Continuing pursuit for ideal systemic anticancer radiotherapeutics.

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：:To explore the clinical significance of the level of HER2/neu gene amplification in a homogenous cohort of 33 patients with HER2-positive metastatic breast cancer (MBC) and available tumor samples treated with a trastuzumab-based regimen, we retrospectively performed dual-color fluorescence in-situ hybridization test ...

journal_title：Investigational new drugs

authors： Gullo G,Bettio D,Torri V,Masci G,Salvini P,Santoro A

更新日期：2009-04-01 00:00:00

abstract：:A retrospective analysis was performed on the medical charts of 160 cancer patients who received esorubicin (ESO or 4'deoxydoxorubicin) in a Phase I clinical trial. The purpose of the review was to characterize the incidence of local venous reactions to this investigational doxorubicin (DOX) analog. The impact of prop...

journal_title：Investigational new drugs

authors： Lee KM,Dorr RT,Robertone A

更新日期：1987-01-01 00:00:00

abstract：:A series of novel 5-(4-methyl-benzylidene)-thiazolidine-2,4-dione derivatives 6 (a-d) and 7 (a-g) were synthesized with different substituted aromatic sulfonyl chlorides (R-SO(2)-Cl) and alkyl halides (R-X) and were characterized by (1)H NMR, LC/MS, FTIR and elemental analyses. All the compounds synthesised were evalu...

journal_title：Investigational new drugs

authors： Chandrappa S,Benaka Prasad SB,Vinaya K,Ananda Kumar CS,Thimmegowda NR,Rangappa KS

更新日期：2008-10-01 00:00:00

abstract：PURPOSE:To investigate the safety, optimal dosing, pharmacokinetics and clinical activity of a regimen of navitoclax (ABT-263) combined with gemcitabine in patients with solid tumors. EXPERIMENTAL DESIGN:Patients with solid tumors for which gemcitabine was deemed an appropriate therapy were enrolled into one of two di...

journal_title：Investigational new drugs

authors： Cleary JM,Lima CM,Hurwitz HI,Montero AJ,Franklin C,Yang J,Graham A,Busman T,Mabry M,Holen K,Shapiro GI,Uronis H

更新日期：2014-10-01 00:00:00

abstract：BACKGROUND:Foretinib is a small-molecule, oral multikinase inhibitor primarily targeting the mesenchymal epithelial transition (MET) factor receptor, and the vascular endothelial growth factor receptor 2. We conducted a phase II study to evaluate the single-agent activity and tolerability of foretinib in patients with ...

journal_title：Investigational new drugs

authors： Seiwert T,Sarantopoulos J,Kallender H,McCallum S,Keer HN,Blumenschein G Jr

更新日期：2013-04-01 00:00:00

abstract：:Androgen receptors are present in both pancreatic cancer tissue and cell lines. Flutamide is a potent antiandrogen widely used in clinical practice for patients with metastatic prostate cancer. This Phase II trial was undertaken to evaluate the impact of flutamide in patients with advanced pancreatic adenocarcinoma wh...

journal_title：Investigational new drugs

authors： Sharma JJ,Razvillas B,Stephens CD,Hilsenbeck SG,Sharma A,Rothenberg ML

更新日期：1997-01-01 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：:Adrenocortical carcinoma (ACC) is an aggressive endocrine cancer with few molecular predictors of malignancy and survival, especially in paediatric patients. Stathmin 1 (STMN1) regulates microtubule dynamics and has been involved in the malignant phenotype of cancer cells. Recently, it was reported that STMN1 is highl...

journal_title：Investigational new drugs

authors： Dos Santos Passaia B,Lima K,Kremer JL,da Conceição BB,de Paula Mariani BM,da Silva JCL,Zerbini MCN,Fragoso MCBV,Machado-Neto JA,Lotfi CFP

更新日期：2020-06-01 00:00:00

abstract：:Fifteen patients with advanced carcinoma of the breast who had failed prior chemotherapy, were treated with recombinant gamma interferon at a dose of 2mg/m2 (1mg = 2.4 X 10(7) international units) intravenously for five consecutive days every other week. The median patient age was 51 and all patients had a performance...

journal_title：Investigational new drugs

authors： Muss HB,Caponera M,Zekan PJ,Jackson DV Jr,Stuart JJ,Richards F,Cooper MR,Levin EA,Reich SD,Capizzi RL

更新日期：1986-01-01 00:00:00

abstract：INTRODUCTION:This multicenter, open-label, phase II study was carried out to compare the efficacy and safety of cilengitide (EMD 121974), a selective inhibitor of the cell-surface integrins αVβ3 and αVβ5, with that of docetaxel in patients with advanced non-small-cell lung cancer (NSCLC). METHODS:Patients (n = 140) wi...

journal_title：Investigational new drugs

authors： Manegold C,Vansteenkiste J,Cardenal F,Schuette W,Woll PJ,Ulsperger E,Kerber A,Eckmayr J,von Pawel J

更新日期：2013-02-01 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：:Breast cancer is commonly treated with anti-estrogens or aromatase inhibitors, but resistant disease eventually develops and new therapies for such resistance are of great interest. We have previously isolated several tamoxifen-resistant variant sub-lines of the MCF-7 breast cancer cell line and provided evidence that...

