Echinomycin: the first bifunctional intercalating agent in clinical trials.

abstract：PURPOSE:To summarize the safety experience obtained from phase II clinical trials conducted with trabectedin as single-agent therapy in patients with advanced solid tumors. METHODS:This retrospective analysis includes 1,132 patients exposed to trabectedin in 19 phase II trials carried out between February 1999 and Apr...

journal_title：Investigational new drugs

authors： Le Cesne A,Yovine A,Blay JY,Delaloge S,Maki RG,Misset JL,Frontelo P,Nieto A,Jiao JJ,Demetri GD

更新日期：2012-06-01 00:00:00

abstract：:Cyclophosphamide (CPA) is widely used against leukemic and lymphoproliferative diseases, but in vitro studies on response to this agent so far have been limited to instable derivatives with poor galenic properties. ASTA Z 7557 is a newly synthesized "activated cyclophosphamide" that circumvents the need for hepatic ac...

journal_title：Investigational new drugs

authors： Osieka R,Pannenbäcker R,Schmidt CG

更新日期：1984-01-01 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：:Twenty-four evaluable patients with epithelial ovarian cancer resistant to primary therapy, or relapsing after response to initial therapy, were treated with acivicin utilizing a daily X 5 schedule. One patient achieved a partial response lasting five months; the remaining 23 patients showed no objective response. Pro...

journal_title：Investigational new drugs

authors： McGuire WP,Blessing JA,DiSaia PJ,Buchsbaum HJ

更新日期：1986-01-01 00:00:00

abstract：BACKGROUND:We performed a phase I study to determine the dose and safety of everolimus as a combination chemotherapy in peripheral T-cell lymphoma (PTCL). METHODS:Four dose levels (2.5 to 10 mg) of everolimus from days 1 to 14 with CHOP (750 mg/m(2) cyclophosphamide, 50 mg/m(2) doxorubicin, and 1.4 mg/m(2) (maximum 2 ...

journal_title：Investigational new drugs

authors： Kim SJ,Kang HJ,Kim JS,Eom HS,Huh J,Ko YH,Lee J,Yim DS,Lee SY,Park WS,Yang WI,Lee SS,Suh C,Kim WS

更新日期：2013-12-01 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：:T cells are important effectors in anti-tumor immunity, and aberrant expression of B7 family members may contribute to tumor evasion. In this study, we analyzed expression of costimulatory molecules on human hematologic tumor cells and explored whether B7-H3, a member of the B7 superfamily, is an effective target for ...

journal_title：Investigational new drugs

authors： Sun X,Yu Y,Ma L,Xue X,Gao Z,Ma J,Zhang M

更新日期：2020-06-01 00:00:00

abstract：:Background PF-06650808 is a novel anti-Notch3 antibody-drug conjugate (ADC) able to deliver an auristatin-based cytotoxic payload to target cells. In this first-in-human, dose-finding, phase I study (NCT02129205), we investigated safety, pharmacokinetics, immunogenicity, and preliminary antitumor activity of single-ag...

journal_title：Investigational new drugs

authors： Rosen LS,Wesolowski R,Baffa R,Liao KH,Hua SY,Gibson BL,Pirie-Shepherd S,Tolcher AW

更新日期：2020-02-01 00:00:00

abstract：:Capecitabine (N4-pentyloxycarbonyl-5'-deoxy-5-fluorocytidine) is a novel fluoropyrimidine carbamate, which was designed to be sequentially converted to 5-fluorouracil (5-FU) by three enzymes located in the liver and in tumors; the final step is the conversion of 5'-deoxy-5-fluorouridine (5'-DFUR) to 5-FU by thymidine ...

journal_title：Investigational new drugs

authors： Ishitsuka H

更新日期：2000-11-01 00:00:00

abstract：:Pharmacological intervention to reduce CRC mortality entails the use of oral agents that can avert carcinogenesis. Silibinin, a major component of silymarin isolated from Silybum marianum (L.) was found to possess attractive remedial features. An in vivo study was designed to elucidate the effect of silibinin on the f...

journal_title：Investigational new drugs

authors： Sangeetha N,Aranganathan S,Nalini N

更新日期：2010-06-01 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：:Ergot alkaloids are psychoactive and vasoconstricting agents of the fungus Claviceps purpurea causing poisoning such as ergotism in medieval times (St. Anthony's Fire). This class of substances also inhibits tumor growth in vitro and in vivo, though the underlying mechanisms are unclear as yet. We investigated six erg...

journal_title：Investigational new drugs

authors： Mrusek M,Seo EJ,Greten HJ,Simon M,Efferth T

更新日期：2015-02-01 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：:Purpose Hepatic arterial infusion chemotherapy (HAIC) is one of the options to treat unresectable hepatocellular carcinoma (HCC). The majority of HCC patients suffer great pain in the course of HAIC treatment. To improve the quality of life and the efficacy of HAIC treatment, the causes of pain, the choice of an analg...

journal_title：Investigational new drugs

authors： Wu Z,Guo W,Chen S,Zhuang W

更新日期：2020-10-01 00:00:00

abstract：:Peloruside A is a microtubule-stabilizing agent that is currently under investigation as a potential anticancer agent. Peloruside A binds to a site on β-tubulin that is distinct to that of the taxanes (paclitaxel and docetaxel) and the epothilones. An attractive clinical quality of microtubule-stabilizing agents is th...

journal_title：Investigational new drugs

authors： Chan A,Singh AJ,Northcote PT,Miller JH

更新日期：2015-06-01 00:00:00

abstract：:Anthracycline antibiotics (ANT), such as doxorubicin or daunorubicin, are a class of anticancer drugs that are widely used in oncology. Although highly effective in cancer therapy, their usefulness is greatly limited by their cardiotoxicity. Possible mechanisms of ANT cardiotoxicity include their conversion to seconda...

