Phase I studies of weekly administration of cytotoxic agents: implications of a mathematical model.

abstract：:Aberrant activation of the Wnt/β-catenin signaling pathway promotes osteosarcoma tumorigenesis and metastasis. In this study, we tested the hypothesis that osteosarcoma progression may be delayed by disrupting the Wnt/β-catenin pathway using small molecule inhibitors such as curcumin and PKF118-310. Effective inhibiti...

journal_title：Investigational new drugs

authors： Leow PC,Tian Q,Ong ZY,Yang Z,Ee PL

更新日期：2010-12-01 00:00:00

abstract：:Chemoprevention opens new perspectives in the prevention of cancer and other degenerative diseases. Use of target-organ biological models at the histological and genetic levels can markedly facilitate the identification of potential chemopreventive agents. Our aim was to study the chemopreventive efficacy of pronyl-ly...

journal_title：Investigational new drugs

authors： Panneer Selvam J,Aranganathan S,Nalini N

更新日期：2008-12-01 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：BACKGROUND:TAS-102 is a nucleoside antitumor agent consisting of trifluridine (FTD) and tipiracil hydrochloride (TPI). We investigated the recommended dose (RD) of TAS-102 plus irinotecan for metastatic colorectal cancer refractory to 5-fluorouracil (5-FU) and oxaliplatin. METHODS:This study was used a escalated dose ...

journal_title：Investigational new drugs

authors： Doi T,Yoshino T,Fuse N,Boku N,Yamazaki K,Koizumi W,Shimada K,Takinishi Y,Ohtsu A

更新日期：2015-10-01 00:00:00

abstract：PURPOSE:Amrubicin is a novel 9-aminoanthracycline. This multicenter phase II study was conducted to evaluate the efficacy and safety of amrubicin in patients with non-small-cell lung cancer (NSCLC). PATIENTS AND METHODS:Sixty-one previously untreated patients with stage III or IV NSCLC were entered this study. The pat...

journal_title：Investigational new drugs

authors： Sawa T,Yana T,Takada M,Sugiura T,Kudoh S,Kamei T,Isobe T,Yamamoto H,Yokota S,Katakami N,Tohda Y,Kawakami A,Nakanishi Y,Ariyoshi Y

更新日期：2006-03-01 00:00:00

abstract：:Purpose Anticancer agents are known to increase cancer-associated thrombosis (CAT) onset. CAT onset rate is reported to be 1.92% in cisplatin-based therapy, 6.1% in paclitaxel plus ramucirumab combination therapy, and 11.9% in bevacizumab monotherapy. Because immune checkpoint inhibitors (ICIs) cause a sudden increase...

journal_title：Investigational new drugs

authors： Ando Y,Hayashi T,Sugimoto R,Nishibe S,Ito K,Kawada K,Ikeda Y,Yamada S,Imaizumi K

更新日期：2020-08-01 00:00:00

abstract：:This study sought to measure the degree of synergy induced by specific small molecule inhibitors of DNA-PK [NU7026 and IC486241 (ICC)], a major component of the non-homologous end-joining (NHEJ) pathway, with SN38 or oxaliplatin. Synergy between the DNA damaging drugs and the DNA-PK inhibitors was assessed using the s...

journal_title：Investigational new drugs

authors： Davidson D,Coulombe Y,Martinez-Marignac VL,Amrein L,Grenier J,Hodkinson K,Masson JY,Aloyz R,Panasci L

更新日期：2012-06-01 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：: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：:Purpose Among alkaloids, abundant secondary metabolites in plants, aporphines constitute a class of compounds with interesting biological activities, including anticancer effects. The present study evaluated the anticancer activities of 14 substances, including four aporphine derivatives acquired through the biomonito...

journal_title：Investigational new drugs

authors： Rodrigues-Junior DM,de Almeida Pontes NM,de Albuquerque GE,Carlin V,Perecim GP,Raminelli C,Vettore AL

更新日期：2020-02-01 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：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：:Six patients with incurable malignancies were originally treated with vitamin E, 3200 IU/day for fourteen days, followed by the same dose of vitamin E daily plus LCV (20 mg/m2 i.v. bolus daily x 5) with 5FU (425 mg/m2 i.v. bolus immediately following LCV). The same schedule of LCV and 5FU was repeated 4 weeks later, t...

journal_title：Investigational new drugs

authors： Blanke CD,Stipanov M,Morrow J,Rothenberg M,Chinery R,Shyr Y,Coffey R,Johnson DH,Leach SD,Beauchamp RD