journal_title：Investigational new drugs

authors： Leung E,Rewcastle GW,Joseph WR,Rosengren RJ,Larsen L,Baguley BC

更新日期：2012-12-01 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：PURPOSE:Vorinostat (V) at levels >2.5 µM enhances chemotherapy in vitro. Yet the approved oral dose of 400 mg inconsistently achieves this level in patients. We developed an intermittent oral pulse-dose schedule of V to increase serum levels. We combined V with the cyclin dependent kinase inhibitor flavopiridol (F) whi...

journal_title：Investigational new drugs

authors： Dickson MA,Rathkopf DE,Carvajal RD,Grant S,Roberts JD,Reid JM,Ames MM,McGovern RM,Lefkowitz RA,Gonen M,Cane LM,Dials HJ,Schwartz GK

更新日期：2011-10-01 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：:Objective The aim of the current study was to examine the anticancer activity and the detailed mechanism of novel diisoquinoline derivatives in human gastric cancer cells (AGS). Methods The viability of AGS cells was measured by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. Cell cycle analy...

journal_title：Investigational new drugs

authors： Pawłowska N,Gornowicz A,Bielawska A,Surażyński A,Szymanowska A,Czarnomysy R,Bielawski K

更新日期：2018-12-01 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：: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：:As HER2 is a client protein of the molecular chaperone Hsp90, targeting Hsp90 may be beneficial in HER2-positive breast cancer. In this study, the activity of the Hsp90 inhibitor NVP-AUY922 was assessed in HER2 overexpressing breast cancer cell lines, including two cell line models of acquired trastuzumab-resistance. ...

journal_title：Investigational new drugs

authors： Canonici A,Qadir Z,Conlon NT,Collins DM,O'Brien NA,Walsh N,Eustace AJ,O'Donovan N,Crown J

更新日期：2018-08-01 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：:The matrix metalloproteinases (MMPs) are a family of at least fifteen secreted and membrane-bound zinc-endopeptidases. Collectively, these enzymes can degrade all of the components of the extracellular matrix, including fibrallar and non-fibrallar collagens, fibronectin, laminin and basement membrane glycoproteins. MM...

journal_title：Investigational new drugs

authors： Wojtowicz-Praga SM,Dickson RB,Hawkins MJ

更新日期：1997-01-01 00:00:00

abstract：:L1210 leukemia cells, because of their rapid growth rate in suspension culture and high growth fraction, are ideally suited to screen in vitro for cytotoxic compounds. Although L1210 cells may mimic rapidly growing tumors, they have not been effective in selecting agents active against slow growing solid tumors. We ex...

journal_title：Investigational new drugs

authors： Badiner GJ,Hamilton RD,Li LH,Bhuyan BK

更新日期：1987-01-01 00:00:00

abstract：:Neuroblastoma is an extracranial, solid, and heterogeneous malignancy in children. The conventional therapeutic modalities are mostly ineffective and thus new therapeutic strategies for malignant neuroblastoma are urgently warranted. We examined the synergistic efficacy of combination of sorafenib (SF) and genistein (...

journal_title：Investigational new drugs

authors： Roy Choudhury S,Karmakar S,Banik NL,Ray SK

更新日期：2010-12-01 00:00:00

abstract：PURPOSE:The transcription factor nuclear factor-kB (NFkB) is implicated in gastric cancer carcinogenesis and survival, and its inhibition by proteosome inhibition is associated with preclinical gastric cancer anti-tumor activity. We examined the single agent efficacy of bortezomib, a selective proteasome inhibitor, in ...

journal_title：Investigational new drugs

authors： Shah MA,Power DG,Kindler HL,Holen KD,Kemeny MM,Ilson DH,Tang L,Capanu M,Wright JJ,Kelsen DP

更新日期：2011-12-01 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：:Infantile hemangioma is the most common vascular tumor of childhood. It is characterized by clinical expansion of endothelial cells and promoted by angiogenic factors. Luteolin is a flavonoid compound that carries anti-cancer and anti-angiogenesis properties. The study aimed to investigate the effect of luteolin in tr...

journal_title：Investigational new drugs

authors： Dai Y,Zheng H,Liu Z,Wang Y,Hu W

更新日期：2021-01-07 00:00:00

abstract：:VEGF signaling through VEGFR-2 is the major factor in glioblastoma angiogenesis. CT-322, a pegylated protein engineered from the 10th type III human fibronectin domain, binds the VEGFR-2 extracellular domain with high specificity and affinity to block VEGF-induced VEGFR-2 signaling. This study evaluated CT-322 in an o...

journal_title：Investigational new drugs

authors： Schiff D,Kesari S,de Groot J,Mikkelsen T,Drappatz J,Coyle T,Fichtel L,Silver B,Walters I,Reardon D

更新日期：2015-02-01 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：:Chemotherapy has always been the first therapeutic option for patients with advanced non-small cell lung cancer (NSCLC) with untreatable oncogenic mutations. However, chemotherapy has demonstrated limited success and is associated with severe side effects. This research aimed to investigate the antitumor efficacy and ...

journal_title：Investigational new drugs

authors： Han J,Zhao Y,Zhao X,Ma T,Hao T,Liu J,Zhang Z,Zhang J,Wang J

更新日期：2020-08-01 00:00:00