Contributions from emerging transcriptomics technologies and computational strategies for drug discovery.

abstract：:Hepatocellular carcinoma (HCC) is the most prevalent type of tumor among primary liver tumors and is the second highest cause of cancer-related deaths worldwide. Current therapies are controversial, and more research is needed to identify effective treatments. A new synthetic compound, potassium 5-cyano-4-methyl-6-oxo...

journal_title：Investigational new drugs

authors： da Silva EFG,Lima KG,Krause GC,Haute GV,Pedrazza L,Catarina AV,Gassen RB,de Souza Basso B,Dias HB,Luft C,Garcia MCR,Costa BP,Antunes GL,Basso LA,Donadio MVF,Machado P,de Oliveira JR

更新日期：2020-12-01 00:00:00

abstract：:Bryostatin 1 (Bryo) is a naturally occurring macrocyclic lactone with antineoplastic activity. Like the phorbol ester 12-O-tetradecanoyl-phorbol 13-acetate (TPA) it directly activates the calcium- and phospholipid-dependent protein kinase C (PKC), thus generating a number of different cellular responses. We investigat...

journal_title：Investigational new drugs

authors： Steube KG,Grunicke D,Drexler HG

更新日期：1994-01-01 00:00:00

abstract：BACKGROUND:Although its efficacy is unproven, 5-fluorouracil plus cisplatin (FP) is used to prevent postoperative relapse in gastric cancer. We investigated the safety and feasibility of S-1 plus cisplatin (SP) vs. FP for stage IIIB-IV (M0) gastric cancer. METHODS:Following curative resection, 41 stage IIIB-IV (M0) ga...

journal_title：Investigational new drugs

authors： Lee SS,Jeung HC,Chung HC,Noh SH,Hyung WJ,Ahn JY,Rha SY

更新日期：2012-02-01 00:00:00

abstract：:Nafazatrom was tested against a variety of human malignancies with the human tumor stem cell assay at one or more of the following concentrations: 1, 10, 25, and 100 micrograms/ml X 1 h or 0.05, 0.5, or 5 micrograms/ml by continuous exposure. Major (greater than or equal to 70%) inhibition was noted in 7/52 adenocarci...

journal_title：Investigational new drugs

authors： Haas CD,Kyle GW,Crissman JD,Schaldenbrand MF

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：: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：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：:Human topoisomerase II (hTopoII) inhibitors are important chemotherapeutic agents in many different settings including treatment of malignant mesothelioma. Topoisomerase poisons, such as etoposide and doxorubicin, function by trapping the DNA-enzyme covalent complex producing DNA strand breaks which can ultimately lea...

journal_title：Investigational new drugs

authors： Raza A,Jacobson BA,Benoit A,Patel MR,Jay-Dixon J,Hiasa H,Ferguson DM,Kratzke RA

更新日期：2012-08-01 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：:The effect of administering increasing intravenous doses of difluoromethylornithine on human tumor cell polyamine levels was determined in patients with hematologic malignancies. Difluoromethylornithine from 5.5. to 64 gm/m2 per day was administered to nine patients with refractory acute leukemia or multiple myeloma. ...

journal_title：Investigational new drugs

authors： Maddox AM,Freireich EJ,Keating MJ,Frasier-Scott KF,Haddox MK

更新日期：1988-06-01 00:00:00

abstract：BACKGROUND:Although bevacizumab plus FOLFOX is a standard treatment for metastatic colorectal cancer, oxaliplatin must be withdrawn in many patients because of cumulative neurotoxicity. We postulated that a reduced dose of oxaliplatin and modified treatment schedule would prolong the time to treatment failure and evalu...

journal_title：Investigational new drugs

authors： Nakayama N,Sato A,Tanaka S,Shimada K,Konishi K,Sasaki E,Hibi K,Ichikawa H,Kikuchi Y,Sakuyama T,Sekikawa T,Hayashi K,Nishina H,Tokyo Cooperative Oncology Group, Tokyo, Japan.

更新日期：2015-08-01 00:00:00

abstract：:Cis-diaminechloro-[2-(diethylamino) ethyl 4-amino-benzoate, N(4)]-chloride platinum (II) monohydrochloride monohydrate (DPR) is a new platinum triamine complex obtained from the synthesis of cisplatin and procaine. In this paper we analyzed, adopting a disease-oriented strategy, the tumour selectivity of this compound...

journal_title：Investigational new drugs

authors： Mariggiò MA,Cafaggi S,Ottone M,Parodi B,Vannozzi MO,Mandys V,Viale M

更新日期：2004-01-01 00:00:00

abstract：:The population approach has been implemented prospectively in the clinical development of docetaxel (Taxotere). Overall 640 patients were evaluable for the population PK/PD analysis. The PK analysis evidenced significant covariates explaining the inter-patient variability of docetaxel clearance and the PK/PD analysis ...