更新日期：2001-01-01 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：:The diarylsulfonylureas have shown promise in xenograft models of childhood cancer. Sulofenur has been evaluated in phase I and II trials in adults with a variety of solid tumors, but the toxicity and maximum tolerated dose of sulofenur in children and adolescents have not been determined. In a phase I study, sulofenu...

journal_title：Investigational new drugs

authors： Pratt CB,Bowman LC,Marina N,Pappo A,Avery L,Luo X,Meyer WH

更新日期：1995-01-01 00:00:00

abstract：PURPOSE:Erlotinib (Tarceva®, OSI-774) is a small molecule inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. As high-grade gliomas frequently show amplification, overexpression and/or mutation of EGFR, this drug has been tested in several clinical trials with glioblastoma patients, but unfortunat...

journal_title：Investigational new drugs

authors： de Vries NA,Buckle T,Zhao J,Beijnen JH,Schellens JH,van Tellingen O

更新日期：2012-04-01 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：: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：: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：BACKGROUND:ASP9521 is a first-in-class orally available inhibitor of the enzyme 17 β-hydroxysteroid dehydrogenase type 5 (17 βHSD5; AKR1C3), catalysing the conversion of dehydroepiandrosterone and androstenedione into 5-androstenediol and testosterone. It has demonstrated anti-tumour activity in in vitro and in vivo pr...

journal_title：Investigational new drugs

authors： Loriot Y,Fizazi K,Jones RJ,Van den Brande J,Molife RL,Omlin A,James ND,Baskin-Bey E,Heeringa M,Baron B,Holtkamp GM,Ouatas T,De Bono JS

更新日期：2014-10-01 00:00:00

abstract：:Angiogenesis is recognized as an important biological process that allows growth of a tumor beyond an initial small size. PTK787/ZK222584, a potent orally active angiogenesis inhibitor capable of inhibiting all known isoforms of Vascular Endothelial Growth Factor (VEGF) receptor, belongs to the class of aminophthalazi...

journal_title：Investigational new drugs

authors： Sharma S,Freeman B,Turner J,Symanowski J,Manno P,Berg W,Vogelzang N

更新日期：2009-02-01 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：:Twenty-four patients with advanced epidermoid carcinoma of the esophagus were treated with trimetrexate (TMTX), a lipid soluble non-classical antifol. Patients were given TMTX 8 mg/m2 intravenously day 1-5 every 28 days. In nine of these patients the dose was escalated to 12 mg/m2 day 1-5 every 28 days. Three patients...

journal_title：Investigational new drugs

authors： Alberts AS,Falkson G,Badata M,Terblanche AP,Schmid EU

更新日期：1988-12-01 00:00:00

abstract：:Epidermal growth factor receptor (EGFR) gene mutations activate the KRAS-RAF-MEK-ERK pathway in lung cancer cells. EGFR tyrosine kinase inhibitors (TKIs) such as gefitinib induce apoptosis of cancer cells, but prolonged treatment is often associated with acquired resistance. Here, we identified a novel MEK1/2 inhibito...

journal_title：Investigational new drugs

authors： Song JY,Kim CS,Lee JH,Jang SJ,Lee SW,Hwang JJ,Lim C,Lee G,Seo J,Cho SY,Choi J

更新日期：2013-12-01 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：: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

abstract：:The aim of this study was to determine the antitumor activity of irofulven when administered in combination with a variety of antimitotic agents. Irofulven in combination with either paclitaxel or docetaxel demonstrated synergistic activity in both the in vitro and in vivo studies. The majority of xenograft bearing an...

journal_title：Investigational new drugs

authors： Kelner MJ,McMorris TC,Rojas RJ,Trani NA,Velasco TR,Estes LA,Suthipinijtham P

更新日期：2002-08-01 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：:Purpose The aim of this study is to detect apoptotic and cytotoxic/antiproliferative effects of a ligand substance and its metal derivatives. The substances were investigated by using an h-ras oncogene transformed rat embryo fibroblast cell line (5RP7). Methods The cytotoxic influences of dipyrido[3,2-a:2',3'c]phenazi...

journal_title：Investigational new drugs

authors： Kaplan A,Benkli K,Koparal AT

更新日期：2018-10-01 00:00:00

abstract：:We have previously shown that the insulinotropic imidazoline compound RX871024 induces death of insulinoma MIN6 cells, an effect involving stimulation of c-Jun N-terminal kinase (JNK) and caspase 3. It has also been reported that AMP-activated protein kinase (AMPK) activates JNK and induces β-cell death. Here we show ...

journal_title：Investigational new drugs

authors： Zaitseva II,Zaitsev SV,Berggren PO

更新日期：2016-08-01 00:00:00