journal_title：Investigational new drugs

authors： Piska K,Koczurkiewicz P,Bucki A,Wójcik-Pszczoła K,Kołaczkowski M,Pękala E

更新日期：2017-06-01 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：:Ninhydrin (2,2-dihydroxy-1,3-indane dione) was evaluated for its antitumor and cytotoxic properties in Ehrlich ascites carcinoma cell (EAC Cell)-bearing mice. The rationale behind this study has been mainly the literature reports of its characteristic interference with DNA synthesis and calcium homeostasis. Antitumor ...

journal_title：Investigational new drugs

authors： Qureshi S,Al-Shabanah OA,Al-Bekairi AM,Al-Harbi MM,Al-Gharably NM,Raza M

更新日期：2000-08-01 00:00:00

abstract：:BMS-754807 is an inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor that also represses aurora kinase. Cancers that express high levels of IGF-1/IGF-1R are sensitive to BMS-754807; however, it shows limited efficacy in non-small cell lung cancer (NSCLC) in which IGF-1R-driven signals may ...

journal_title：Investigational new drugs

authors： Lee SJ,Kim EJ,Lee HJ,Kim SY,Oh SJ,Ryu JS,Moon DH,Ahn JH,Kim SW

更新日期：2013-06-01 00:00:00

abstract：:Fluorinated pyrimidines, particularly 5-fluorouracil (FUra), have been the subject of intense and almost continuous basic and clinical study since development in the late 1950's by Dr. Charles Heidelberger. Despite this intensive effort, the most important mechanisms by which FUra influences tumor growth in individual...

journal_title：Investigational new drugs

authors： Kovach JS,Beart RW Jr

更新日期：1989-04-01 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：: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：:Menogaril, a semisynthetic anthracycline antibiotic, was administered to patients with metastatic adenocarcinoma of the prostate. Forty-five patients with measurable disease and 45 patients with evaluable disease received 150-200 mg/m2 over 1 hour every 28 days. There were three partial responses (PR) among 87 patient...

journal_title：Investigational new drugs

authors： Taylor SA,Blumenstein BA,Stephens RL,Crawford ED,Pistone B,Hill JB

更新日期：1994-01-01 00:00:00

abstract：:Background We determined the safety, pharmacokinetics, pharmacodynamics, and antitumour activity of abexinostat in B-cell lymphoma or chronic lymphocytic leukaemia. Patients and methods Thirty-five patients received oral abexinostat 30, 45, or 60 mg/m(2) bid in a 3 + 3 design in three 21-day schedules: 14 days on trea...

journal_title：Investigational new drugs

authors： Morschhauser F,Terriou L,Coiffier B,Bachy E,Varga A,Kloos I,Lelièvre H,Sarry AL,Depil S,Ribrag V

更新日期：2015-04-01 00:00:00

abstract：PURPOSE:Preclinical data indicate that combination HER2-directed and anti-VEGF therapy may bypass resistance to trastuzumab. A phase I trial was performed to assess safety, activity, and correlates. EXPERIMENTAL DESIGN:Patients with advanced, refractory malignancy were enrolled (modified 3 + 3 design with expansions f...

journal_title：Investigational new drugs

authors： Falchook GS,Moulder S,Naing A,Wheler JJ,Hong DS,Piha-Paul SA,Tsimberidou AM,Fu S,Zinner R,Janku F,Jiang Y,Huang M,Parkhurst KL,Kurzrock R

更新日期：2015-02-01 00:00:00

abstract：:An inflammatory myofibroblastic tumor (IMT) is a rare mesenchymal neoplasm that typically develops in the lungs and seldom in the head and neck region. It is often related to the anaplastic lymphoma kinase (ALK) fusion gene. Crizotinib, a first-generation ALK inhibitor, has been shown to have a notable response in pat...

journal_title：Investigational new drugs

authors： Honda K,Kadowaki S,Kato K,Hanai N,Hasegawa Y,Yatabe Y,Muro K

更新日期：2019-08-01 00:00:00

abstract：INTRODUCTION:Continuous efforts from scientists of diverse fields are necessary not only to better understand the mechanism by which multidrug resistant (MDR) cancer cells occur, but also to boost the discovery of new cytotoxic compounds. This work was designed to assess the cytotoxicity and the mechanism of action of ...

journal_title：Investigational new drugs

authors： Kuete V,Sandjo LP,Djeussi DE,Zeino M,Kwamou GM,Ngadjui B,Efferth T

更新日期：2014-12-01 00:00:00

abstract：:UCN-01 is undergoing Phase I evaluation and is a candidate for combination strategies in the clinic. UCN-01 has been shown to have a variety of effects on cellular targets and the cell cycle. It has also been reported to sensitize cells to several clinical drugs in vitro, possibly in a manner related to p53 status. Th...

journal_title：Investigational new drugs

authors： Monks A,Harris ED,Vaigro-Wolff A,Hose CD,Connelly JW,Sausville EA

更新日期：2000-05-01 00:00:00

abstract：:Fifteen patients with advanced, cisplatin-refractory germ cell tumors (GCT) were treated with iproplatin (CHIP). No objective responses were noted in any of the patients treated. By restricting the entry criteria to heavily pre-treated patients, the identification of new active agents in phase II trials may be hindere...

journal_title：Investigational new drugs

authors： Murphy BA,Motzer RJ,Bosl GJ

更新日期：1992-11-01 00:00:00