journal_title：Investigational new drugs

authors： Bruno R,Vivier N,Veyrat-Follet C,Montay G,Rhodes GR

更新日期：2001-05-01 00:00:00

abstract：BACKGROUND:To explore the activity of lapatinib with a novel trial design focused on the drug target rather than on histology. METHODS:Patients with HER2 amplified gastro-esophageal, bladder, ovarian, or uterine tumors were enrolled into a double-blinded randomized discontinuation study of lapatinib 1,500 mg PO daily....

journal_title：Investigational new drugs

authors： Galsky MD,Von Hoff DD,Neubauer M,Anderson T,Fleming M,Nagarwala Y,Mahoney JM,Midwinter D,Vocila L,Zaks TZ

更新日期：2012-04-01 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：: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：BACKGROUND:Lactoferrin is an iron-binding glycoprotein first identified in breast milk as a protein product of mammary epithelial cells. Its immunomodulatory functions include activation of NK and lymphokine-activated killer cells and enhancement of PMN and macrophage cytotoxicity. Studies in animal models have shown p...

journal_title：Investigational new drugs

authors： Hayes TG,Falchook GF,Varadhachary GR,Smith DP,Davis LD,Dhingra HM,Hayes BP,Varadhachary A

更新日期：2006-05-01 00:00:00

abstract：:Mezerein, the most active antitumor compound isolated from the daphne species of plants, has a structural similarity to phorbol myristate acetate (PMA), the major active compound isolated from croton oil. PMA is known to have tumor promoting activity and is a potent inflammatory agent. Mezerein has similarly been repo...

journal_title：Investigational new drugs

authors： Barton K,Randall G,Sagone AL Jr

更新日期：1989-07-01 00:00:00

abstract：:Background This Phase 1b study aimed to determine the recommended Phase 2 dose of LY2334737, an oral pro-drug of gemcitabine, in combination with capecitabine, an oral pro-drug of 5-fluorouracil, in patients with advanced solid tumors. In addition, pharmacokinetics (PK) and tumor response were evaluated. Patients and ...

journal_title：Investigational new drugs

authors： Infante JR,Benhadji KA,Dy GK,Fetterly G,Ma WW,Bendell J,Callies S,Adjei AA

更新日期：2015-04-01 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：: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：:In this multi-institutional phase II study, VM-26 or Teniposide was administered to forty-two patients with advanced colorectal cancer. Patients were initially treated at 60 mg/M2 daily for 5 days with dose adjustments depending on toxicity. One complete response and one partial response were observed lasting six and ...

journal_title：Investigational new drugs

authors： Oishi N,Fleming TR,Laufman L,Ungerleider JS,Natale RB,Einstein AB Jr,Von Hoff DD,Macdonald JS

更新日期：1990-02-01 00:00:00

abstract：UNLABELLED:Although UFT 300 mg/m2/day and leucovorin 90 mg/day administered orally in divided doses administered every 8 hours for 28 days repeated every 35 days could be administered safely to patients with advanced hepatomas and good performance status, this combination and schedule has limited activity in treating a...

journal_title：Investigational new drugs

authors： Mani S,Schiano T,Garcia JC,Ansari RH,Samuels B,Sciortino DF,Tembe S,Shulman KL,Baker A,Benner SE,Vokes EE

更新日期：1998-01-01 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：:The modulation of intracellular nuclear factor-kappaB (NF-κB) signaling pathway involved in the deregulated expression of cell proliferation and cell cycle regulatory molecules is a pragmatic approach for chemoprevention. Eugenol (4-allyl-1-hydroxy-2-methoxybenzene), a natural phenolic constituent of oils of cloves is...

journal_title：Investigational new drugs

authors： Manikandan P,Vinothini G,Vidya Priyadarsini R,Prathiba D,Nagini S

更新日期：2011-02-01 00:00:00

abstract：PURPOSE:DDB (dimethyl-4,4'-dimethoxy-5,6,5'6'-dimethylene dioxybiphenyl-2,2'-dicarboxylate) is a synthetic hepatoprotectant which has been widely used to treat chronic viral hepatitis B patients in China for more than 20 years. In this study, we evaluated DDB as a multidrug resistance (MDR) chemosensitizing agent. MET...

journal_title：Investigational new drugs

authors： Jin J,Sun H,Wei H,Liu G

更新日期：2007-04-01 00:00:00

abstract：:A phase II trial of gemcitabine (Gemzar), a nucleoside analogue with broad activity in solid tumors, was performed in patients with recurrent or metastatic squamous cell carcinoma of the head and neck. A total of 26 eligible patients were registered to receive a dose of 1250 mg/m2 weekly for 3 weeks, followed by a 1 w...

journal_title：Investigational new drugs

authors： Samlowski WE,Gundacker H,Kuebler JP,Giguere JK,Mills GM,Schuller DE,Ensley JF

更新日期：2001-01-01 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：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：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