250 mg/M2) follo...

journal_title：Investigational new drugs

authors： Martino RL,Fleming TR,Morrell LM,Ardalan B,Richman SP,Macdonald JS

更新日期：1996-01-01 00:00:00